Antibody Information
General Information of This Antibody
Antibody ID | ANI0FIZAK |
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Antibody Name | Trastuzumab |
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Brand Name | HERCEPTIN |
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Organization | Genentech, Inc.; Roche Holding AG; Roche, F. Hoffmann-La Roche Ltd. |
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Indication | Gastric cancer; Breast cancer; Colorectal cancer |
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Approval Date | Sep. 1998 |
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Synonyms |
4D5V8; ABP980; ABP 980; ABP-980; ABP-980 (TRASTUZUMAB BIOSIMILAR); BMAB-200; CANHERA; DMB-3111; DMB-3111 (TRASTUZUMAB BIOSIMILAR); EG12014; EG-12014; EG-12014 (TRASTUZUMAB BIOSIMILAR); EG12014 TRASTUZUMAB BIOSIMILAR; HERZUMA; HLX02; HLX 02; HLX-02; HLX-02 TRASTUZUMAB BIOSIMILAR; KANJINTI; OGIVRI; ONTRUZANT; PF-05280014; R-597; RHUMAB HER2; RO0452317; RO-0452317; SB-3 (TRASTUZUMAB BIOSIMILAR); SYD977; SYD-977; TRASTUZUMAB; TRASTUZUMAB ANNS; TRASTUZUMAB-ANNS; TRASTUZUMAB BETA; TRASTUZUMAB BIOSIMILAR (ABP-980); TRASTUZUMAB DKST; TRASTUZUMAB-DKST; TRASTUZUMAB DTTB; TRASTUZUMAB-DTTB; TRASTUZUMAB (HERCEPTIN); TRASTUZUMAB-PFIZER; TRASTUZUMAB PKRB; TRASTUZUMAB-PKRB; TRASTUZUMAB QYYP; TRASTUZUMAB-QYYP; TRASTUZUMAB-ZZXF; TRAZIMERA; ZERCEPAC
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Antibody Type | Monoclonal antibody (mAb) |
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Antibody Subtype | Humanized IgG1-kappa |
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Antigen Name | Receptor tyrosine-protein kinase erbB-2 (ERBB2) |
Antigen Info | ||||
ChEMBI ID | ||||||
PDB ID | ||||||
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Drug Central ID | ||||||
Click to Show/Hide the Sequence Information of This Antibody | ||||||
Heavy Chain Sequence |
EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY
ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGG PSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYN STYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREE MTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRW QQGNVFSCSVMHEALHNHYTQKSLSLSPGK Click to Show/Hide
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Heavy Chain Varible Domain |
EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY
ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS Click to Show/Hide
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Heavy Chain Constant Domain 1 |
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKV Click to Show/Hide
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Heavy Chain Constant Domain 2 |
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK Click to Show/Hide
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Heavy Chain Constant Domain 3 |
GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS
DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK Click to Show/Hide
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Heavy Chain Hinge Region |
EPKSCDKTHTCPPCP
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Heavy Chain CDR 1 |
GFNIKDTY
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Heavy Chain CDR 2 |
IYPTNGYT
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Heavy Chain CDR 3 |
SRWGGDGFYAMDY
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Light Chain Sequence |
DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS
RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide
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Light Chain Varible Domain |
DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS
RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIK Click to Show/Hide
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Light Chain Constant Domain |
RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD
SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide
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Light Chain CDR 1 |
QDVNTA
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Light Chain CDR 2 |
SAS
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Light Chain CDR 3 |
QQHYTTPPT
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The Activity Data of This Antibody
Antibody Activity Information 1 | [1] | |||||
Half Maximal Effective Concentration (EC50)
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1.35
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nM
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Antibody Function | Confirm the effect of the drug conjugation with the anti-HER2 (Trastuzumab) Ab on binding activity to HER2. | |||||
Antibody Antigen Binding Assay | Evaluate the antigen binding capacity of our ADC by indirect ELISA binding assay. |
Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
Trastuzumab emtansine [Approved]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
Efficacy Data | Objective Response Rate (ORR) |
21.40%
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Positive HER2 expression (HER2 +++/++) | ||
Patients Enrolled |
Untreated, asymptomatic BM or controlled brain disease treated with radiotherapy >14 days before enrollment; had received prior HER2-targeted therapy and chemotherapy; and had progressed on or after their most recent treatment of advanced breast cancer.
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Administration Dosage |
3.6 mg/kg intravenously every 3 weeks.
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Related Clinical Trial | |||||
NCT Number | NCT01702571 | Clinical Status | Phase 3 | ||
Clinical Description |
A two-cohort, open-label, multicenter study of trastuzumab emtansine (T-DM1) in HER2-positive locally advanced or metastatic breast cancer patients who have received prior anti-HER2 and chemotherapy-based treatment.
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Primary Endpoint |
Objective response rate=21.40% (95% CI 14.60-29.60), clinical benefit rate=42.90% (95% CI 34.10-52.00).
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Other Endpoint |
Median PFS=5.50 months (95% CI, 5.30-5.60), overall survival =18.90 months (95% CI, 17.10-21.30).
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Experiment 2 Reporting the Activity Date of This ADC | [6] | ||||
Efficacy Data | Objective Response Rate (ORR) |
5.10%
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Positive HER2 expression (HER2+++/++) | ||
Patients Enrolled |
HER2 positive advanced urothelial bladder cancer or pancreatic cancer/cholangiocarcinoma
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Administration Dosage |
Received singleagent TDM1 2.4 mg/kg once weekly (qw) or 3.6 mg/kg every 3 weeks (q3w).
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Related Clinical Trial | |||||
NCT Number | NCT02999672 | Clinical Status | Phase 2 | ||
Clinical Description |
A study to determine best tumor response with trastuzumab emtansine in human epidermal growth factor receptor 2 (HER2) overexpressing solid tumors (KAMELEON).
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Primary Endpoint |
BOR, Urothelial bladder cancer (n=13); PR N=5 (38.46%);SD N=1 (7.7%);PD N=6 (46.2%);NE N=1 (7.69%). Pancreatic cancer/cholangiocarcinoma (n=7) PR N=1 (14.29%);SD N=3 (42.86%);PD N=2 (28.57%); NE N=1 (14.29%).
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Other Endpoint |
PFS, Urothelial bladder cancer (n=13), Median PFS, months (95% CI) 2.20 (1.18-4.30), Median OS, months (95% CI) 7.03 (3.75-NE). Pancreatic cancer/cholangiocarcinoma (n=7), Median PFS, months (95% CI) 2.58 (1.31-9.99), Median OS, months (95% CI) NE (1.45-NE).
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Experiment 3 Reporting the Activity Date of This ADC | [7] | ||||
Efficacy Data | Objective Response Rate (ORR) |
5.60% (Day 21)
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Patients Enrolled |
38 patients were enrolled and 36 included in efficacy analysis.Patients were treated with the standard intravenous dosing of T- DM1, that is 3.6mg/kg every 3 weeks for a 21-day cycle.
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Administration Dosage |
3.6 mg/kg every 3 weeks for a 21-day cycle, until toxicity or progression.
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Related Clinical Trial | |||||
NCT Number | NCT02465060 | Clinical Status | Phase 2 | ||
Clinical Description |
Targeted therapy directed by genetic testing in treating patients with advanced refractory solid tumors, lymphomas, or multiple myeloma (the MATCH screening trial).
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Primary Endpoint |
ORR was 2/36 (5.56%) with 90% confidence interval (90% CI, 1.00% to 16.50%)
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Other Endpoint |
6-mouth sPFS=23.60%.
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Experiment 4 Reporting the Activity Date of This ADC | [9] | ||||
Efficacy Data | Objective Response Rate (ORR) |
45.00%
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Positive HER2 expression (HER2 +++/++) | ||
Patients Enrolled |
An Eastern Cooperative Oncology Group performance status of 0 or 1 and centrally confirmed, measurable, HER2-positive advanced breast cancer previously treated with trastuzumab and a taxane.
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Administration Dosage |
3.6 mg/kg ( trastuzumab emtansine) and 1200 mg (Atezolizumab) intravenously every 3 weeks.
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Related Clinical Trial | |||||
NCT Number | NCT02924883 | Clinical Status | Phase 2 | ||
Clinical Description |
A randomized, multicenter, double-blind, placebo-controlled phase II study of the efficacy and safety of trastuzumab emtansine in combination with atezolizumab or atezolizumab-placebo in patients with HER2-positive locally advanced or metastatic breast cancer who have received prior trastuzumab and taxane based therapy.
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Primary Endpoint |
Median PFS=8.20 months (95% CI 5.80-10.70).
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Other Endpoint |
Median overall survival was not estimable (95% CI NE-NE); Objective response rate=45.00% (95% CI 28.06-50.30).
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Experiment 5 Reporting the Activity Date of This ADC | [14] | ||||
Efficacy Data | Objective Response Rate (ORR) |
20.00%
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High HER2 expression (HER2+++) | ||
Patients Enrolled |
HER2-positive, metastatic breast cancer previously treated with taxane, trastuzumab, and pertuzumab, and were T-DM1-nave.
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Administration Dosage |
The study consisted of a dose de-escalation (dose-finding) cohort, followed by an expansion cohort at the recommended phase II dose (RP2D), T-DM1 3.60 mg/kg intravenously every 21 days, and pembrolizumab 200mg intravenously every 21 days, if one or fewer DLTs were noted in the first six patients at that dose level, it would be declared the RP2D.
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Related Clinical Trial | |||||
NCT Number | NCT03032107 | Clinical Status | Phase 1b | ||
Clinical Description |
A phase 1b study of pembrolizumab in combination with trastuzumab-dm1 in metastatic HER2-positive breast cancer.
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Primary Endpoint |
OrR=20.00% (95% CI 5.70%-43.70%), and median PFS=9.60 months (95%CI 2.80-16.00 months).
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Other Endpoint |
There were no dose-limiting toxicities. The RP2D was 3.60 mg/kg T-DM1 plus 200 mg pembrolizumab every 21 days.
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Experiment 6 Reporting the Activity Date of This ADC | [17] | ||||
Patients Enrolled |
Newly diagnosed, HER2-positive, nonmetastatic, histologically confirmed, operable primary invasive breast carcinoma.
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Administration Dosage |
T-DM1 was dosed at 3.60 mg/kg once every 3 weeks. Trastuzumab was dosed at 6 mg/kg once every 3 weeks after an 8 mg/kg loading dose and started concurrently with the taxane. Pertuzumab was dosed at 420 mg once every 3 weeks after an 840 mg loading dose and administered concurrently with T-DM1 or trastuzumab-plus-taxane. An interval of 3 weeks from the last dose of anthracycline to initiation of HER2-targeted therapy was required. After the taxane-concurrent phase in the trastuzumab-containing arm, trastuzumab-plus-pertuzumab was continued for 1 year. In the T-DM1containing arm, T-DM1-plus-pertuzumab was continued for 1 year.
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Related Clinical Trial | |||||
NCT Number | NCT01966471 | Clinical Status | Phase 3 | ||
Clinical Description |
A randomized, multicenter, open-label, phase 3 trial comparing trastuzumab plus pertuzumab plus a taxane following anthracyclines versus trastuzumab emtansine plus pertuzumab following anthracyclines as adjuvant therapy in patients with operable HER2-positive primary breast cancer.
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Primary Endpoint |
82 (9.90%) IDFS events had occurred in the AC-THP arm and 80 (9.60%) had occurred in the AC-KP arm.
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Other Endpoint |
3-year IDFS rates were 94.10% (95% CI, 92.50 to 95.70) with AC-THP and 92.80% (95% CI, 91.00 to 94.50) with AC-KP.
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Discovered Using Patient-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 1.10% (Day 28) | Low HER2 expression (HER2+) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | Breast cancer PDX model (PDX: ST565) | ||||
Experiment 2 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 19.20% (Day 28) | Low HER2 expression (HER2+) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | Breast cancer PDX model (PDX: ST313) | ||||
Experiment 3 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 37.60% (Day 28) | High HER2 expression (HER2+++) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | Gastric cancer PDX model (PDX model: NIBIO G016) | ||||
Experiment 4 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.20% (Day 21) | Moderate HER2 expression (HER2++) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | Breast cancer PDX model (PDX: ST225) | ||||
Experiment 5 Reporting the Activity Date of This ADC | [19] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.40% | Positive HER2 expression (HER2+++/++) | ||
Method Description |
T-DM1 (Genentech) was administered i.p. at 10 mg/kg once per week.
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In Vivo Model | Breast cancer PDX model (PDX: PDX12) |
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 7.10% (Day 21) | Low HER2 expression (HER2+) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; CFPAC-1 (low-expression). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | CFPAC-1 cell line xenograft model | ||||
In Vitro Model | Pancreatic ductal adenocarcinoma | CFPAC-1 cells | CVCL_1119 | ||
Experiment 2 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 15.50% (Day 7) | High HER2 expression (HER2+++) | ||
Method Description |
The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 1 mg/kg trastuzmab-MCC-DM1.
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In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
Experiment 3 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 27.10% (Day 48) | High HER2 expression (HER2+++) | ||
Method Description |
Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 0.3 mg/kg for a total of three injections.
