Payload Information
General Information of This Payload
| Payload ID | PAY0JAEKD |
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| Name | Eribulin |
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| Synonyms |
Eribulin; 253128-41-5; Eribulin [INN]; Halaven; UNII-LR24G6354G; ER 086526; CHEBI:63587; LR24G6354G; 2-(3-Amino-2-hydroxypropyl)hexacosahydro-3-methoxy-26-methyl-20,27-bis(methylene)11,15-18,21-24,28-triepoxy-7,9-ethano-12,15-methano-9H,15H-furo(3,2-i)furo(2',3'-5,6)pyrano(4,3-b)(1,4)dioxacyclopentacosin-5-(4H)-one; B 1939; (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]hentetracontan-24-one; ER-086526; (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-bis(methylene)-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.1(3,32).1(3,33).1(6,9).1(12,16).0(18,22).0(29,36).0(31,35)]hentetracontan-24-one; NSC-707389; ERIBULIN [MI]; ERIBULIN [VANDF]; ERIBULIN [MART.]; ERIBULIN [WHO-DD]; e7389-lf; GTPL6813; CHEMBL1683590; SCHEMBL15783821; EX-A4873D; UFNVPOGXISZXJD-JBQZKEIOSA-N; DTXSID101009321; AKOS040740784; AT36513; DB08871; NCGC00510497-02; BP-29357; HY-13442; MS-31267; Q408717; (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]hentetracontan-24-o; ;(1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.1~3,32~.1~3,33~.1~6,9~.1~12,16~.0~18,22~.0~29,36~.0~31,35~]hentetracontan-24-one (non-preferred name)
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| Target | Microtubule (MT) | |||||
| Structure |
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| Formula | C40H59NO11 |
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| Isosmiles | C[C@@H]1C[C@@H]2CC[C@H]3C(=C)C[C@@H](O3)CC[C@]45C[C@@H]6[C@H](O4)[C@H]7[C@@H](O6)[C@@H](O5)[C@@H]8[C@@H](O7)CC[C@@H](O8)CC(=O)C[C@H]9[C@H](C[C@H](C1=C)O2)O[C@@H]([C@@H]9OC)C[C@@H](CN)O |
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| PubChem CID | ||||||
| InChI |
InChI=1S/C40H59NO11/c1-19-11-24-5-7-28-20(2)12-26(45-28)9-10-40-17-33-36(51-40)37-38(50-33)39(52-40)35-29(49-37)8-6-25(47-35)13-22(42)14-27-31(16-30(46-24)21(19)3)48-32(34(27)44-4)15-23(43)18-41/h19,23-39,43H,2-3,5-18,41H2,1,4H3/t19-,23+,24+,25-,26+,27+,28+,29+,30-,31+,32-,33-,34-,35+,36+,37+,38-,39+,40+/m1/s1
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| InChIKey |
UFNVPOGXISZXJD-JBQZKEIOSA-N
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| IUPAC Name |
(1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]hentetracontan-24-one
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| Pharmaceutical Properties | Molecule Weight |
729.9 |
Polar area |
146 |
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Complexity |
1380 |
xlogp Value |
1.1 |
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Heavy Count |
52 |
Rot Bonds |
4 |
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Hbond acc |
12 |
Hbond Donor |
2 |
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The activity data of This Payload
| Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
|---|---|---|---|---|---|---|
| Half Maximal Inhibitory Concentration (IC50) | 1.66 | nM |
MES-SA cells
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Uterine sarcoma
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[1] | |
| Half Maximal Inhibitory Concentration (IC50) | 1.66 | nM |
MES-SA cells
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Uterine sarcoma
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[2] | |
| Half Maximal Inhibitory Concentration (IC50) | 20 | nM |
DLD-1 cells
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Colon adenocarcinoma
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[1] | |
| Half Maximal Inhibitory Concentration (IC50) | 20 | nM |
DLD-1 cells
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Colon adenocarcinoma
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[2] | |
| Half Maximal Inhibitory Concentration (IC50) | 204 | nM |
HCT 15 cells
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Colon adenocarcinoma
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[1] | |
| Half Maximal Inhibitory Concentration (IC50) | 204 | nM |
HCT 15 cells
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Colon adenocarcinoma
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[2] | |
| Half Maximal Inhibitory Concentration (IC50) | 5 | nM |
PT-45 cells
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Pancreatic carcinoma
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[3] |
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
BB-1701 [Phase 2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
30%
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| Patients Enrolled |
Key eligibility: Adults (≥18) with advanced/metastatic HER2+ tumors (measurable per RECIST 1.1), ECOG 0-1, life expectancy ≥12 weeks. Major exclusions: active CNS metastases requiring steroids (>10mg prednisone), Grade ≥2 peripheral neuropathy, QTcF >450/470ms (M/F), active ILD/pneumonitis, HIV/HBV/HCV infections, or prior cumulative doxorubicin >360mg/m2. Fresh tumor tissue required for HER2 confirmation.