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In Vivo Model | Trastuzumab-resistant breast cancer CDX model | ||||
In Vitro Model | Invasive breast carcinoma of no special type | BT-474 EEI cells | CVCL_AR96 | ||
Experiment 4 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 31.70% (Day 21) | Low HER2 expression (HER2+) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; Capan-1 (weak positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | Capan-1 cell line xenograft model | ||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 5 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 33.10% (Day 21) | Negative HER2 expression (HER2-) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; GCIY (negative). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | GCIY cell line xenograft model | ||||
In Vitro Model | Gastric adenocarcinoma | GCIY cells | CVCL_1228 | ||
Experiment 6 Reporting the Activity Date of This ADC | [22] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 36.00% (Day 33) | Moderate HER2 expression (HER2++) | ||
Method Description |
Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
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In Vivo Model | HT29 CDX model | ||||
In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
Experiment 7 Reporting the Activity Date of This ADC | [22] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 36.00% (Day 33) | Low HER2 expression (HER2 +) | ||
Method Description |
SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
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In Vivo Model | SW48 CDX model | ||||
In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 | ||
Experiment 8 Reporting the Activity Date of This ADC | [23] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 42.00% (Day 58) | Low HER2 expression (HER2 +) | ||
Method Description |
11-18 cells (4,000,000 ) and HCC827 cells (2,000,000 ) were injected subcutaneously into the backs on both sides of the mice. T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
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In Vivo Model | 11-18 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | 11-18 cells | CVCL_6659 | ||
Experiment 9 Reporting the Activity Date of This ADC | [23] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 42.00% (Day 58) | Low HER2 expression (HER2+) | ||
Method Description |
Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
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In Vivo Model | 11-18 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | 11-18 cells | CVCL_6659 | ||
Experiment 10 Reporting the Activity Date of This ADC | [24] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 43.30% (Day 30) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Trastuzumab-emtansine (3 mg/kg, every seven days 4) induces efficient tumor cell killing in cell line-derived models of BT-474/R1-7 cells with HER2 expression with high expression.
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In Vivo Model | BT-474 CDX model (T-DM1 resistant) | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells (Trastuzumab emtansine resistant) | CVCL_0179 | ||
Experiment 11 Reporting the Activity Date of This ADC | [24] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 45.00% (Day 21) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Trastuzumab-emtansine (3 mg/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of SK-OV-3 cells with HER2 expression with high expression.
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In Vivo Model | SK-OV-3 CDX model (Expressing YES1 Y537F) | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells (YES1 Y537F expression) | CVCL_0532 | ||
Experiment 12 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 45.50% (Day 48) | High HER2 expression (HER2+++) | ||
Method Description |
Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 1 mg/kg for a total of three injections.
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In Vivo Model | Trastuzumab-resistant breast cancer CDX model | ||||
In Vitro Model | Invasive breast carcinoma of no special type | BT-474 EEI cells | CVCL_AR96 | ||
Experiment 13 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 46.20% (Day 7) | High HER2 expression (HER2+++) | ||
Method Description |
The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 3 mg/kg trastuzmab-MCC-DM1.
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In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
Experiment 14 Reporting the Activity Date of This ADC | [22] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 55.00% (Day 33) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
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In Vivo Model | HT-29 CDX model | ||||
In Vitro Model | Colon adenocarcinoma | HT-29 cells | CVCL_0320 | ||
Experiment 15 Reporting the Activity Date of This ADC | [22] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 55.00% (Day 33) | Moderate HER2 expression (HER2 ++) | ||
Method Description |
SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
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In Vivo Model | HT-29 CDX model | ||||
In Vitro Model | Colon adenocarcinoma | HT-29 cells | CVCL_0320 | ||
Experiment 16 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 58.50% (Day 21) | Moderate HER2 expression (HER2++) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; JIMT-1 (moderate positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | JIMT-1 cell line xenograft model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 17 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 58.70% (Day 48) | High HER2 expression (HER2+++) | ||
Method Description |
Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 3 mg/kg for a total of three injections.
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In Vivo Model | Trastuzumab-resistant breast cancer CDX model | ||||
In Vitro Model | Invasive breast carcinoma of no special type | BT-474 EEI cells | CVCL_AR96 | ||
Experiment 18 Reporting the Activity Date of This ADC | [23] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 63.00% (Day 58) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
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In Vivo Model | H3255 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H3255 cells | CVCL_6831 | ||
Experiment 19 Reporting the Activity Date of This ADC | [23] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 63.00% (Day 58) | High HER2 expression (HER2 +++) | ||
Method Description |
T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks,.
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In Vivo Model | H3255 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H3255 cells | CVCL_6831 | ||
Experiment 20 Reporting the Activity Date of This ADC | [22] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 63.30% (Day 33) | High HER2 expression (HER2 +++) | ||
Method Description |
SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
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In Vivo Model | LS174T CDX model | ||||
In Vitro Model | Colon adenocarcinoma | LS174T cells | CVCL_1384 | ||
Experiment 21 Reporting the Activity Date of This ADC | [23] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 66.70% (Day 51) | Low HER2 expression (HER2+) | ||
Method Description |
Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
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In Vivo Model | HCC827 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 | ||
Experiment 22 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 74.00% (Day 7) | High HER2 expression (HER2+++) | ||
Method Description |
The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 10 mg/kg trastuzmab-MCC-DM1.
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In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
Experiment 23 Reporting the Activity Date of This ADC | [25] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 76.54% (Day 24) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (1 mg/kg) via the tail vein on Day 0.
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In Vivo Model | KPL-4 CDX model | ||||
In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 24 Reporting the Activity Date of This ADC | [25] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 82.90% (Day 24) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 5 mg/kg) via the tail vein on Day 0.
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In Vivo Model | KPL-4 CDX model | ||||
In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 25 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 83.90% (Day 10) | High HER2 expression (HER2+++) | ||
Method Description |
Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
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In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
Experiment 26 Reporting the Activity Date of This ADC | [25] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 84.39% (Day 24) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 1 mg/kg) via the tail vein on Day 0.
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In Vivo Model | KPL-4 CDX model | ||||
In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 27 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 88.70% (Day 7) | High HER2 expression (HER2+++) | ||
Method Description |
The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 15 mg/kg trastuzmab-MCC-DM1.
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In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
Experiment 28 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.10% (Day 7) | High HER2 expression (HER2+++) | ||
Method Description |
The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 30 mg/kg trastuzmab-MCC-DM1.
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In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
Experiment 29 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.70% (Day 48) | High HER2 expression (HER2+++) | ||
Method Description |
Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 10 mg/kg for a total of three injections.
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In Vivo Model | Trastuzumab-resistant breast cancer CDX model | ||||
In Vitro Model | Invasive breast carcinoma of no special type | BT-474 EEI cells | CVCL_AR96 | ||
Experiment 30 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.30% (Day 14) | High HER2 expression (HER2+++) | ||
Method Description |
KPL-4 human breast tumor cells were inoculated (3 million cells per mouse, in Matrigel) into the mammary fat pads of SCID beige mice. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Trastuzumab-maytansinoid conjugates were given by single 15 mg/kg iv injection.
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In Vivo Model | Breast cancer CDX model | ||||
In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 31 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.70% (Day 48) | High HER2 expression (HER2+++) | ||
Method Description |
Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 15 mg/kg for a total of three injections.
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In Vivo Model | Trastuzumab-resistant breast cancer CDX model | ||||
In Vitro Model | Invasive breast carcinoma of no special type | BT-474 EEI cells | CVCL_AR96 | ||
Experiment 32 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.40% (Day 21) | High HER2 expression (HER2+++) | ||
Method Description |
The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; KPL-4 (strong positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.
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In Vivo Model | KPL-4 cell line xenograft model | ||||
In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 33 Reporting the Activity Date of This ADC | [26] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 56) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
HER2-positive HCC1954 cells were either treated with vehicle (control) or T-DM1 for 5 days, trypsinized, washed in PBS and sorted by flow cytometry based on the surface ROR1 expression. ROR1- and ROR1+ or unfractionated cells were injected into the subcutaneous site of 6-8-week old Nu/J mice (n=3/group).
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In Vivo Model | HCC1954 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
Experiment 34 Reporting the Activity Date of This ADC | [27] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 35) | High HER2 expression (HER2+++) | ||
Method Description |
Mice were inoculated subcutaneously in the right flank with either 5x106 cells/mouse of BTC cell line KKU-100, mice were randomized to the control group or treatment with T-DM1 20 mg/kg groups.
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In Vivo Model | KMCH-1 CDX model | ||||
In Vitro Model | Combined hepatocellular carcinoma and cholangiocarcinoma | KMCH-1 cells | CVCL_7970 | ||
Experiment 35 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Minimal Effective Dose (MED) | < 5.00 mg/kg | Moderate HER2 expression (HER2++) | ||
Method Description |
Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: two T-DM1 groups, treated with 20 mg/kg and 60 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
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In Vivo Model | Gastric cancer CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 36 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Maximum Tolerated Dose (MTD) | > 20.00 mg/kg | High HER2 expression (HER2+++) | ||
Method Description |
Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: two T-DM1 groups, treated with 20 mg/kg and 60 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
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In Vivo Model | Gastric cancer CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Obtained from the Model Organism Data
Experiment 1 Reporting the Activity Date of This ADC | [29] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.98% (Day 7) | High HER2 expression (HER2 +++) | ||
Method Description |
An allograft was propagated from the Fo5 mmty transgenic mouse which does not respond to.or responds poorly to HERCEPTIN therapy. Subjects were treated once with ADC (10 mg/kg); and placebo PBS buffer control (Vehicle) andmonitored over 3 weeks.
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In Vivo Model | Breast cancer model MMTV-HER2 Fo5 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [31] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 nM±0.12 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [31] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.57 nM±0.10 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 6 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.76 nM
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Moderate HER2 expression (HER2 ++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 7 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.71 nM
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Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 8 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.26 nM
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High HER2 expression (HER2+++) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 9 Reporting the Activity Date of This ADC | [31] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.89 nM±3.51 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 10 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.40 nM±4.80 nM
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Positive HER2 expression (HER2 +++/++) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 11 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
18.37 nM
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Low HER2 expression (HER2+; IHC 1+) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 12 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 13 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 14 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
220.00 nM±39.50 nM
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Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 15 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
317.00 nM±93.70 nM
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Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 | ||
Experiment 16 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 17 Reporting the Activity Date of This ADC | [29] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.00-15.00 ng/mL
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High HER2 expression (HER2+++) | ||
Method Description |
Exposing mammalian cells having HER2 receptors to ADC in a cell culture medium; culturing the cells for a period from about 6 hours to about 5 days; and measuring cell viability Cell-based in vitro assays were used to measure viability, cytotoxicity, and induction of apoptosis of the ADC of the invention.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 18 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.00 ug/mL
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Negative HER2 expression (HER2-) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Invasive breast carcinoma of no special type | BT-474 EEI cells | CVCL_AR96 | ||
Experiment 19 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.01 ug/mL
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Moderate HER2 expression (HER2++; IHC 2+) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 20 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.01 ug/mL
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Positive HER2 expression (HER2+++/++; HER2 MFI=95.7) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 21 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 ug/mL
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High HER2 expression (HER2+++) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
Experiment 22 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 ug/mL
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High HER2 expression (HER2+++) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Experiment 23 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 ug/mL
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Low HER2 expression (HER2+) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Gastric tubular adenocarcinoma | MKN7 cells | CVCL_1417 |
Trastuzumab deruxtecan [Approved]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
Efficacy Data | Objective Response Rate (ORR) |
52.90% (In HR+ cohort)
52.30% (In HR+ and HR- cohort) |
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Patients Enrolled |
HER2-low metastatic breast cancer who had received one or two previous lines of chemotherapy.
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Administration Dosage |
Intravenously every 3 weeks at a dose of 5.40 mg per kilogram of body weight.
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Related Clinical Trial | |||||
NCT Number | NCT03734029 | Clinical Status | Phase 3 | ||
Clinical Description |
A phase 3, multicenter, randomized, open-label, active controlled trial of DS-8201a, an Anti-HER2-antibody drug conjugate (ADC), versus treatment of physician's choice for HER2-low, unresectable and/or metastatic breast cancer subjects.
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Primary Endpoint |
In HR+ cohort, for ENHERTU (N=331), median Progression-Free Survival (mFPS)=10.10 months (95% Cl 9.50-11.50), for Chemotherapy (N=163), median Progression-Free Survival (mFPS)=5.40 months(95% Cl 4.40-7.10), hazard radio=0.51 (95% Cl 0.40-0.64) and p-value<0.0001.
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Other Endpoint |
In HR+ cohort, for ENHERTU (N=331), median overall survival (months)=23.90 (95% Cl 20.80-24.80), Confirmed Objective Response Rate=52.90% (95% Cl 47.30-58.40), Complete Response rate=36.00%, Partial Response rate= 49.50%, median Duration of Response (months)=10.70 (95% Cl 8.50-13.70); for Chemotherapy (N=163), median overall survival (months)=17.50 (95% Cl 15.20-24.80), Confirmed Objective Response Rate=16.60% (95% Cl 11.20-23.20), Complete Response rate=0.60%, Partial Response rate= 16.00%, median Duration of Response (months)=6.80 (95% Cl 6.50-9.90). In HR+ and HR- cohort, for ENHERTU (N=373), median Progression-Free Survival (mFPS)=9.90 months (95% Cl 9.00-11.30), median overall survival (months) = 23.40 (95% Cl 20.00-24.80), Confirmed Objective Response Rate = 52.30% (95% Cl 47.10-57.40), Complete Response rate=35.00%, Partial Response rate= 49.10%, median Duration of Response(months)=10.70 (95% Cl 8.50-13.20); for Chemotherapy (N=184), median Progression-Free Survival (mFPS)=5.40 months(95% Cl 4.20-6.80), median overall survival (months)=16.80(95% Cl 14.50-20.00), Confirmed Objective Response Rate=16.30% (95% Cl 11.30-22.50), Complete Response rate=11.00%, Partial Response rate= 15.20%, median Duration of Response(months)=6.80 (95% Cl 6.00-9.90).
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Experiment 2 Reporting the Activity Date of This ADC | [4] | ||||
Efficacy Data | Objective Response Rate (ORR) |
79.70%
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Patients Enrolled |
HER2-positive metastatic breast cancer previously treated with trastuzumab and a taxane.
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Administration Dosage |
Intravenously every 3 weeks at a dose of 5.40 mg per kilogram of body weigh.
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Related Clinical Trial | |||||
NCT Number | NCT03529110 | Clinical Status | Phase 3 | ||
Clinical Description |
A phase 3, multicenter, randomized, open-label, active-controlled study of DS-8201a (Trastuzumab Deruxtecan), an Anti-HER2 antibody drug conjugate (ADC), versus Ado Trastuzumab Emtansine (T-DM1) for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with trastuzumab and taxane.
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Primary Endpoint |
For ENHERTU 5.40 mg/kg, Median Progression-Free Survival (mPFS)=not reached (95% Cl 18.5-not estimable); For Ado-trastuzumab emtansine 3.60 mg/kg, Median Progression-Free Survival (mPFS)=6.80months (95% Cl 5.60-8.20), hazard radio=0.28 (95% Cl 0.22-0.37) and p-value<0.0001.
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Other Endpoint |
For ENHERTU 5.40 mg/kg, Confirmed Objective Response Rate (ORR)=79.70% (95% Cl 74.30%-84.40%), complete response rate=16.10%, partial response rate=63.60%; For Ado-trastuzumab emtansine 3.60 mg/kg, Confirmed Objective Response Rate (ORR)=34.20% (95% Cl 28.50%-40.30%), complete response rate=8.70%, partial response rate=25.50%.
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Experiment 3 Reporting the Activity Date of This ADC | [5] | ||||
Efficacy Data | Objective Response Rate (ORR) |
79.70%
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Patients Enrolled |
HER2-positive unresectable or metastatic breast cancer who were previously treated with trastuzumab and a taxane in the advanced or metastatic setting.
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Related Clinical Trial | |||||
NCT Number | NCT03529110 | Clinical Status | Phase 3 | ||
Clinical Description |
A phase 3, multicenter, randomized, open-label, active-controlled study of DS-8201a (Trastuzumab Deruxtecan), an Anti-HER2 antibody drug conjugate (ADC), versus Ado Trastuzumab Emtansine (T-DM1) for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with trastuzumab and taxane.
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Primary Endpoint |
The median patient age was 54 years. Approximately 50% of patients were treated with 0-1 prior lines of therapy in the metastatic setting, and 50% were treated with 2 prior treatment regimens. At baseline, 16.50% of patients in the T-DXd group and 14.80% of those in the T-DM1 group had brain metastases. At a median follow-up of 15.90 months, T-DXd significantly improved PFS by 72% compared with T-DM1 across all patient subgroups. Findings were consistent irrespective of hormone receptor status, prior treatment with pertuzumab, number of prior lines of therapy, presence or absence of visceral disease, and presence or absence of brain metastases. The overall response rate (ORR) in the overall study cohort was 79.70% and 34.20% in the T-DXd and T-DM1 groups, respectively, representing an absolute improvement in ORR of 45% with T-DXd Findings were consistent across all patient subgroups, with the absolute improvement in ORR associated with T-DXd relative to T-DM1 ranging from 39% to 52%.
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Experiment 4 Reporting the Activity Date of This ADC | [8] | ||||
Efficacy Data | Objective Response Rate (ORR) |
43.00%
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Positive HER2 expression (HER2+++/++; HER2 MFI=562) | ||
Patients Enrolled |
HER2-positive gastric or gastroesophageal junction adenocarcinoma that had progressed while they were receiving at least two previous therapies, including trastuzumab.
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Administration Dosage |
6.40 mg per kilogram of body weight every 3 weeks.
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Related Clinical Trial | |||||
NCT Number | NCT03329690 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 2, multicenter, open-label study of DS-8201a in subjects with HER2-expressing advanced gastric or gastroesophageal junction adenocarcinoma.
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Primary Endpoint |
In the trastuzumab deruxtecan group, confirmed objective response rate=43.00% (95% Cl 34.00-52.00%), complete response rate=8.00%, partial response rate=34.00%. In the chemotherapy group, confirmed objective response rate=12.00% (95% Cl 5.00-24.00%), complete response rate=0.00%, partial response rate=12.00%.
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Other Endpoint |
In the trastuzumab deruxtecan group (N=119), confirmed disease control rate=86.00% (95% Cl 78.00-91.00%), median Duration of Response (mDOR)=11.30 months (95% Cl 5.60-not estimable), median overall survival (mOS)=12.50 months (95% Cl 9.60-14.30), estimated overall survival was 80.00% at 6 months and 52.00% at 12 months, median progression-free survival (mPFS)=5.60 months (95% CI, 4.30-6.90), estimated progression-free survival=43.00% at 6 months and 30.00% at 12 months In the chemotherapy group (N=56), confirmed disease control rate=62.00% (95% Cl 49.00-75.00%), median Duration of Response (mDOR)=3.90 months (95% Cl 3.0-4.9), median overall survival (mOS)=8.40 months (95% Cl 6.90-10.70), estimated overall survival was 66.00% at 6 months and 29.00% at 12 months, median progression-free survival (mPFS)=3.50 months (95% CI, 2.00-4.30), estimated progression-free survival=21.00% at 6 months and 0.00% at 12 months.
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Experiment 5 Reporting the Activity Date of This ADC | [10] | ||||
Efficacy Data | Objective Response Rate (ORR) |
45.30%
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High HER2 expression (HER2 +++) | ||
Patients Enrolled |
86 patients with metastatic colorectal cancer (mCRC) were enrolled and received at least 1 dose of T-DXd, including 53 patients in cohort A (HER2-positive, immunohistochemistry [IHC] 3+ or IHC 2+/in situ hybridization [ISH]+), 15 patients in cohort B (HER2 IHC 2+/ISH), and 18 patients in cohort C (HER2 IHC 1+).
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Administration Dosage |
6.4 mg/kg every 3 weeks
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Related Clinical Trial | |||||
NCT Number | NCT04744831 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 2, multicenter, randomized, study of trastuzumab deruxtecan in participants with HER2-overexpressing locally advanced, unresectable or metastatic colorectal cancer (DESTINY-CRC02).
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Primary Endpoint |
ORR of 45.30% in cohort A
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Other Endpoint |
No responses occurred in cohorts B or C. Median progression-free survival, overall survival, and duration of response were 6.90, 15.50, and 7.00 months, respectively.
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Experiment 6 Reporting the Activity Date of This ADC | [11] | ||||
Efficacy Data | Objective Response Rate (ORR) |
55.00%
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Positive HER2 expression (HER2+++/++; HER2 MFI=1016) | ||
Patients Enrolled |
HER2-overexpressing or HER2-mutant non-small cell lung cancer (NSCLC).
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Administration Dosage |
Intravenously every 3 weeks at a dose of 6.40 mg per kilogram of body weight.
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Related Clinical Trial | |||||
NCT Number | NCT03505710 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 2, multicenter, open-label, 2-cohort study of Trastuzumab Deruxtecan (DS-8201a), an anti-HER2 antibody drug conjugate (ADC), for HER2-over-expressing or -mutated, unresectable and/or metastatic non small cell lung cancer (NSCLC) (DESTINY-Lung01).
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Primary Endpoint |
Confirmed objective response rate=55.00% (95% CI, 44.00%-65.00%), confirmed complete response rate=1.00%, confirmed partial response=54.00%.
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Other Endpoint |
Median duration of response (mDOR) = 9.30 months (95% CI, 5.70-14.70), Median progression-free survival (mPFS) = 8.20 months (95% CI, 6.00-11.90), median overall survival=17.80 months (95% CI, 13.80-22.10).
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Experiment 7 Reporting the Activity Date of This ADC | [12] | ||||
Efficacy Data | Objective Response Rate (ORR) |
57.70%
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Negative HER2 expression (HER2-; HER2 MFI=10) | ||
Patients Enrolled |
HER2-mutated metastatic non-small cell lung cancer (NSCLC).
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Administration Dosage |
6.40 mg/kg administered by intravenous infusion every 3 weeks (Q3W).
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Related Clinical Trial | |||||
NCT Number | NCT04644237 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 2, multicenter, randomized study of trastuzumab deruxtecan in subjects with HER2-mutated metastatic non-small cell lung cancer (NSCLC) (DESTINY-LUNG02).
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Primary Endpoint |
Confirmed Objective Response Rate=57.70% (95% CI, 43.20-71.30%), Complete Response rate=19.00%, Partial Response=55.80%.
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Other Endpoint |
Median Duration of Response (mDOR) = 8.70 months (95% Cl 7.10-not estimable).
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Experiment 8 Reporting the Activity Date of This ADC | [13] | ||||
Efficacy Data | Objective Response Rate (ORR) |
60.90%
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Positive HER2 expression (HER2+++/++; HER2 MFI=957) | ||
Patients Enrolled |
Pathologically documented HER2-positive, unresectable or metastatic breast cancer who had received previous treatment with trastuzumab emtansine.
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Administration Dosage |
5.4 mg per kilogram administered by intravenous infusion every 3 weeks.
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Related Clinical Trial | |||||
NCT Number | NCT03248492 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 2, multicenter, open-label study of DS-8201a, an anti-HER2-antibody drug conjugate (ADC) for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with T-DM1 (DESTINY-Breast01).
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Primary Endpoint |
Confirmed Objective Response Rate=60.90% (95% CI, 53.40%-68.00%), complete response rate=6.00%, partial response rate= 54.90%.
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Other Endpoint |
Disease-control rate was 97.30% (95% CI, 93.80-99.10), Median Duration of Response (months)=14.80 (95% CI, 13.80-16.90), clinical-benefit rate was 76.10% (95% CI, 69.30-82.10), median duration of progression-free survival was 16.40 months (95% CI, 12.70-not reached), estimated overall survival was 93.90% (95% CI, 89.30-96.60) at 6 months and 86.20% (95% CI, 79.80-90.70) at 12 months.
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Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Objective Response Rate (ORR) |
73.33%
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Patients Enrolled |
HER2-positive breast cancer and newly diagnosed untreated brain metastases or brain metastases progressing after previous local therapy, previous exposure to trastuzumab and pertuzumab and no indication for immediate local therapy.
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Administration Dosage |
5.40 mg per kg bodyweight once every 3 weeks intravenously.
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Related Clinical Trial | |||||
NCT Number | NCT04752059 | Clinical Status | Phase 2 | ||
Clinical Description |
Phase 2 study of trastuzumab-deruxtecan (T-DX; DS-8201a) in HER2-positive breast cancer patients with newly diagnosed or progressing brain metastases.
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Primary Endpoint |
In the ITT population (n=15 patients), intracranial response rate by RANO-BM was 73.33% (95% CI 48.10-89.10%) (11/15 patients; 2 patients in complete remission (13.33%); 9 patients in partial remission (60.00%)). In the per protocol population (PP;n=14 patients), the response rate was 78.57% (95% CI 49.20-95.30%) (11/14). Two patients had stable disease for 6 months and one patient had stable disease at first restaging and progressed after four cycles of trastuzumab deruxtecan. Clinical benefit rate was 13/14 (92.86%; 95% CI 66.10-99.80%) in the PP population.
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Other Endpoint |
In patients with extracranial metastases at baseline (n=13), a partial response by RECIST 11 was observed in 5/13 (27.8%; 95% CI 13.9-68.4%) patients, with the remainder having stable disease. None of the patients progressing on trastuzumab deruxtecan had extracranial progression as the first site of progressive disease In patients with measurable extracranial disease at baseline (n=8), a partial remission was observed in 5/8 (62.50%; 95% CI 24.50-91.50%) patients, with the remainder having stable disease.
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Experiment 10 Reporting the Activity Date of This ADC | [15] | ||||
Efficacy Data | Objective Response Rate (ORR) |
37.00%
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Low HER2 expression (HER2 -) | ||
Patients Enrolled |
54 patients with HER2-low breast cancer
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Administration Dosage |
5.4 or 6.4 mg/kg.
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Related Clinical Trial | |||||
NCT Number | NCT02564900 | Clinical Status | Phase 1 | ||
Clinical Description |
Phase 1, two-part, multicenter, non-randomized, open-label, multiple dose first-in-human study of DS-8201A, in subjects with advanced solid malignant tumors.
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Primary Endpoint |
Median duration of response = 10.40 months, median progression free survival (PFS) = 11.10 months, median overall survival = 29.40 months.
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Other Endpoint |
Confirmed ORR = 24.00 ; DOR, Median=11.00 months; TTR, months Median=2.80 ;PFS, months Median=8.00.
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Experiment 11 Reporting the Activity Date of This ADC | [16] | ||||
Efficacy Data | Objective Response Rate (ORR) |
54.50% (HER2-high)
70.00% (HER2-low) |
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Patients Enrolled |
Recurrent uterine carcinosarcoma (UCS) with HER2 immunohistochemistry scores 1+ previously treated with chemotherapy were included.
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Administration Dosage |
6.40 or 5.40 mg/kg was administered intravenously once every 3 weeks.
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Discovered Using Patient-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 88.90% (Day 28) | High HER2 expression (HER2+++; IHC 3+) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 3 mg/kg or 10 mg/kg DS-8201a was i.v. respectively to the tumor-bearing mice.
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In Vivo Model | Gastric cancer PDX model (PDX: NIBIO G016) | ||||
Experiment 2 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.30% (Day 28) | Low HER2 expression (HER2+; IHC 1+) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a was i.v. to the tumor-bearing mice.
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In Vivo Model | Breast cancer PDX model (PDX: ST313) | ||||
Experiment 3 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.20% (Day 28) | Low HER2 expression (HER2+; IHC 1+) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a was i.v. to the tumor-bearing mice.
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In Vivo Model | Breast cancer PDX model (PDX: ST565) | ||||
Experiment 4 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.60% (Day 21) | Moderate HER2 expression (HER2++; IHC 2+) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a was i.v. to the tumor-bearing mice.