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| Administration Dosage |
BB-1701 will be administered as an intravenous infusion, every 3 weeks or every 4 weeks or every 6 weeks.
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| Related Clinical Trial | |||||
| NCT Number | NCT04257110 | Phase Status | PHASE1 | ||
| Clinical Description |
A First-in-human, Open Label, Multiple Dose, Dose Escalation and Cohort Expansion Phase I Study to Investigate the Safety, Tolerability, Pharmacokinetics and Antitumor Activities of BB-1701 in Subjects With Locally Advanced/Metastatic HER2 Expressing Solid Tumors
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| Primary Endpoint |
Primary endpoints include safety evaluation (AEs, SAEs, DLTs) and MTD determination during Cycle 1 (21-day cycles) in HER2-expressing solid tumor patients, with monitoring continuing for up to 2 years to assess BB-1701's safety profile.
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| Other Endpoint |
Secondary objectives comprise PK characterization (AUC0-inf, Cmax), immunogenicity assessment (ADA incidence), and preliminary anti-tumor activity evaluation (ORR, PFS, DOR) through serial tumor assessments per RECIST 1.1 for up to 2 years.
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| Experiment 2 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Disease control rate (DCR) |
60%
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| Patients Enrolled |
Key eligibility: Adults (≥18) with advanced/metastatic HER2+ tumors (measurable per RECIST 1.1), ECOG 0-1, life expectancy ≥12 weeks. Major exclusions: active CNS metastases requiring steroids (>10mg prednisone), Grade ≥2 peripheral neuropathy, QTcF >450/470ms (M/F), active ILD/pneumonitis, HIV/HBV/HCV infections, or prior cumulative doxorubicin >360mg/m2. Fresh tumor tissue required for HER2 confirmation.
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| Administration Dosage |
BB-1701 will be administered as an intravenous infusion, every 3 weeks or every 4 weeks or every 6 weeks.
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| Related Clinical Trial | |||||
| NCT Number | NCT04257110 | Phase Status | PHASE1 | ||
| Clinical Description |
A First-in-human, Open Label, Multiple Dose, Dose Escalation and Cohort Expansion Phase I Study to Investigate the Safety, Tolerability, Pharmacokinetics and Antitumor Activities of BB-1701 in Subjects With Locally Advanced/Metastatic HER2 Expressing Solid Tumors
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| Primary Endpoint |
Primary endpoints include safety evaluation (AEs, SAEs, DLTs) and MTD determination during Cycle 1 (21-day cycles) in HER2-expressing solid tumor patients, with monitoring continuing for up to 2 years to assess BB-1701's safety profile.
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| Other Endpoint |
Secondary objectives comprise PK characterization (AUC0-inf, Cmax), immunogenicity assessment (ADA incidence), and preliminary anti-tumor activity evaluation (ORR, PFS, DOR) through serial tumor assessments per RECIST 1.1 for up to 2 years.
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| Experiment 3 Reporting the Activity Date of This ADC | [5] | ||||
| Patients Enrolled |
Key eligibility: Adults (≥18) with HER2-positive/HER2-low metastatic BC (1-3 prior chemo regimens, T-DXd exposed), measurable disease (RECIST 1.1), ECOG 0-1. Major exclusions: active CNS metastases, prior eribulin, Grade ≥2 peripheral neuropathy/ILD, QTcF >470ms, uncontrolled infections (HIV/HBV/HCV exceptions), or LVEF <50%. Tumor tissue must be available for central HER2 confirmation.
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| Administration Dosage |
BB-1701 will be administered as an intravenous infusion, every 3 weeks (21-day cycle).