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In Vivo Model | Breast cancer PDX model (PDX: ST225) |
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [20] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 0.00% | Negative HER2 expression (HER2 -) | ||
Method Description |
Volume of tumors formed by HCT116-Mock, HCT116-H2L or HCT116-H2H cells in nude mice injected intraperitoneally once every 3 weeks with PBS vehicle or trastuzumab deruxtecan (DS-8201a, 3 mg/kg) beginning at Day 0.
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In Vivo Model | HCT116-Mock CDX model | ||||
In Vitro Model | Colon carcinoma | HCT 116-Mock cells (Negative HER2 expression) | CVCL_0291 | ||
Experiment 2 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 13.50% (Day 21) | Low HER2 expression (HER2+) | ||
Method Description |
The antitumor activity of DS-8201a and trastuzumab were evaluated in various mice xenograft models with different HER2 expression levels; CFPAC-1 (low-expression). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 1 mg/kg DS-8201a or 10 mg/kg trastuzumab was i.v. to the tumor-bearing mice.
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In Vivo Model | CFPAC-1 cell line xenograft model | ||||
In Vitro Model | Pancreatic ductal adenocarcinoma | CFPAC-1 cells | CVCL_1119 | ||
Experiment 3 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 17.20% (Day 21) | Negative HER2 expression (HER2-) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; GCIY (negative). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.
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In Vivo Model | GCIY cell line xenograft model | ||||
In Vitro Model | Gastric adenocarcinoma | GCIY cells | CVCL_1228 | ||
Experiment 4 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 28.80% (Day 21) | Positive HER2 expression (HER2+++/++; HER2 MFI=1016) | ||
Method Description |
The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice. The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0 In this group, 0.25 mg/kg DS-8201a was iv to the tumor-bearing mice.
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In Vivo Model | HER2-positive NCI-N87 xenograft model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 58.50% (Day 21) | Moderate HER2 expression (HER2++) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; JIMT-1 (moderate positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.
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In Vivo Model | JIMT-1 cell line xenograft model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 61.60% (Day 21) | Low HER2 expression (HER2+) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; Capan-1 (weak positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.
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In Vivo Model | Capan-1 cell line xenograft model | ||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 7 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 62.50% (Day 21) | Positive HER2 expression (HER2+++/++; HER2 MFI=1016) | ||
Method Description |
The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice. The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0 In this group, 0.5 mg/kg DS-8201a was iv to the tumor-bearing mice.
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In Vivo Model | HER2-positive NCI-N87 xenograft model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 8 Reporting the Activity Date of This ADC | [20] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 66.70% (Day 18) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Trastuzumab deruxtecan (10 mg/kg, every seven days 2) induces efficient tumor cell killing in cell line-derived models of EMT6-hHER2 cells with HER2 expression with high expression.
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In Vivo Model | EMT6 CDX model (Expressing hHER2) | ||||
In Vitro Model | Mammary gland malignant neoplasms | EMT6 cells (High HER2 expression) | CVCL_1923 | ||
Experiment 9 Reporting the Activity Date of This ADC | [20] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 68.70% (Day 24) | Low HER2 expression (HER2 +, IHC 1+) | ||
Method Description |
Volume of tumors formed by HCT116-Mock, HCT116-H2L or HCT116-H2H cells in nude mice injected intraperitoneally once every 3 weeks with PBS vehicle or trastuzumab deruxtecan (DS-8201a, 3 mg/kg) beginning at Day 0.
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In Vivo Model | HCT116-H2L CDX model | ||||
In Vitro Model | Colon carcinoma | HCT 116-H2L cells (Low HER2 expression) | CVCL_0291 | ||
Experiment 10 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 86.00% (Day 21) | Positive HER2 expression (HER2+++/++; HER2 MFI=1016) | ||
Method Description |
The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 1 mg/kg DS-8201a was i.v. to the tumor-bearing mice.
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In Vivo Model | HER2-positive NCI-N87 xenograft model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 11 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 88.30% (Day 21) | Positive HER2 expression (HER2+++/++; HER2 MFI=95.7) | ||
Method Description |
The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; KPL-4 (strong positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.
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In Vivo Model | KPL-4 cell line xenograft model | ||||
In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 12 Reporting the Activity Date of This ADC | [20] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.10% (Day 24) | High HER2 expression (HER2 +++, IHC 3+) | ||
Method Description |
Volume of tumors formed by HCT116-Mock, HCT116-H2L or HCT116-H2H cells in nude mice injected intraperitoneally once every 3 weeks with PBS vehicle or trastuzumab deruxtecan (DS-8201a, 3 mg/kg) beginning at Day 0.
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In Vivo Model | HCT116-H2H CDX model | ||||
In Vitro Model | Colon carcinoma | HCT 116-H2H cells (High HER2 expression) | CVCL_0291 | ||
Experiment 13 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.30% (Day 21) | Positive HER2 expression (HER2+++/++; HER2 MFI=1016) | ||
Method Description |
The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 2 mg/kg DS-8201a was i.v. to the tumor-bearing mice.
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In Vivo Model | HER2-positive NCI-N87 xenograft model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 14 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.10% (Day 21) | Positive HER2 expression (HER2+++/++; HER2 MFI=1016) | ||
Method Description |
The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 4 mg/kg DS-8201a was i.v. to the tumor-bearing mice.
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In Vivo Model | HER2-positive NCI-N87 xenograft model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.70 ng/mL±1.50 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.80 ng/mL±0.70 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.10 ng/mL±1.00 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
Experiment 4 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.30 ng/mL±0.20 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 5 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.10 ng/mL±2.70 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
Experiment 6 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.70 ng/mL
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Method Description |
The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 7 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.60 ng/mL±0.50 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 8 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.60 ng/mL±0.20 ng/mL
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Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 9 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.10 ng/mL±1.30 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor BAY1898344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 10 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.00 ng/mL±1.60 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus ATR inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
Experiment 11 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
11.50 ng/mL±3.20 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
Experiment 12 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15.10 ng/mL±1.70 ng/mL
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Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Experiment 13 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15.70 ng/mL±2.90 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 14 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
24.90 ng/mL±7.50 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 15 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
25.40 ng/mL
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Method Description |
The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 16 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
26.80 ng/mL
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Method Description |
The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
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In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
Experiment 17 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
32.70 ng/mL±20.80 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 18 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
34.80 ng/mL±0.40 ng/mL
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Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Experiment 19 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
41.70 ng/mL±22.70 ng/mL
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Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Experiment 20 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
41.80 ng/mL±4.40 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Experiment 21 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3000 ng/mL | High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 22 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3000 ng/mL | Negative HER2 expression (HER2 -) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
Experiment 23 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3000 ng/mL | High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 24 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3000 ng/mL | Negative HER2 expression (HER2 -) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
Experiment 25 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3000 ng/mL | High HER2 expression (HER2 +++) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 26 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3000 ng/mL | Negative HER2 expression (HER2 -) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
Experiment 27 Reporting the Activity Date of This ADC | [33] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3000 ng/mL | Negative HER2 expression (HER2 -) | ||
Method Description |
In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
Experiment 28 Reporting the Activity Date of This ADC | [20] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.00 ng/mL
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High HER2 expression (HER2 +++, IHC 3+) | ||
Method Description |
Viability of NCI-N87 cells as well as of parental HCT116 cells and their derivatives (Mock, H2L and H2H) after incubation with the indicated concentrations of trastuzumab deruxtecan (DS-8201a) or T-DM1 for 144 h.
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In Vitro Model | Colon carcinoma | HCT 116-H2H cells (High HER2 expression) | CVCL_0291 | ||
Experiment 29 Reporting the Activity Date of This ADC | [18] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | |||
Method Description |
The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 30 Reporting the Activity Date of This ADC | [20] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
97.00 ng/mL
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High HER2 expression (HER2 +++) | ||
Method Description |
Viability of NCI-N87 cells as well as of parental HCT116 cells and their derivatives (Mock, H2L and H2H) after incubation with the indicated concentrations of trastuzumab deruxtecan (DS-8201a) or T-DM1 for 144 h.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
A-166 [NDA]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [34] | ||||
Efficacy Data | Partial Response (PR) |
25.92%
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Patients Enrolled |
Locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified.
|
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Administration Dosage |
0.30, 1.20, 3.60, 4.80 mg/kg, every 3 weeks from date of enrollment until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 24 months.
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Related Clinical Trial | |||||
NCT Number | NCT03602079 | Clinical Status | Phase 1 | ||
Clinical Description |
A phase 1-2, FIH Study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.
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Primary Endpoint |
Overall incidence of ophthalmic toxicities in the 3.60 mg/kg cohort was 80% and in the 4.80 mg/kg cohort it was 83.00%. Responses were seen only at the dose levels of 3.60 mg/kg and 4.80 mg/kg. Among the 27 patients evaluable for efficacy,best response was progression of disease in 11 patients (40.74%), stable disease in 9 patients (33.33%) and partial response in 7 patients (25.92%),for the total disease control rate of 59%.
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Experiment 2 Reporting the Activity Date of This ADC | [35] | ||||
Efficacy Data | Objective Response Rate (ORR) |
73.90% (4.8 mg/kg)
68.60% (6.0 mg/kg) |
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Patients Enrolled |
Patients with HER2-expressing advanced solid tumours.
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Administration Dosage |
0.10, 0.30, 0.60, 1.20, 2.40, 3.60, 4.80 or 6.00 mg/kg Q3W.
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Related Clinical Trial | |||||
NCT Number | NCT05311397 | Clinical Status | Phase 1 | ||
Clinical Description |
A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of A166 in patients with unresectable, locally advanced or metastatic HER2-expressing solid tumors (KL166-I-01-CTP).
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Experiment 3 Reporting the Activity Date of This ADC | [39] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05346328 | Clinical Status | Phase 2 | ||
Clinical Description |
An open-clinical trial phase , injection of A166 for HER2-positive patients with refractory unresectable locally advanced or metastatic breast cancer KL166-2S-001.
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Experiment 4 Reporting the Activity Date of This ADC | [40] | ||||
Related Clinical Trial | |||||
NCT Number | NCT03602079 | Clinical Status | Phase 1/2 | ||
Clinical Description |
A phase 1-2, FIH study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.
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Trastuzumab duocarmazine [NDA]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [36] | ||||
Related Clinical Trial | |||||
NCT Number | NCT03262935 | Clinical Status | Phase 3 | ||
Clinical Description |
A multi-centre, open-label, randomized clinical trial comparing the efficacy and safety of the antibody-drug conjugate SYD985 to physician's choice in patients with HER2-positive unresectable locally advanced or metastatic breast cancer.
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||||
Experiment 2 Reporting the Activity Date of This ADC | [37] | ||||
Related Clinical Trial | |||||
NCT Number | NCT04205630 | Clinical Status | Phase 2 | ||
Clinical Description |
A single-arm phase 2 trial to evaluate the safety and efficacy of the antibody-drug conjugate (ADC) SYD985 in patients with human epidermal growth factor receptor 2 (HER2)-expressing endometrial carcinoma who previously progressed on or after first line platinum-based chemotherapy.
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Experiment 3 Reporting the Activity Date of This ADC | [38] | ||||
Related Clinical Trial | |||||
NCT Number | NCT01042379 | Clinical Status | Phase 2 | ||
Clinical Description |
I-SPY trial (investigation of serial studies to predict your therapeutic response with imaging and molecular analysis 2).
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Experiment 4 Reporting the Activity Date of This ADC | [41] | ||||
Related Clinical Trial | |||||
NCT Number | NCT04983238 | Clinical Status | Phase 1 | ||
Clinical Description |
A multicenter, randomized, double-blind, placebo-controlled trial with a single arm run-in period to evaluate the safety and efficacy of sodium thiosulfate (BYON5667) Eye drops to reduce ocular toxicity in cancer patients treated with SYD985.
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Experiment 5 Reporting the Activity Date of This ADC | [42] | ||||
Related Clinical Trial | |||||
NCT Number | NCT04602117 | Clinical Status | Phase 1 | ||
Clinical Description |
ISPY-P1.01: evaluating the safety of weekly paclitaxel with trastuzumab duocarmazine (SYD985) in patients with metastatic cancer: a phase 1/Ib trial.
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Experiment 6 Reporting the Activity Date of This ADC | [43] | ||||
Related Clinical Trial | |||||
NCT Number | NCT04235101 | Clinical Status | Phase 1 | ||
Clinical Description |
A two-part phase 1 study with the antibody-drug conjugate SYD985 in combination with niraparib to evaluate safety, pharmacokinetics and efficacy in patients with HER2-expressing locally advanced or metastatic solid tumors.
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Experiment 7 Reporting the Activity Date of This ADC | [44] | ||||
Related Clinical Trial | |||||
NCT Number | NCT02277717 | Clinical Status | Phase 1 | ||
Clinical Description |
A two part first-in-human phase 1 study (with expanded cohorts) with the antibody-drug conjugate SYD985 to evaluate the safety, pharmacokinetics and efficacy in patients with locally advanced or metastatic solid tumors.
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Discovered Using Patient-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 33.30% (Day 76) | High HER2 expression (HER2+++; IHC 3+; FISH+) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
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||||
In Vivo Model | Breast cancer PDX model (PDX: MAXF-1162) | ||||
Experiment 2 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 42.90% (Day 80) | Low HER2 expression (HER2+; IHC +; FISH-) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
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||||
In Vivo Model | Breast cancer PDX model (PDX: MAXF 449) | ||||
Experiment 3 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 65.00% (Day 80) | Moderate HER2 expression (HER2++; IHC 2+; FISH-) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
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||||
In Vivo Model | Breast cancer PDX model (PDX: HBCx-34) | ||||
Experiment 4 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 66.70% (Day 31) | Moderate HER2 expression (HER2++; IHC 2+; FISH-) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Breast cancer PDX model (PDX: ST313) | ||||
Experiment 5 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 75.00% (Day 28) | Low HER2 expression (HER2+; IHC +; FISH-) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Gastric cancer PDX model (PDX: GXA3057) | ||||
Experiment 6 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.00% (Day 46) | Moderate HER2 expression (HER2++; IHC 2+; FISH-) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Gastric cancer PDX model (PDX: GXA3038) | ||||
Experiment 7 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 20) | High HER2 expression (HER2+++; IHC 3+; FISH+) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Gastric cancer PDX model (PDX: GXA3054) | ||||
Experiment 8 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 21) | Moderate HER2 expression (HER2++; IHC 2+; FISH+) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Gastric cancer PDX model (PDX: GXA3067) | ||||
Experiment 9 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 41) | High HER2 expression (HER2+++; IHC 3+; FISH+) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Bladder cancer PDX model (PDX: BXF439) | ||||
Experiment 10 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 32) | Low HER2 expression (HER2+; IHC +; FISH-) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Breast cancer PDX model (PDX: MAXF-MX1) | ||||
Experiment 11 Reporting the Activity Date of This ADC | [45] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 40) | Low HER2 expression (HER2+; IHC +; FISH-) | ||
Method Description |
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
|
||||
In Vivo Model | Breast cancer PDX model (PDX: HBCx-10) |
SHR-A1811 [Phase 3]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [46] | ||||
Efficacy Data | Objective Response Rate (ORR) |
61.60%
81.50% (HER2-positive BC) 55.80% (HER2-low BC) |
|||
Patients Enrolled |
Pts were eligible if they had HER2 positive breast cancer (BC), HER2 positive gastric/GEJ carcinoma, HER2 low-expressing BC, HER2-expressing/mutated NSCLC, or other HER2-expressing/mutated solid tumors, and were refractory or intolerant to standard therapy.
|
||||
Administration Dosage |
SHR-A1811 at doses of 1.00-8.00 mg/kg was given Q3W (IV).
|
||||
Related Clinical Trial | |||||
NCT Number | NCT04446260 | Clinical Status | Phase 1 | ||
Clinical Description |
A phase 1 multi-country, multi-center, open-label study to evaluate the safety, tolerability, pharmacokinetics and efficacy of SHR-A1811 in HER2 expressing or mutated advanced malignant solid tumor subjects.
|
||||
Experiment 2 Reporting the Activity Date of This ADC | [48] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05424835 | Clinical Status | Phase 3 | ||
Clinical Description |
A phase 3, multicenter, randomized, open-label, parallel controlled study of SHR-A1811 versus pyrotinib in combination with capecitabine for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with trastuzumab and taxane.
|
||||
Experiment 3 Reporting the Activity Date of This ADC | [49] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05769010 | Clinical Status | Phase 2 | ||
Clinical Description |
A prospective, open-label explorative study of SHR-A1811 in HER2-expression advanced breast cancer with brain metastases.
|
||||
Experiment 4 Reporting the Activity Date of This ADC | [50] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05749588 | Clinical Status | Phase 2 | ||
Clinical Description |
Precision platform study of refractory triple-negative breast cancer based on molecular subtyping (a phase 2, open-label, single-center platform study).
|
||||
Experiment 5 Reporting the Activity Date of This ADC | [51] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05671822 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 1b/2 study of SHR-A1811 combinations in patients with advanced/metastatic HER2+ gastric /gastroesophageal junction adenocarcinoma.
|
||||
Experiment 6 Reporting the Activity Date of This ADC | [52] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05635487 | Clinical Status | Phase 2 | ||
Clinical Description |
A single-arm, phase 2 study of SHR-A1811 combined with pyrotinib maleate as neoadjuvant treatment in HER2-positive breast cancer patients.
|
||||
Experiment 7 Reporting the Activity Date of This ADC | [53] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05594095 | Clinical Status | Phase 2 | ||
Clinical Description |
Precision platform study of HR+/ HER2-advanced breast cancer based on snf typing (a prospective, open-label, multi-center, phase 2 platform study).
|
||||
Experiment 8 Reporting the Activity Date of This ADC | [54] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05353361 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 1b/2 multicenter, open-label clinical trial of SHR-A1811 injection in combination with pyrotinib or pertuzumab or SHR-1316 or paclitaxel for injection (albumin bound) in HER2-positive breast cancer.
|
||||
Experiment 9 Reporting the Activity Date of This ADC | [55] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05349409 | Clinical Status | Phase 2 | ||
Clinical Description |
A phase 1b/2 clinical study on the dosage exploration and efficiency expansion of SHR-A1811 for injection in combination with fluzoparib capsule in HER2-expressing advanced solid tumors of patients.
|
||||
Experiment 10 Reporting the Activity Date of This ADC | [56] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05582499 | Clinical Status | Phase 1/2 | ||
Clinical Description |
Fudan university shanghai cancer center breast cancer precision platform series study- neoadjuvant therapy (FASCINATE-N).
|
||||
Experiment 11 Reporting the Activity Date of This ADC | [57] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05482568 | Clinical Status | Phase 1/2 | ||
Clinical Description |
Phase 1B/2 clinical study of the safety, tolerability, pharmacokinetics, and efficacy of injectable SHR-A1811 in combination with pyrotinib or SHR-1316 in subjects with advanced non-small cell lung cancer with HER2.
|
||||
Experiment 12 Reporting the Activity Date of This ADC | [58] | ||||
Related Clinical Trial | |||||
NCT Number | NCT04818333 | Clinical Status | Phase 1/2 | ||
Clinical Description |
Phase 1/2 clinical study of the safety, tolerability, pharmacokinetics, and efficacy of SHR-A1811 for injection in subjects with advanced non-small cell lung cancer who have HER2 expression, amplification, or mutation.
|
||||
Experiment 13 Reporting the Activity Date of This ADC | [59] | ||||
Related Clinical Trial | |||||
NCT Number | NCT04513223 | Clinical Status | Phase 1 | ||
Clinical Description |
Safety, tolerability, pharmacokinetics, and antitumour activity of SHR-A1811, in patients with HER2-expressing advanced gastric or gastroesophageal junction adenocarcinoma and colorectal cancer: a phase 1 study.
|
LCB14-0110 [Phase 3]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [47] | ||||
Efficacy Data | Objective Response Rate (ORR) |
66.70% (> 1.00 mg/kg)
42.90% (HER2-Low) |
|||
Patients Enrolled |
Patients with HER2-expresssing advanced solid tumors who had failed prior standard of care therapies.
|
||||
Administration Dosage |
FS-1502 was given IV once in 21-day or 28-day cycle at doses of 0.10-3.50 mg/kg.
|
GQ-1001 [Phase 2]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [60] | ||||
Efficacy Data | Partial Response (PR) |
40.00%
|
|||
Patients Enrolled |
HER2-positive advanced solid tumors.
|
||||
Administration Dosage |
Administered intravenously as a monotherapy on Day 1 of 21-day cycles. The starting dose was 1.20 mg/kg, followed by 2.40, 3.60, 4.80, 6.00, 7.20 and 8.40 mg/kg.
|
||||
Related Clinical Trial | |||||
NCT Number | NCT04450732 | Clinical Status | Phase 1 | ||
Clinical Description |
A phase 1, first-in-human, multicenter, open-label, study of GQ1001, a HER2 targeted antibody-drug conjugate, administered intravenously, in adult patients with HER2-positive advanced solid tumors.
|
||||
Experiment 2 Reporting the Activity Date of This ADC | [62] | ||||
Related Clinical Trial | |||||
NCT Number | NCT05575804 | Clinical Status | Phase 1/2 | ||
Clinical Description |
Phase 1b/2 study of GQ1001 and pyrotinib in HER2 positive metastatic breast cancer patients who had failed previous anti-HER2 treatment GRACE.
|
BDC-1001 [Phase 1/2]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [61] | ||||
Patients Enrolled |
Patients with advanced metastatic HER2-expressing (IHC2/3+) or amplified solid tumors. Patients had received a median of 4 prior therapies.
|
||||
Administration Dosage |
4 dose levels (0.15-5.00 mg/kg) every 3 weeks.
|
||||
Related Clinical Trial | |||||
NCT Number | NCT04278144 | Clinical Status | Phase 1/2 | ||
Clinical Description |
Phase 1/2 study of BDC-1001 as a single agent and in combination with nivolumab in patients with advanced HER2-expressing solid tumors.
|
B-003 [Phase 2]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [63] | ||||
Related Clinical Trial | |||||
NCT Number | NCT03953833 | Clinical Status | Phase 1 | ||
Clinical Description |
Phase 1 clinical trial on the safety, tolerability, pharmacokinetics of B003 in the treatment of HER2-positive recurrent or metastatic breast cancer.
|
SHR-A1201 [Phase 1]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [64] | ||||
Patients Enrolled |
HER2-positive locally advanced or metastatic breast cancer (positivity for HER2 was defined as a score of 2+ in immunohistochemical analysis and a positive result in fluorescence in situ hybridization or a score of 3+ in immunohistochemical analysis), the standard treatment was invalid or there was no effective standard treatment plan, the Eastern Cooperative Oncology Group performance status score was 0-1.
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||||
Administration Dosage |
4 dose-escalation sequences, 1.20 mg/kg, 2.40 mg/kg, 3.60 mg/kg and 4.80 mg/kg, once every 21days, as a 90-min intravenous infusion.
|
Tra-IR700 [Clinical candidate]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 54.50% (Day 7) | Negative HER2 expression (HER2 -) | ||
Method Description |
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (with NIR light 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
|
||||
In Vivo Model | MDA-MB-468GFP CDX model | ||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 | ||
Experiment 2 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 81.80% (Day 7) | Negative HER2 expression (HER2 -) | ||
Method Description |
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (with NIR light 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
|
||||
In Vivo Model | MDA-MB-468GFP CDX model | ||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 |
Trastuzumab-SYNtansine [Investigative]
Discovered Using Patient-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [65] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 80.60% (Day 23) | High HER2 expression (HER2+++) | ||
Method Description |
25 mice with T226 tumor (P12.1.4/0) between 75 and 196 mm3 were allocated, according to their tumor volume to give homogenous mean and median tumor volume in each treatment arm (5 mice/group). Treatments were initiated when the median tumor volume was 126 mm3 by intravenous injection with either vehicle (control), and trastuzumab-SYNtansine 3 mg/kg.
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|
||||
In Vivo Model | Breast cancer PDX model (PDX: T226) | ||||
Experiment 2 Reporting the Activity Date of This ADC | [65] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 23) | High HER2 expression (HER2+++) | ||
Method Description |
25 mice with T226 tumor (P12.1.4/0) between 75 and 196 mm3 were allocated, according to their tumor volume to give homogenous mean and median tumor volume in each treatment arm (5 mice/group). Treatments were initiated when the median tumor volume was 126 mm3 by intravenous injection with either vehicle (control), and trastuzumab-SYNtansine 9 mg/kg.
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||||
In Vivo Model | Breast cancer PDX model (PDX: T226) |
WO2021249228A1 ADC-6 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 0.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
|
||||
In Vivo Model | NCI-H1975 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
Experiment 2 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 84.50% (Day 31) | Positive EGFR expression (EGFR+++/++) | ||
Method Description |
To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
|
||||
In Vivo Model | NCI-H1975 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
Experiment 3 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
|
||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.70% (Day 31) | Positive EGFR expression (EGFR+++/++) | ||
Method Description |
To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
|
||||
In Vivo Model | NCI-H1975 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
435.86 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Trastuzumab-Compound (la) DAR 1.6 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 0.00% (Day 42) | Positive CD20 expression (CD20+++/++) | ||
Method Description |
Daudi human NHL fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (1 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
|
||||
In Vivo Model | Daudi CDX model | ||||
In Vitro Model | Burkitt lymphoma | Daudi cells | CVCL_0008 | ||
Experiment 2 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 25.30% (Day 24) | Positive CD33 expression (CD33+++/++) | ||
Method Description |
HL-60 human AML fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (1 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
|
||||
In Vivo Model | HL-60 CDX model | ||||
In Vitro Model | Adult acute myeloid leukemia | HL-60 cells | CVCL_0002 | ||
Experiment 3 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 82.76% (Day 30) | High HER2 expression (HER2+++) | ||
Method Description |
BT474 human breast carcinomas fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); pertuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
|
||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
25.00 pM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
OHPAS ADC-3 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 0.00% (Day 78) | High HER2 expression (HER2 +++) | ||
Method Description |
We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (0.5 mg/kg) on day one (initial tumor volume 100 mm3).
|
||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 71.10% (Day 78) | High HER2 expression (HER2 +++) | ||
Method Description |
We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (2 mg/kg) on day one (initial tumor volume 100 mm3).