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| Related Clinical Trial | |||||
| NCT Number | NCT06188559 | Phase Status | PHASE2 | ||
| Clinical Description |
An Open-label, Multicenter, Phase 2 Dose Optimization and Expansion Study to Evaluate the Safety and Efficacy of BB-1701, an Anti-human Epidermal Growth Factor Receptor 2 (Anti-HER2) Antibody-drug Conjugate (ADC), in Previously Treated Subjects With HER2-positive or HER2-low Unresectable or Metastatic Breast Cancer
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| Primary Endpoint |
Primary endpoints include comprehensive safety evaluation (AEs, lab abnormalities, vital signs, ECGs, ECOG status) during dose optimization (Part 1, 35 months) and ORR assessment by investigator (Part 1) or BICR (Part 2) per RECIST v1.1 in HER2-positive/HER2-low metastatic breast cancer patients previously treated with T-DXd.
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| Other Endpoint |
Secondary objectives encompass efficacy measures (DOR, PFS, OS, DCR, CBR, TTR) and detailed PK analysis (Cmax, Tmax, AUC, t1/2, CL, Vss, Ctrough) of BB-1701 components in both parts (35 months), with Part 2 featuring BICR-confirmed assessments and additional safety monitoring identical to Part 1.
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| Experiment 4 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
50.00
70.60 % |
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| Patients Enrolled |
Patients with advanced/metastatic HER2-positive solid tumors, who had progressed on, or were intolerant to prior standard therapies, with ECOG PS 2, and measurable disease,.
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| Administration Dosage |
6 dose levels from 0.40 to 2.60 mg/kg Q3W.
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| Related Clinical Trial | |||||
| NCT Number | NCT04257110 | Phase Status | Phase 1 | ||
| Clinical Description |
A first-in-human, open label, multiple dose, dose escalation and cohort expansion phase 1 study to investigate the safety, tolerability, pharmacokinetics and antitumor activities of bb-1701 in subjects with locally advanced/metastatic HER2 expressing solid tumors.
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ILB-3101 [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [7] | ||||
| Patients Enrolled |
Key inclusion: aged 18-80; ECOG 0-1; life expectancy >12 weeks; histologically confirmed advanced/metastatic solid tumors refractory to standard therapy; measurable lesion (s); adequate organ function; negative pregnancy test; effective contraception.
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| Administration Dosage |
There are eight escalating dose cohorts. Intravenous (IV) administration of ILB-3101 Q3W; Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and confirmed disease progression.
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| Related Clinical Trial | |||||
| NCT Number | NCT06426680 | Phase Status | PHASE1 | ||
| Clinical Description |
Phase I/II Study of the ILB-3101 in Patients with Advanced Solid Tumors
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| Primary Endpoint |
Primary endpoints include DLT assessment (Day 21), MTD determination (Day 21) for ILB-3101 in advanced solid tumors.
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| Other Endpoint |
Secondary endpoints comprise ORR (RECIST 1.1, 24 months), AE incidence (CTCAE v5.0, 90 days post-treatment), ADA development (90 days post-treatment), PK parameters (Cmax/Tmax/T1/2/AUC0-t, Cycle 1), and efficacy measures (DOR/DCR/PFS per RECIST 1.1, 24 months).
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BB-1705 [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [8] | ||||
| Patients Enrolled |
Eligible patients are adults (≥18 years) with histologically confirmed advanced/metastatic solid tumors (RECIST 1.1 measurable lesions), ECOG 0-1, and adequate organ function. Key exclusions include recent anticancer therapy, uncontrolled CNS metastases, ≥Grade 2 peripheral neuropathy, active pneumonitis/ILD, or significant comorbidities (e.g., QTc prolongation). Contraception is required during treatment and for 6 months post-dose.
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| Administration Dosage |
BB-1705 will be administered as an intravenous infusion by Q3W for 8cycles
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| Related Clinical Trial | |||||
| NCT Number | NCT05217693 | Phase Status | PHASE1 | ||
| Clinical Description |
A Phase I First-in-human, Open Label, Multicenter, Dose Escalation and Cohort Expansion Study to Investigate the Safety, Tolerability, Pharmacokinetics and Preliminary Antitumor Activity of BB-1705 in Patients With Locally Advanced/Metastatic Solid Tumors
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| Primary Endpoint |
The study evaluates safety by monitoring adverse events (AEs) and serious adverse events (SAEs) for up to 2 years, with dose-limiting toxicities (DLTs) assessed during Cycle 1 (21 days) to determine the maximum tolerated dose (MTD) based on NCI-CTCAE criteria.
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| Other Endpoint |
Pharmacokinetic analysis includes AUC0-inf and Cmax measurements during Cycles 1-8 (21-day cycles), while immunogenicity is assessed via anti-drug antibodies (ADAs). Efficacy endpoints include objective response rate (ORR), progression-free survival (PFS), and duration of response (DOR) evaluated every 6-9 weeks for up to 2 years.