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||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 4 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.58 nM
|
Negative HER2 expression (HER2 -) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014068443A1 ADC3 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 1.62% (Day 32) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 43.50% (Day 32) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.91% (Day 32) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.62 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.75 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
506.44 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
IgG1 (trastuzumab)-vc-MMAE [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [69] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 3.53% (Day 21) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [69] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 15.69% (Day 21) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [69] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 22.02% (Day 21) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [69] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 28.11% (Day 21) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [69] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 30.13% (Day 21) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 6 Reporting the Activity Date of This ADC | [69] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 52.51% (Day 21) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [69] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
27.40 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2021249228A1 ADC-61 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 4.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
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In Vivo Model | NCI-H1975 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
Experiment 2 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 71.20% (Day 31) | Positive EGFR expression (EGFR+++/++) | ||
Method Description |
To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
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In Vivo Model | NCI-H1975 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
Experiment 3 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.00% (Day 31) | Positive EGFR expression (EGFR+++/++) | ||
Method Description |
To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
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In Vivo Model | NCI-H1975 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2014068443A1 ADC4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 8.74% (Day 28) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 81.85% (Day 28) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.84% (Day 28) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.73 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.83 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.00 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
T-DM1-IR700 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 10.10% (Day 7) | Negative HER2 expression (HER2 -) | ||
Method Description |
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
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In Vivo Model | MDA-MB-468GFP CDX model | ||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 | ||
Experiment 2 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 36.40% (Day 7) | Negative HER2 expression (HER2 -) | ||
Method Description |
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
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||||
In Vivo Model | MDA-MB-468GFP CDX model | ||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM - 10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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In Vitro Model | Lung squamous cell carcinoma | NCI-H2170 cells | CVCL_1535 | ||
Experiment 2 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM - 10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Experiment 3 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM - 10 nM
|
Low HER2 expression (HER2+) | ||
Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
Experiment 4 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM - 10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
Experiment 5 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.50 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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In Vitro Model | Breast adenocarcinoma | 3T3/HER2-luc-GFP cells | Mus musculus | ||
Experiment 6 Reporting the Activity Date of This ADC | [32] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
100 nM
|
Negative HER2 expression (HER2 -) | ||
Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 |
WO2014068443A1 ADC14 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 11.68% (Day 18) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 39.11% (Day 27) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 76.82% (Day 27) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.56 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.92 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.18 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Trastuzumab-Gelonin [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [70] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 13.34% (Day 36) | High HER2 expression (HER2+++) | ||
Method Description |
The inhibitory activity of trastuzumab-gelonin against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
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In Vivo Model | Gastric cancer CDX model | ||||
In Vitro Model | Gastric cancer | Gastric cancer cells | Homo sapiens | ||
Experiment 2 Reporting the Activity Date of This ADC | [70] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 50.57% (Day 36) | High HER2 expression (HER2+++) | ||
Method Description |
The inhibitory activity of trastuzumab-gelonin+LE8 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
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In Vivo Model | Gastric cancer CDX model | ||||
In Vitro Model | Gastric cancer | Gastric cancer cells | Homo sapiens | ||
Experiment 3 Reporting the Activity Date of This ADC | [70] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 59.79% (Day 36) | High HER2 expression (HER2+++) | ||
Method Description |
The inhibitory activity of trastuzumab-gelonin+1HE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
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In Vivo Model | Gastric cancer CDX model | ||||
In Vitro Model | Gastric cancer | Gastric cancer cells | Homo sapiens |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [70] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.22±0.08 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The inhibitory activity of trastuzumab-gelonin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [70] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
555.00±69.60 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The inhibitory activity of unconjugated rGel against cancer cell growth was evaluated in various human cancer cell lines in vitro.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2020063676A1 ADC-21 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 15.01% (Day 28) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
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In Vivo Model | SK-BR-3 CDX model | ||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 46.22% (Day 34) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 56.77% (Day 34) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.40% (Day 28) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 6 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
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In Vivo Model | SK-BR-3 CDX model | ||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
WO2014068443A1 ADC5 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 17.49% (Day 28) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 61.28% (Day 28) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.20% (Day 28) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.77 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.85 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.93 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2020063676A1 ADC-22 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 19.82% (Day 28) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
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In Vivo Model | SK-BR-3 CDX model | ||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.38% (Day 28) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 6 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
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In Vivo Model | SK-BR-3 CDX model | ||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
WO2014068443A1 ADC18 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 20.29% (Day 27) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 55.70% (Day 27) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.48% (Day 27) | High HER2 expression (HER2+++) | ||
Method Description |
For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.76 nM
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High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.99 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.22 nM
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Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Trastuzumab-alpha-amanitin conjugate 11 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 28.53% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.60% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
OHPAS ADC-2 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 37.00% (Day 78) | High HER2 expression (HER2 +++) | ||
Method Description |
We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (0.5 mg/kg) on day one (initial tumor volume 100 mm3).
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.60% (Day 78) | High HER2 expression (HER2 +++) | ||
Method Description |
We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (2 mg/kg) on day one (initial tumor volume 100 mm3).
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 4 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
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Moderate HER2 expression (HER2 ++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
Trastuzumab-alpha-amanitin conjugate 4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 37.30% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 76.05% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
HER2-gsADC-46 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 37.39% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.15% (Day 57) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
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Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 66.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
CN105051032B ADC-I-16 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 44.70% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 63.20% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 65.80% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
2.88 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-26 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 45.00% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 47.50% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 87.50% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
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||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
4.17 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-34 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 47.50% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 67.50% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 75.00% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
11.30 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2017089890A1 ADC33 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 53.99% (Day 36) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 89.50% (Day 36) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.23 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.33 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
Trastuzumab-alpha-amanitin conjugate 10 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 55.08% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.16% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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||||
In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
HER2-gsADC-48 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 56.18% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.50% (Day 57) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 66.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2017089890A1 ADC34 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 58.68% (Day 36) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
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||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 87.39% (Day 36) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
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||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
ADC-II-13 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 58.75% | High HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
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||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
73.11 nM
|
Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
73.11 nM
|
Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Trastuzumab-T1000-exatecan [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [77] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 59.00% (Day 27) | Negative HER2 expression (HER2 -) | ||
Method Description |
T moiety (We conducted a four-week (day 1, 8, 15, 22, and 29) intermittent intravenous dose toxicity study of exatecan mesylate in rats (six animals/group) with a four-week recovery period (three of the six animals).
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||||
In Vivo Model | MDA-MB-468 CDX model | ||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Docetaxel-trastuzumab [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [78] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 60.00% (Day 67) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Docetaxel and trastuzumab (5 and 1.9 mg/kg, respectively,every seven days 3) induces efficient tumor cell killing in cell line-derived models of SKBR3 cells with HER2 expression with high expression.
|
||||
In Vivo Model | SKBR-3 CDX model | ||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
CN105051032B ADC-I-25 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 62.50% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
|
||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 62.50% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
|
||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 80.00% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
|
||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
4.75 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2020063676A1 ADC-24 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 62.77% (Day 34) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
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||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 76.32% (Day 34) | Positive HER2 expression (HER2 +++) | ||
Method Description |
Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
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||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2017089890A1 ADC24 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 64.72% (Day 52) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
|
||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.72% (Day 52) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
|
||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
ADC-II-9 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 65.40% (Day 12) | Low HER2 expression (HER2-) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
|
||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 68.86% | High HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
|
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.00% (Day 12) | Low HER2 expression (HER2-) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% | High HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
28.10 nM
|
Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
39.91 nM
|
Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2022078260A1 ADC-1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 68.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.79 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
24.59 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
CN105051032B ADC-I-23 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 70.00% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
|
||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 77.50% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
|
||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 80.00% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
|
||||
In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
4.73 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-alpha-amanitin conjugate 3 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 71.25% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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||||
In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.43% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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||||
In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
OHPAS ADC-1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 74.10% (Day 78) | High HER2 expression (HER2 +++) | ||
Method Description |
We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (0.5 mg/kg) on day one (initial tumor volume 100 mm3).
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||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.50% (Day 78) | High HER2 expression (HER2 +++) | ||
Method Description |
We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (2 mg/kg) on day one (initial tumor volume 100 mm3).
|
||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.60 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
Tmab-SSNPP-DM4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.60% (Day 10) | High HER2 expression (HER2+++) | ||
Method Description |
Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
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||||
In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus |
Tmab-SSNPP-DM3 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.60% (Day 10) | High HER2 expression (HER2+++) | ||
Method Description |
Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
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||||
In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus |
Tmab-SPP-DM1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.60% (Day 10) | High HER2 expression (HER2+++) | ||
Method Description |
Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
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||||
In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.22 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.26 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
41.37 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [21] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100.00 nM | Low HER2 expression (HER2+) | ||
Method Description |
The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
HER2-gsADC-47 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 78.82% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.97% (Day 57) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 66.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
ADC-I-1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 80.39% | High HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
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||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Her-30.1036 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 81.41% (Day 17) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.97% (Day 17) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 28) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 28) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
2.10 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Trastuzumab-E-13 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [81] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 81.83% (Day 34) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six days after JIMT-3 cell implantation, when tumors reached an average size of 220-230 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with E-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [81] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 41) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Six days after Calu-3 cell implantation, when tumors reached an average size of 250-260 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with E-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.
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In Vivo Model | Calu-3 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 |
WO2018098269A2 conjugate 68 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 81.97% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1 mg/kg) on day 1.
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In Vivo Model | OVCAR-3 CDX model | ||||
In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 |
Trastuzumab-G-13 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [81] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 82.41% (Day 34) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six days after JIMT-3 cell implantation, when tumors reached an average size of 220-230 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with G-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [81] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 41) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Six days after Calu-3 cell implantation, when tumors reached an average size of 250-260 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with G-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.
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In Vivo Model | Calu-3 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 |
WO2022078260A1 ADC-3 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.60% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.16 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 2 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.96 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-alpha-amanitin conjugate 15 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 86.62% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.16% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
WO2018098269A2 conjugate 67 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 88.84% (Day 28) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1 mg/kg) on day 1.
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In Vivo Model | OVCAR-3 CDX model | ||||
In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 |
Her-30.0643 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 89.51% (Day 17) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.05% (Day 17) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 28) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 28) | Moderate HER2 expression (HER2++) | ||
Method Description |
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.02 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
1.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Trastuzumab-alpha-amanitin conjugate 7 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.64% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [72] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.16% (Day 87) | High HER2 expression (HER2 +++) | ||
Method Description |
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
ADC-III-9 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 93.05% | High HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 93.79% | High HER2 expression (HER2+++/++) | ||
Method Description |
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
76.70 nM
|
Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
T-PBA [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [83] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 93.10% (Day 30) | High HER2 expression (HER2+++) | ||
Method Description |
The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [83] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.20% (Day 30) | High HER2 expression (HER2+++) | ||
Method Description |
The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
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In Vivo Model | SK-OV-3 CDX model | ||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [83] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.40 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [83] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
56.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [83] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
344.60 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
Trastuzumab-C239I-SG3249 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [84] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.00% (Day 50) | Low HER2 expression (HER2+) | ||
Method Description |
The in vivo efficacy of trastuzumab-C239i-SG3249 was investigated after single-dose injections (0.30 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [84] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.20% (Day 40) | Low HER2 expression (HER2+) | ||
Method Description |
The in vivo efficacy of trastuzumab-Flexmab-SG3710 and trastuzumab-C239i-SG3249 ADCs was investigated after single-dose injections (1 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts,and tumor growth was monitored for 85 days. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [84] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.40 pM
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxic effect of Trastuzumab-C239i-SG32490 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of trastuzumab-Flexmab-SG3710 was assessed on the SKBR-3 cell line after five days of incubation.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Trastuzumab-L6 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [85] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.80%±14.40% | Positive HER2 expression (HER2+++/++) | ||
Method Description |
10 mg/kg TS-L6 administrated once weekly2 inhibited tumor growth in nude and nave mice.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [85] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [85] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [85] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.50 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [85] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.25 nM
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
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In Vitro Model | Colon adenocarcinoma | CT26.WT cells | CVCL_7256 |
WO2022078260A1 ADC-5 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.79 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.22 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2022078260A1 ADC-2 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
|
||||
In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
29.01 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 2 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
52.21 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Anti-HER2_vc-1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [86] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.20% (Day 30) | High HER2 expression (HER2+++) | ||
Method Description |
Approximately 2 million cells (100 L of the mixture) were implanted subcutaneously to the right flank of 68 weeks old female SCID/beige mice. After the tumors reached about 200 to 400 mm3 ,the mice were treated with either anti-HER2_vc-1 or non-targeted ADC at 3 mpk (IP,Q5dx3).
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||||
In Vivo Model | Breast cancer CDX model | ||||
In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
Experiment 2 Reporting the Activity Date of This ADC | [86] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 30) | High HER2 expression (HER2+++) | ||
Method Description |
Approximately 2 million cells (100 L of the mixture) were implanted subcutaneously to the right flank of 68 weeks old female SCID/beige mice. After the tumors reached about 200 to 400 mm3 ,the mice were treated with either anti-HER2_vc-1 or non-targeted ADC at 10 mpk (IP,Q5dx3).
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In Vivo Model | Breast cancer CDX model | ||||
In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 |
WO2017089890A1 ADC23 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.52% (Day 52) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.72% (Day 52) | Moderate HER2 expression (HER2++) | ||
Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
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Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.35 nM
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High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.44 nM
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High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
HER2-gsADC-50 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.95% (Day 57) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 66.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2022078260A1 ADC-7 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.30% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.42 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 2 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.49 nM
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Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
HER2-acetal-ADC 12 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [87] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 30) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
NOD-SCID mice with heterotopic SKBR-3 tumor xenografts were injected intravenously with either ADC 12 (1.12 mg/kg; group A), PBS 1x (vehicle; group B) or Kadcyla (1.12 mg/kg; group C) and tumor volume was measured every 2-3 days for 30 days.
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In Vivo Model | SKBR-3 CDX model | ||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [87] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.22 nM
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Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [87] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
PF-06888667 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [88] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 35) | High HER2 expression (HER2+++) | ||
Method Description |
Athymic mice were inoculated with HER2-positive N87 tumor cells. When tumors reached approximately 300 mm3, mice were administered PBS vehicle or the indicated ADCs at 1 mg/kg every 4 days (days 1, 5, 9, 13).
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Trastuzumab-PNUEDAGly5 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [89] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 60) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
1,000,000 EMT6 mouse breast cancer cells expressing human HER-2 previously determined to be suitable for in vivo growth, were implanted into theright mammary fat pads of female Balb/c mice. Animals were treated onthe same day (day 13) and 7 days later (day 20) byintravenous injection of the reference ADC Kadcyla (15 mg/kg), Trastuzumab-PNU-EDA-Glys (1 mg/kg) or vehicle control.
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In Vivo Model | EMT6 CDX model (Expressing hHER2) | ||||
In Vitro Model | Mammary gland malignant neoplasms | EMT6 cells (High HER2 expression) | CVCL_1923 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [115] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
6.90 ng/mL
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High CD30 expression (CD30 +++) | ||
Method Description |
Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
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In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells | CVCL_1324 | ||
Experiment 2 Reporting the Activity Date of This ADC | [115] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | < 10.00 ug/mL | Low CD30 expression (CD30 +) | ||
Method Description |
Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
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In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 |
Tras-Gly5-EDA-Pnu [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 26) | High HER2 expression (HER2+++; 170,000 HER2 molecules/cell) | ||
Method Description |
JIMT-1 cells were transplanted subcutaneously into CB17.SCID mice and tumors were allowed to grow to a volume of 100-150 mm3. Mice were then treated intravenously 3 times weekly with the 1 mg/kg ADC preparations.
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In Vivo Model | Trastuzumab-resistant breast cancer CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.70 ng/mL
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High HER2 expression (HER2+++; 694,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.70 ng/mL
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Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
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In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
CN105051032B ADC-I-6 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1.25 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≊ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 20 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≉ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
9.47 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-10 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≋ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1.25 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≍ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 20 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≌ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
6.28 ng/mL
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Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-11 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≎ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1.25 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≐ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 20 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≏ 100.00% (Day 56) | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
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In Vivo Model | BT-474 CDX model | ||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
4.77 ng/mL
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Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2018098269A2 conjugate 43B [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 76) | High HER2 expression (HER2+++) | ||
Method Description |
Female CB-17 SCID mice were inoculated subcutaneously with NCI-N87 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1.5 mg/kg) on day 1.
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In Vivo Model | NCI-N87 CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.01 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.15 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.53 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Trastuzumab-AJICAP-maytansinoid [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Minimal Effective Dose (MED) | < 5.00 mg/kg | High HER2 expression (HER2+++) | ||
Method Description |
Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
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In Vivo Model | Gastric cancer CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Maximum Tolerated Dose (MTD) | > 120.00 mg/kg | High HER2 expression (HER2+++) | ||
Method Description |
Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
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In Vivo Model | Gastric cancer CDX model | ||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2017089895A1 ADC33 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
53.68% (Day 36)
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (0.5 mg/kg).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
89.84% (Day 36)
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.23 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.33 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC34 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
58.23% (Day 36)
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (0.5 mg/kg).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
87.94% (Day 36)
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC24 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
64.86% (Day 52)
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
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||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
95.44% (Day 52)
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (5 mg/kg).
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||||
In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC23 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
96.08% (Day 52)
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Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
99.23% (Day 52)
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (5 mg/kg).
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In Vivo Model | JIMT-1 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.21 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.35 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.44 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 8 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 9 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2013055987A1 Tmab-110 [Investigative]
Obtained from the Model Organism Data
Experiment 1 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 5.82% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
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In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 2 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 31.56% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 3 mg/kg ADC dosing on day 0.
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In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 3 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 47.90% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 6 mg/kg ADC dosing on day 0.
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||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
102.78 ug/mL
|
High HER2 expression (HER2 +++) | ||
Method Description |
Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 ug/mL | Negative HER2 expression (HER2 -) | ||
Method Description |
Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014159981A2 ADC-110 [Investigative]
Obtained from the Model Organism Data
Experiment 1 Reporting the Activity Date of This ADC | [93] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 69.98% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
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||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 2 Reporting the Activity Date of This ADC | [93] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.86% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 3 mg/kg ADC dosing on day 0.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 3 Reporting the Activity Date of This ADC | [93] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.16% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 6 mg/kg ADC dosing on day 0.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 |
WO2014159981A2 ADC-120 [Investigative]
Obtained from the Model Organism Data
Experiment 1 Reporting the Activity Date of This ADC | [93] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 75.29% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 0.3 mg/kg ADC dosing on day 0.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 2 Reporting the Activity Date of This ADC | [93] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 86.01% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 3 Reporting the Activity Date of This ADC | [93] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.39% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 3 mg/kg ADC dosing on day 0.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 |
WO2013055987A1 Tmab-101 [Investigative]
Obtained from the Model Organism Data
Experiment 1 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 78.27% (Day 11) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 1 mg/kg injection of the ADC.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 2 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 86.68% (Day 14) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 3 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 87.51% (Day 11) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 3 mg/kg injection of the ADC.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Experiment 4 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.92% (Day 11) | High HER2 expression (HER2 +++) | ||
Method Description |
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 10 mg/kg injection of the ADC.
|
||||
In Vivo Model | Breast cancer model MMTV-HER2 Fo5 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
22.12 ug/mL
|
High HER2 expression (HER2 +++) | ||
Method Description |
Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [92] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 ug/mL | Negative HER2 expression (HER2 -) | ||
Method Description |
Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
ADC3-5 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
62.80%
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | HCC1569 cells | CVCL_1255 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
4.36 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | HCC1569 cells | CVCL_1255 |
ADC3-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
66.40%
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | HCC1569 cells | CVCL_1255 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
78.60%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.68 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
3.15 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | HCC1569 cells | CVCL_1255 |
ADC3-4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
74.40%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.68 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC3-3 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
79.00%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.50 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC3-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
79.10%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.52 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-49 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
81.10%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.20 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC-2-64-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
82.10%
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
92.50%
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.15 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
2.56 nM
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 |
ADC2-50 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
83.00%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.21 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-A [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
83.10%
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
88.40%
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
95.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.03 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.17 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
3.94 nM
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 |
ADC-2-64-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
83.20%
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
94.00%
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.08 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.30 nM
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 |
ADC2-51 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
83.20%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.19 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-57 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
83.60%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.21 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-58 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
84.70%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.21 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC-2-62-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
84.80%
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
91.70%
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.09 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
1.84 nM
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 |
ADC2-46 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
85.60%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-45 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
85.80%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC-2-63-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
86.10%
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
94.40%
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.09 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.30 nM
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 |
ADC-2-62-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
86.30%
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
94.20%
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.07 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.29 nM
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 |
ADC2-54 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
86.50%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.14 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-44 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
87.10%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.19 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-48 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
87.80%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.11 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-61 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
87.90%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.17 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-59 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
88.10%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC-2-63-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
88.90%
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
91.70%
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.18 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
3.07 nM
|
Low HER2 expression (HER2 +) | ||
Method Description |
Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
|
||||
In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 |
ADC2-38 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
89.10%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-27 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
89.80%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-60 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
90.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.27 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-34 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
90.60%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.21 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-35 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
91.20%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.24 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-24 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
91.50%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.14 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-22 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
91.50%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.11 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-30 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
91.80%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.13 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-B [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
92.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
92.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
92.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
92.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 6 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 7 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 8 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-23 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
93.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-25 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
93.60%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-40 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
94.20%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.22 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-33 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
94.20%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.26 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-32 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
95.20%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-26 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
95.50%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.08 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-37 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Maximum inhibition efficiency (MIE) |
96.80%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.43 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
76.50%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.26 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-7-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
90.70%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.13 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-6-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
91.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
95.70%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
96.30%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-9-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
96.50%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
ADC2-9-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Max inhibition rate (MIR) |
97.40%
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [94] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.01 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Trastuzumab DVD-ADC [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [95] | ||||
Efficacy Data | Inhibition rate (100nM) |
0.00%
|
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-) | ||
Method Description |
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 2 Reporting the Activity Date of This ADC | [95] | ||||
Efficacy Data | Inhibition rate (100nM) |
0.00%
|
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-) | ||
Method Description |
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
Experiment 3 Reporting the Activity Date of This ADC | [95] | ||||
Efficacy Data | Inhibition rate (100nM) | > 50.00% | High HER2 expression (HER2+++); Moderate TRKB expression (TRKB++) | ||
Method Description |
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
HER-SG3249 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [96] | ||||
Efficacy Data | Half Maximum Growth Inhibitory Concentration (GI50) |
1.74 ng/mL
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxic effect of Her-SG3249 was assessed in cell viability assays for breast cancer. The potency of Her-SG3249 was assessed on the SKBR-3 cell line. Process aggregation assessed by SEC.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Site-specific HER-SG3249 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [96] | ||||
Efficacy Data | Half Maximum Growth Inhibitory Concentration (GI50) |
2.62 ng/mL
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxic effect of site-specific Her-SG3249 was assessed in cell viability assays for breast cancer. The potency of site-specific Her-SG3249 was assessed on the SKBR-3 cell line. Process aggregation assessed by SEC.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Trastuzumab-Compound (la) DAR 8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.80 pM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15.00 pM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
61.00 pM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
Experiment 5 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | High HER2 expression (HER2+++/++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 6 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | High grade ovarian serous adenocarcinoma | FU-OV-1 cells | CVCL_2047 |
Trastuzumab-Compound (lc) DAR 8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.00 pM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
TTZ-2-MMAE [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [97] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15.70 pM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
TTZ-1-MMAE [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [97] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
20.00 pM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
TTZ-4-MMAE [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [97] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
22.10 pM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
TTZ-3-MMAE [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [97] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
27.20 pM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Trastuzumab-Compound (ld) DAR 1.6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
74.00 pM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
HER2-azide-alkyne MMAE conjugate [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
88.00 pM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.90 ng/mL
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low HER2 expression (HER2+) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
OHPAS ADC-4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.01 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [30] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
ADC Trast-14 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.01 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
|
||||
In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
Experiment 2 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2017089895A1 ADC77 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC62 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
ADC Trast-11 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
|
||||
In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
Experiment 2 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2017089890A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC77 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2018098269A2 conjugate 52 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.18 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15.82 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2018098269A2 conjugate 46A [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.56 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2018098269A2 conjugate 48 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
18.47 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
HER2-gsADC-49 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 66.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2017089895A1 ADC53 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC50 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC49 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC48 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC45 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC44 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC43 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC42 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC41 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC39 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC38 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC32 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.32 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.35 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.40 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC29 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.41 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.49 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC28 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.36 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.36 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC25 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.36 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC17 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC17 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC38 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC42 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC44 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC48 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC50 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC53 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC25 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.36 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC28 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.36 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.36 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC29 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.41 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.49 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC32 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.32 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.35 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.40 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC39 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC41 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC43 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC45 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC49 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC78 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.33 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.76 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.40 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.50 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.70 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.29 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.60 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.78 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-14 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.19 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2018098269A2 conjugate 46B [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.03 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
100.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
T-DM1-2.6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [73] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 66.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2017089895A1 ADC55 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC51 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC47 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC37 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC37 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC47 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC51 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC55 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC52 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2018098269A2 conjugate 50 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.19 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.84 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2017089895A1 ADC54 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC30 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.15 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.19 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.30 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.35 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.41 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC27 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.29 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.43 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC16 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC54 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC27 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.29 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.43 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC30 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.30 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.35 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.41 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC58 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.64 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.73 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.95 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC14 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC16 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC58 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.64 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.73 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.95 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC52 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.40 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-7 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.40 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
79.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC31 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC26 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.22 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC20 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.29 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC20 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.29 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC26 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC62 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014068443A1 ADC22 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 0.08 nM | High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.54 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2017089895A1 ADC21 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.25 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.88 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC36 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.22 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
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Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.15 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.42 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Esophageal adenocarcinoma | OE19 cells | CVCL_1622 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.75 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.19 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 8 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.37 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 9 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 10 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC14 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC21 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
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High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.25 nM
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High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.88 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-11 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.96 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.60 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.60 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC18 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC9 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.18 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC7 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.44 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.32 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.97 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.21 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.32 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.97 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.21 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC18 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC7 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.44 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC9 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.10 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC35 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.19 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
21.00 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
Trastuzumab-iCME [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [101] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM±0.07 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treating with ADC and cholesterol-linked endosome-disruptive peptide (Chol-EDP) for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [101] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.00 nM±5.00 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treating with ADC for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [101] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.00 nM±8.00 nM
|
Negative HER2 expression (HER2 -) | ||
Method Description |
To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treatment for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
CN109641910A ADC-3 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.80 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.60 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
118.80 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.30 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.40 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC10 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.64 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Trastuzumab-Compound (lc) [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2017089890A1 ADC10 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.64 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-15 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.76 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.05 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC19 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
Trastuzumab-Compound (Ib) DAR1.5 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [67] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2017089890A1 ADC19 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC35 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.19 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC36 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.13 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.22 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
HER2-norbornene-tetrazine MMAE conjugate [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
21.80 ng/mL
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low HER2 expression (HER2+) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
ADC-II-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2017089890A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.42 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Esophageal adenocarcinoma | OE19 cells | CVCL_1622 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.75 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.19 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 6 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC31 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.14 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.10 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.70 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC5 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.15 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.19 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.40 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.97 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.01 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 8 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 9 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC5 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.15 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.40 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.97 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.04 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
HER2-cyclopropene-tetrazine MMAE conjugate [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15.40 ng/mL
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [98] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low HER2 expression (HER2+) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
ADC-III-1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
CN109641910A ADC-5 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.40 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
29.40 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
105.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
353.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2014068443A1 ADC79 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.53 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
762.24 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2017089895A1 ADC15 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.52 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.70 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC15 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
Trastuzumab-Val-Cit linker-MMAE 2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [102] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.18 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2017089895A1 ADC13 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.19 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.63 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.87 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.09 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC13 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.19 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.09 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
ADC-II-5 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
High HER2 expression (HER2+++/++) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [76] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Low HER2 expression (HER2-) | ||
Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