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| Experiment 2 Reporting the Activity Date of This ADC | [13] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05217693 | Phase Status | Phase 1/2 | ||
| Clinical Description |
A phase 1/2 first-in-human, open label, multicenter, dose escalation and cohort expansion study to investigate the safety, tolerability, pharmacokinetics and preliminary antitumor activity of BB-1705 in patients with locally advanced/metastatic solid tumors.
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Farletuzumab ecteribulin [Phase 2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [9] | ||||
| Patients Enrolled |
Eligibility requires histologically confirmed metastatic NSCLC adenocarcinoma (IASLC 8th ed.), measurable disease (RECIST 1.1), and ECOG PS 0-1. Exclusions include non-adenocarcinoma NSCLC histologies, uncontrolled third-space fluid accumulation, prior pneumonectomy (<12 months), recent chest radiotherapy (<6 months), and protocol-specified criteria affecting safety or study integrity.
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| Administration Dosage |
Specified dose on specified days
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| Related Clinical Trial | |||||
| NCT Number | NCT05577715 | Phase Status | PHASE2 | ||
| Clinical Description |
A Phase 2, Open-label, Randomized Study of MORAb-202 (Farletuzumab Ecteribulin), a Folate Receptor Alpha-targeting Antibody-Drug Conjugate, in Participants With Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC) After Progression on Prior Therapies
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| Primary Endpoint |
Primary endpoints assess treatment-related adverse events (TRAEs) leading to discontinuation and objective response rate (ORR) by RECIST 1.1, both evaluated over a 2-year timeframe through investigator assessment to determine safety and efficacy profiles.
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| Other Endpoint |
Safety monitoring tracks adverse events (AEs), serious AEs (SAEs), treatment-related AEs/SAEs, AEs of special interest (AESIs), deaths, and lab abnormalities over 2 years. Key efficacy measures include progression-free survival (PFS), disease control rate (DCR), and duration of response (DoR), all assessed via RECIST 1.1 by investigators during the same 2-year period.
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| Experiment 2 Reporting the Activity Date of This ADC | [10] | ||||
| Patients Enrolled |
Eligible participants must have confirmed high-grade serous ovarian/peritoneal/fallopian tube cancer with platinum-resistant disease (1-3 prior lines) and measurable progression per RECIST v1.1. Key exclusions include non-HGS histologies, platinum-refractory status, significant pulmonary/ILD issues, uncontrolled effusions, hypersensitivity to study drugs, and protocol-specified lab/clinical abnormalities that may compromise safety or interpretation.
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| Administration Dosage |
Specified dose on specified days
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| Related Clinical Trial | |||||
| NCT Number | NCT05613088 | Phase Status | PHASE2 | ||
| Clinical Description |
A Phase 2 Open-label Randomized Study of Farletuzumab Ecteribulin (MORAb-202), a Folate Receptor Alpha-targeting Antibody-drug Conjugate, Versus Investigator's Choice Chemotherapy in Women With Platinum-resistant High-grade Serous (HGS) Ovarian, Primary Peritoneal, or Fallopian Tube Cancer
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| Primary Endpoint |
The primary endpoints evaluate efficacy and tolerability, measuring objective response rate (ORR) by RECIST v1.1 and treatment-related adverse events (TRAEs) causing study discontinuation, both assessed over a 2-year period to determine the treatment's clinical benefit and safety profile.
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| Other Endpoint |
Secondary outcomes include comprehensive safety monitoring of adverse events (AEs), serious AEs (SAEs), AE-related discontinuations, and laboratory abnormalities, along with efficacy assessments of disease control rate (DCR), duration of response (DoR), and progression-free survival (PFS) by RECIST v1.1 - all tracked for 2 years to characterize the treatment's overall risk-benefit profile.
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| Experiment 3 Reporting the Activity Date of This ADC | [11] | ||||
| Patients Enrolled |
Eligible participants (≥20 years, ECOG 0-1) require FRA-positive solid tumors (Part 1) or specific ovarian/NSCLC histologies (Part 2) with adequate organ function. Key exclusions: uncontrolled cardiovascular disease, active infections, ILD, brain metastases, prior FRalpha/eribulin intolerance, or concurrent malignancies. Reproductive-age participants must use contraception, and prior anticancer therapies require appropriate washout periods (2-4 weeks depending on treatment type).
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| Administration Dosage |
Part 1: farletuzumab ecteribulin intravenous (IV) infusion administered every 3 weeks starting at a 0.3 mg/kg dose and successively increasing doses until DLT. Part 2: farletuzumab ecteribulin administered IV every 3 weeks at a dose determined in Part 1 until any of the criteria for discontinuation are met.
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| Related Clinical Trial | |||||
| NCT Number | NCT03386942 | Phase Status | PHASE1 | ||
| Clinical Description |
A Phase 1 Study of MORAb-202 in Subjects With Solid Tumors
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| Primary Endpoint |
The study evaluates safety through dose-limiting toxicities (DLTs) in Cycle 1 (21 days), including severe hematologic events (grade 4 neutropenia/thrombocytopenia/anemia) and clinically significant grade 3-4 non-hematologic toxicities. Additional safety assessments over 50 months monitor AEs, SAEs, lab abnormalities, vital signs, ECOG PS changes, and immunogenicity via ADA titers to characterize the treatment's long-term safety profile.
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| Other Endpoint |
Pharmacokinetics analysis measures maximum serum concentration (Cmax) of farletuzumab ecteribulin, total antibody, and free eribulin to establish the maximum tolerated dose (MTD) and recommended dose (RD) based on DLT rates (target 25%). Efficacy outcomes over 50 months include RECIST v1.1-based responses (ORR, DCR, CBR, BOR), with Part 2 specifically tracking survival metrics (PFS, OS) and duration of response (DOR) in defined cohorts.
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| Experiment 4 Reporting the Activity Date of This ADC | [12] | ||||
| Patients Enrolled |
Eligible participants (≥18 years, ECOG 0-1) include platinum-resistant ovarian, TNBC, NSCLC adenocarcinoma, or endometrial cancer patients with measurable disease and adequate organ function. Key exclusions: prior FRalpha/eribulin therapy, uncontrolled cardiovascular/autoimmune conditions, active infections (HIV/hepatitis), untreated brain metastases, pregnancy, or ILD risk factors (e.g., abnormal PFTs, chest radiotherapy <2 years). Contraception is mandated for reproductive-age participants, with washout periods (2-4 weeks) required for prior therapies.
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| Administration Dosage |
The initial cohort has enrolled 7 patients at a MORAb-202 25 mg/m2 IV Q3W dose and is ongoing; further enrollment of patients at 25 mg/m2 and 33 mg/m2 will occur following ILD safety evaluation. Tumor assessments will be conducted by investigators using RECIST v1.1 at screening, every 6 weeks for 24 weeks, then every 12 weeks or as needed.
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| Related Clinical Trial | |||||
| NCT Number | NCT04300556 | Phase Status | PHASE1|||PHASE2 | ||
| Clinical Description |
A Multicenter, Open-Label Phase 1/2 Trial Evaluating the Safety, Tolerability, and Efficacy of MORAb-202, a Folate Receptor Alpha (FRalpha)-Targeting Antibody-drug Conjugate (ADC) in Subjects With Selected Tumor Types
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| Primary Endpoint |
The study assesses safety through dose-limiting toxicities (DLTs) in Cycle 1 (21 days), including severe hematologic and non-hematologic events (grade 3-4 per NCI CTCAE v5.0). Long-term safety (up to ~4 years 8 months) monitors SAEs, AEs leading to discontinuation, AEIs (e.g., ILD), lab/vital sign abnormalities, and immunogenicity via ADA titers. Efficacy endpoints include ORR (RECIST v1.1, up to ~24 weeks) and dose-finding for the RP2D.
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| Other Endpoint |
Secondary outcomes evaluate pharmacokinetics (Cmax, AUC, t½) of farletuzumab ecteribulin and its components, alongside RECIST v1.1-based efficacy measures (DOR, DCR, CBR, PFS, OS) over ~4.8 years. Exploratory analyses correlate tumor FRA expression with clinical outcomes (ORR, PFS). Additional metrics include ECOG PS changes, SpO2 levels, and cardiac/laboratory parameters to comprehensively assess treatment impact.