HER2-B Antibody-Compound (XIV) [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [103] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2017089895A1 ADC12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.51 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.79 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.01 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC3 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.29 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.32 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.04 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.34 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.63 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 8 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 9 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.01 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
233.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-13 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.20 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.79 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.90 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.41 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
31.60 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014068443A1 ADC12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.21 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.65 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
796.00 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
CN109641910A ADC-16 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.95 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-9 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.25 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
23.90 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
30.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
30.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
77.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014068443A1 ADC39 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.25 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.81 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
539.32 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 652.88 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2017089895A1 ADC1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.41 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.47 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 4 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.69 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 6 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 7 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.33 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 8 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
241 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 9 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
275 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2017089895A1 ADC76 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
Trastuzumab-MCC-CpG conjugate [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [104] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [104] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.43 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
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In Vitro Model | Esophageal adenocarcinoma | OE19 cells | CVCL_1622 | ||
Experiment 3 Reporting the Activity Date of This ADC | [104] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2017089890A1 ADC76 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC3 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.29 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.04 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.34 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.63 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2020063676A1 ADC-4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.30 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
ADC Trast-10 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.30 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
CN109641910A ADC-6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.30 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.51 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
37.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC61 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.32 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [91] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.32 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
WO2014068443A1 ADC26 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.33 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.91 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.94 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC16 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.36 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.85 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
646.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
836.00 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2020063676A1 ADC-17 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC7 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.32 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2020063676A1 ADC-15 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.38 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.69 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 850.00 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC42 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.39 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.55 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC54 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.39 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.68 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
38.18 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC60 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.39 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.80 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
467.40 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
977.31 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC23 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.39 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.71 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2020063676A1 ADC-3 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.43 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC24 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.43 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.13 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC37 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.44 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.73 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC10 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.44 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.13 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
645.00 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC52 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.44 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.73 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
78.29 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
297.62 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
ADC Trast-7 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.46 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [99] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative HER2 expression (HER2-) | ||
Method Description |
In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2014068443A1 ADC53 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.46 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.73 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.76 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2020063676A1 ADC-13 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.47 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2017089890A1 ADC1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.47 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.69 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 4 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
241.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 5 Reporting the Activity Date of This ADC | [75] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
275.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2020063676A1 ADC-6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.48 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.48 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2020063676A1 ADC-16 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.49 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.52 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.03 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
123.00 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
580.30 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2020063676A1 ADC-14 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.53 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC15 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.56 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.04 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.13 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
749.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC9 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.57 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
38.70 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
626.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
734.00 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2014068443A1 ADC71 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.60 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.03 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC11 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.64 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.26 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC72 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.64 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.27 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC31 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.65 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.30 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC49 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.67 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.71 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC38 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.68 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.92 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
678.88 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 971.38 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2020063676A1 ADC-11 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.73 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC63 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.75 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.79 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
650.25 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
909.59 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC78 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.76 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.22 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
247.49 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC55 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.78 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.18 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.83 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC19 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.78 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.01 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.05 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC28 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.79 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.34 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 517.93 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2020063676A1 ADC-12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.82 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC64 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.86 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.58 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
180.13 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
329.21 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2014068443A1 ADC73 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.91 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.94 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
323.99 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2014068443A1 ADC29 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.94 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.39 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
220.98 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC48 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.95 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.39 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC33 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.97 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.09 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
25.12 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
55.12 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Trastuzumab-DVP-linker-MMAE 1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [102] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.00 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2014068443A1 ADC62 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.04 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.32 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC75 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.07 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.09 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC77 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.07 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.29 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
180.28 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC66 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC21 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.15 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.35 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC41 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.12 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.29 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC17 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.15 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.48 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.27 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
16.10 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2014068443A1 ADC76 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.16 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.36 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC25 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.17 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.52 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC59 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.18 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.90 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
704.93 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC65 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.20 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.36 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
44.69 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
86.59 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2014068443A1 ADC30 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.22 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.88 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.26 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC34 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.33 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.96 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.28 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
29.45 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2020063676A1 ADC-10 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.36 nM
|
Positive HER2 expression (HER2 +++) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [71] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50.00 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.37 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
292.35 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC20 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.41 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.68 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.72 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC61 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.43 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.46 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
17.83 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Trastuzumab-DVP-linker-MMAE 4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [102] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.45 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2022078260A1 ADC-6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.45 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
19.10 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC36 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.49 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.06 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC56 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.58 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.70 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
166.11 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
253.89 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2022078260A1 ADC-8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.86 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [79] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.58 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC70 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.91 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.33 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
19.62 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Trastuzumab-DVP-linker-MMAE 3 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [102] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.40 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2014068443A1 ADC47 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.64 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500.46 nM | High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC50 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.96 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.01 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC32 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.10 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.23 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC51 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.28 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.61 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
HER2 ADC-19 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.80 nM±1.40 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 | ||
Experiment 3 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
CN109641910A ADC-10 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.80 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
124.00 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 4 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 5 Reporting the Activity Date of This ADC | [100] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
300.00 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.
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In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
WO2014068443A1 ADC27 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.54 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.30 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC35 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.52 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC80 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.88 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.05 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC58 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.52 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
40.99 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2018098269A2 conjugate 34B [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.96 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
11.73 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
17.97 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
20.99 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
29.39 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2014068443A1 ADC82 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.99 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
35.58 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC67 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
10.35 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
95.43 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2018098269A2 conjugate 34A [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
11.06 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
21.91 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
22.07 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
27.70 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
29.14 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
HER2 ADC-20 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
11.30 nM±2.70 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
|
||||
In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 | ||
Experiment 3 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014068443A1 ADC74 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.40 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
68.25 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
HER2 ADC-18 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.00 nM±5.90 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
487.00 nM±194.00 nM
|
Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 3 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 | ||
Experiment 4 Reporting the Activity Date of This ADC | [105] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 500 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014068443A1 ADC68 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14.21 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
17.62 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
369.90 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
697.16 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 |
WO2014068443A1 ADC57 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
17.02 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
525.65 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
HER2-acetal-ADC 11 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [87] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
22.00 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [87] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
100 nM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2014068443A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
27.27 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
33.94 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
T-Py-DM1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [106] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were plated at 5,000, 2,500, and 2,500 cells/well, respectively, and allowed to rest for 24 h. Five-fold serial dilutions of the antibodies were added starting at 150 nM and incubated for 72-144 h.
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||||
In Vitro Model | Bone marrow neuroblastoma | SH-SY5Y cells | CVCL_0019 | ||
Experiment 2 Reporting the Activity Date of This ADC | [106] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
144 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were plated at 5,000, 2,500, and 2,500 cells/well, respectively, and allowed to rest for 24 h. Five-fold serial dilutions of the antibodies were added starting at 150 nM and incubated for 72-144 h.
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||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
Trastuzumab-RSL3-NH2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [107] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
100.00 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
The inhibitory activity of Trastuzumab-RSL3-NH2 against cancer cell growth was evaluated by MTT cytotoxicity assay.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
WO2018098269A2 conjugate 31A [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2018098269A2 conjugate 31B [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 100.00 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2021249228A1 ADC-10 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
115.99 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2021249228A1 ADC-2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
116.33 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2021249228A1 ADC-12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [66] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
135.30 nM
|
Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
WO2014068443A1 ADC81 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
162.74 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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In Vitro Model | Amelanotic melanoma | MDA-MB-435 cells | CVCL_0417 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
370.55 nM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Amelanotic melanoma | MDA-MB-435 cells | CVCL_0417 |
WO2014068443A1 ADC43 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
162.75 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 517.76 nM | High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Trastuzumab-PC4AP-DOX [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [108] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
203 nM
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
SK-BR-3 cells were incubated with 500 nM of trastuzumab and 39 respectively for 30 min at rt, followed by incubation After washing 3 times with PBS, cells were stained with DAPI (300 uL, 10 ug/mL) at rt for 7 min.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [108] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2 -) | ||
Method Description |
MCF7 cells were incubated with 500 nM of trastuzumab and 39 respectively for 30 min at rt, followed by incubation After washing 3 times with PBS, cells were stained with DAPI (300 uL, 10 ug/mL) at rt for 7 min.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2018098269A2 conjugate 25 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2018098269A2 conjugate 28 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | High HER2 expression (HER2+++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [82] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | < 300.00 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2014068443A1 ADC44 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
311.48 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC13 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
367.92 nM
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
500.49 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
501.26 nM
|
High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
WO2014068443A1 ADC45 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 502.15 nM | High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 507.59 nM | High HER2 expression (HER2+++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 3 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [68] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Negative HER2 expression (HER2-) | ||
Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Tras-Gly3-Vakl-Cit-PAB-PNU-159682 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 ng/mL
|
High HER2 expression (HER2+++; 694,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
12.00 ng/mL
|
Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
T-D4-1508 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.11 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 2 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 ng/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 3 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
T-D6-1508 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.14 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 2 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 ng/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 3 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
T-D8-1508 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.16 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 2 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 ng/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 3 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
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||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
Trastuzumab-SG3227 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [110] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.48 ng/mL
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxic effect of Trastuzumab-SG3227 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of Trastuzumab-SG3227 was assessed on the NCI-N87 cell line.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [110] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2130.00 ng/mL
|
Negative expression (HER2-) | ||
Method Description |
The cytotoxic effect of Trastuzumab-SG3227 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of Trastuzumab-SG3227 was assessed on the MDA-MB-468 cell line.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 |
Tras-Gly5-EDA-Nemo [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.80 ng/mL
|
High HER2 expression (HER2+++; 694,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Tras-Gly5-EDA-Dox [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.80 ng/mL
|
High HER2 expression (HER2+++; 694,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Trastuzumab-SG3600 high DAR [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [111] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.60 ng/mL
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
Experiment 2 Reporting the Activity Date of This ADC | [111] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.37 ng/mL
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [111] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.90 ng/mL
|
Low HER2 expression (HER2+) | ||
Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 4 Reporting the Activity Date of This ADC | [111] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
36.10 ng/mL
|
Negative expression (HER2-) | ||
Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 5 Reporting the Activity Date of This ADC | [111] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative expression (HER2-) | ||
Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
T-D2-1508 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.40 ng/mL
|
Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 2 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 ng/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
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In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 3 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Moderate HER2 expression (HER2 ++) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-361 cells | CVCL_0620 | ||
Experiment 4 Reporting the Activity Date of This ADC | [109] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low HER2 expression (HER2 +) | ||
Method Description |
Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 |
Tras-Gly5-May [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
18.00 ng/mL
|
High HER2 expression (HER2+++; 694,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
|
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [90] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 110.00 ng/mL | Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell) | ||
Method Description |
Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
T-FcBP-DM1 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [112] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
81.64 ng/mL
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Experiment 2 Reporting the Activity Date of This ADC | [112] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 800 ng/mL | Negative HER2 expression (HER2 -) | ||
Method Description |
Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
|
||||
In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
Trastuzumab-Me-PRX conjugate [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [113] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.50 uM
|
Negative HER2 expression (HER2-) | ||
Method Description |
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
|
||||
In Vitro Model | Endocervical adenocarcinoma | HeLa cells | CVCL_0030 | ||
Experiment 2 Reporting the Activity Date of This ADC | [113] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.75 uM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
|
||||
In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Experiment 3 Reporting the Activity Date of This ADC | [113] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.02 uM
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 |
Trastuzumab/nab-paclitaxel [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [114] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.24 ug/mL
|
Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Paclitaxel, nab-paclitaxel and trastuzumab/nab-paclitaxel, respectively, at a concentration of 0.24 ug/ml paclitaxel equivalent for 48 h.
|
||||
In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 |
Her-30.1033 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.01 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 2 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.03 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 3 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
7.90 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
Her-30.1165 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.11 nM
|
High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
|
||||
In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
Experiment 2 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 nM | High HER2 expression (HER2 +++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [80] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 nM | Moderate HER2 expression (HER2++) | ||
Method Description |
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 |
CN105051032B ADC-I-33 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
2.89 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
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|
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-38 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
5.13 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-19 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
5.18 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-20 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
5.72 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-36 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
5.74 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-22 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
6.70 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-39 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
7.00 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-21 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
7.09 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-35 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
10.30 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-32 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
12.70 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-37 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
13.00 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-18 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
14.30 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
CN105051032B ADC-I-24 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [74] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
68.40 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
Method Description |
The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-MMAE conjugate DAR12 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.04 nM
7.13 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-MMAE conjugate DAR8 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.05 nM
8.79 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-MMAE conjugate DAR6 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.08 nM
12.68 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-MMAE conjugate DAR4 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [116] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.10 nM
16.05 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-MMAE conjugate DAR2 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.07 nM
10.67 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
Experiment 3 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.41 nM
6.20 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
Trastuzumab-Gal-beta-1,4GlcNAc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.04 nM
6.08 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.07 nM
11.07 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Trastuzumab-Glc-beta-1,4GlcNAc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.04 nM
6.39 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.07 nM
10.67 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
|
||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
Trastuzumab-Man-beta-1,4GlcNAc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10.00 uM | Negative HER2 expression (HER2-) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
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In Vitro Model | Invasive breast carcinoma | T-47D cells | CVCL_0553 | ||
Experiment 2 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.05 nM
7.06 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 3 Reporting the Activity Date of This ADC | [117] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.07 nM
11.07 ng/mL |
High HER2 expression (HER2+++) | ||
Method Description |
The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
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In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
ADCT-502 [Terminated in phase 1]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [118] | ||||
Efficacy Data | Objective Response Rate (ORR) |
20.00% (150 ug/kg)
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Patients Enrolled |
Patients with HER2-positive advanced solid tumors.
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Administration Dosage |
Seven dose cohorts (30, 60, 120, 150, 180, 210, 240 ug/kg on day 1, iv once every 3 weeks.
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Related Clinical Trial | |||||
NCT Number | NCT03125200 | Clinical Status | Phase 1 | ||
Clinical Description |
A phase 1, open-label, dose-escalation study to evaluate the safety, tolerability, pharmacokinetics, and antitumor activity of ADCT-502 in patients with advanced solid tumors with HER2 expression.
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References
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