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Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 2.10% | Moderate FOLR1 expression (FOLR1++) | ||
| Method Description |
The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 2.5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
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| In Vivo Model | Breast cancer PDX model (PDX: OD-BRE-0631) | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 65.70% | Moderate FOLR1 expression (FOLR1++) | ||
| Method Description |
The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
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| In Vivo Model | Breast cancer PDX model (PDX: OD-BRE-0631) | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.30% | High FOLR1 expression (FOLR1+++) | ||
| Method Description |
The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
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| In Vivo Model | Breast cancer PDX model (PDX: IM-BRE-563) | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.01 pM
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High FOLR1 expression (FOLR1+++) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.74 pM
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High FOLR1 expression (FOLR1+++) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1 pM | Negative FOLR1 expression (FOLR1-) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
23 pM
|
Moderate FOLR1 expression (FOLR1++) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Skin squamous cell carcinoma | A431-A3 cells | CVCL_0037 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.02 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.42 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.43 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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||||
| In Vitro Model | Ovarian serous adenocarcinoma | Caov-3 cells | CVCL_0201 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.75 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.03 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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||||
| In Vitro Model | Endometrial adenocarcinoma | HEC-59 cells | CVCL_2930 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.42 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.76 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | MKN74 cells | CVCL_2791 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.81 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Endometrial adenocarcinoma | HEC-1-A cells | CVCL_0293 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.17 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | MKN7 cells | CVCL_1417 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.42 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13.15 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Endometrial carcinoma | HEC-251 cells | CVCL_2927 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
24.58 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Gastric carcinoma | NUGC-3 cells | CVCL_1612 | ||
| Experiment 17 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
FOLR1-Suc/SPAAC-PEG4-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.3 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
FOLR1-Mal-PEG2-Ala-Ala-Asn-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.8 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
32 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
FOLR1-Mal-PEG2-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.1 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.7 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
FOLR1-Mal-Caproyl-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.9 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
FOLR1-Mal-PEG8-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.1 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
86 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
FOLR1-Mal-PEG4-tria-PEG3-Dis-dim-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.27 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.85 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
FOLR1-Mal-PEG4-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.28 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
22 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
FOLR1-Mal-PEG2-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.33 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
38 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
FOLR1-Mal-PEG4-tria-PEG3-Sulfo-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.37 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.69 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.8 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
FOLR1-Suc/SPAAC-PEG3-Dis-dim-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.55 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.9 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.7 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
MSLN-Mal-PEG4-tria-PEG3-Sulfo-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.99 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.4 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
MSLN-Suc/SPAAC-PEG3-Dis-dim-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
10 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
11 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
MSLN-Mal-PEG4-tria-PEG3-Dis-dim-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.2 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.4 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.1 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
FOLR1-Suc/SPAAC-PEG4-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.3 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
46 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
FOLR1-Suc/SPAAC-PEG3-Sulfonamide-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.7 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.8 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
25 nM
|
Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
MSLN-Suc/SPAAC-PEG3-Sulfonamide-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
19 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
28 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
FOLR1-Suc/SPAAC-PEG2-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.3 nM
|
High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
38 nM
|
Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Mal-Caproyl-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.8 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
14 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Mal-PEG2-Ala-Ala-Asn-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.1 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.9 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
34 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
MSLN-Mal-PEG2-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.5 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Suc/SPAAC-PEG4-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
13 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
31 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Mal-PEG8-Val-Cit-PABC-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
26 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
34 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Mal-PEG4-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
32 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
76 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Suc/SPAAC-PEG4-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
39 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
61 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Mal-PEG2-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
43 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
50 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
MSLN-Suc/SPAAC-PEG2-Eribulin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
76 nM
|
Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
86 nM
|
Moderate MSLN expression(MSLN++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [15] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative MSLN expression(MSLN-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
|
||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
AU2023279443A1 Example A14 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | > 50% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.
Click to Show/Hide
|
||||
| In Vivo Model | NCI-N87 female BALB/c-nu/nu mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
AU2023279443A1 Example A16 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | > 50% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.
Click to Show/Hide
|
||||
| In Vivo Model | NCI-N87 female BALB/c-nu/nu mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
AU2023279443A1 Example A17 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | > 50% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.
Click to Show/Hide
|
||||
| In Vivo Model | NCI-N87 female BALB/c-nu/nu mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
AU2023279443A1 Example A18 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | > 103% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.
Click to Show/Hide
|
||||
| In Vivo Model | NCI-N87 female BALB/c-nu/nu mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
MORAb-003 ADC5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [17] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | High FRA expression (FRA +++) | ||
| Method Description |
Use crystal violet analysis to evaluate the in vitro efficacy of the prepared ADCs. Initially screen all MORAb003 ADCs on IGROV1 (FRi (+++)) and SJSA - 1 (FReg (-)) cells.
|
||||
| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
AU2023279443A1 Example A21 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
AU2023279443A1 Example A22 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [16] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References
