Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ID: DRG0CRYVT)
| ADC Name |
Trastuzumab envedotin
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| Synonyms |
trastuzumab envedotin; DP303c; SYA1501; SYSA1501
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| Organization |
CSPC Pharmaceutical Group (Originator)
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| Drug Status |
Phase 3
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| Drug-to-Antibody Ratio |
2
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| Structure |
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| Antibody Name |
Trastuzumab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (HER2)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Payload Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
NH2-PEG3-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Enzymatic Catalysis
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| Combination Type |
envedotin
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2027 Update
The disease landscape of This ADC
2027 Update
The clinical trial pipelines of This ADC
| Indication | Phase 1 | Phase 2 | Phase 3 | Approved | |||||
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| Unspecific solid tumor |
2 Trials
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| Gastric cancer |
1 Trials
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| Peritoneal cancer |
1 Trials
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| Breast cancer |
1 Trials
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2 Trials
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| Ovarian cancer |
1 Trials
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| Fallopian tube cancer |
1 Trials
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2027 Update
General Information of The ADMET Data Related to This ADC
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) | 23.6 | ng/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 1.0 mg/kg, n=3.
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[1] |
| Maximum Observed Concentration (Cmax) | 46.7 | ng/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 2.0 mg/kg, n=6.
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[1] |
| Maximum Observed Concentration (Cmax) | 78.7 | ng/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 3.0 mg/kg, n=6.
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[1] |
| Maximum Observed Concentration (Cmax) | 110 | ng/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 4.0 mg/kg, n=6.
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[1] |
| Maximum Observed Concentration (Cmax) | 73 | ng/mL |
Pharmacokinetic parameters for DP303c, Dose expansion 3.0 mg/kg, n=72.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 1330 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 1.0 mg/kg, n=3, AUC0-t.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 4130 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 2.0 mg/kg, n=6, AUC0-t.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 6550 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 3.0 mg/kg, n=6, AUC0-t.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 11300 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 4.0 mg/kg, n=6, AUC0-t.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 5940 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose expansion 3.0 mg/kg, n=72, AUC0-t.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 1430 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 1.0 mg/kg, n=3, AUC0-inf.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 4240 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 2.0 mg/kg, n=6, AUC0-inf.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 6800 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 3.0 mg/kg, n=6, AUC0-inf.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 11900 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose escalation 4.0 mg/kg, n=6, AUC0-inf.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 6350 | ng·h/mL |
Pharmacokinetic parameters for DP303c, Dose expansion 3.0 mg/kg, n=72, AUC0-inf.
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[1] |
| Time to Maximum Concentration (Tmax) | 1.98 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 1.0 mg/kg, n=3.
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[1] |
| Time to Maximum Concentration (Tmax) | 2.08 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 2.0 mg/kg, n=6.
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[1] |
| Time to Maximum Concentration (Tmax) | 2.03 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 3.0 mg/kg, n=6.
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[1] |
| Time to Maximum Concentration (Tmax) | 1.9 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 4.0 mg/kg, n=6.
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[1] |
| Time to Maximum Concentration (Tmax) | 1.97 | h |
Pharmacokinetic parameters for DP303c, Dose expansion 3.0 mg/kg, n=72.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
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| Volume of Distribution (Vd) | 2.54 | L |
Pharmacokinetic parameters for DP303c, Dose escalation 1.0 mg/kg, n=3.
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[1] |
| Volume of Distribution (Vd) | 3.29 | L |
Pharmacokinetic parameters for DP303c, Dose escalation 2.0 mg/kg, n=6.
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[1] |
| Volume of Distribution (Vd) | 2.62 | L |
Pharmacokinetic parameters for DP303c, Dose escalation 3.0 mg/kg, n=6.
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[1] |
| Volume of Distribution (Vd) | 2.86 | L |
Pharmacokinetic parameters for DP303c, Dose escalation 4.0 mg/kg, n=6.
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| Volume of Distribution (Vd) | 3.17 | L |
Pharmacokinetic parameters for DP303c, Dose expansion 3.0 mg/kg, n=72.
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
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| Elimination Half-Life (t1/2) | 1.8 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 1.0 mg/kg, n=3.
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[1] |
| Elimination Half-Life (t1/2) | 2.71 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 2.0 mg/kg, n=6.
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[1] |
| Elimination Half-Life (t1/2) | 2.69 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 3.0 mg/kg, n=6.
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[1] |
| Elimination Half-Life (t1/2) | 3.69 | h |
Pharmacokinetic parameters for DP303c, Dose escalation 4.0 mg/kg, n=6.
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[1] |
| Elimination Half-Life (t1/2) | 2.98 | h |
Pharmacokinetic parameters for DP303c, Dose expansion 3.0 mg/kg, n=72.
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[1] |
| Clearance (CL) | 0.0408 | L/h |
Pharmacokinetic parameters for DP303c, Dose escalation 1.0 mg/kg, n=3.
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[1] |
| Clearance (CL) | 0.0361 | L/h |
Pharmacokinetic parameters for DP303c, Dose escalation 2.0 mg/kg, n=6.
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[1] |
| Clearance (CL) | 0.0345 | L/h |
Pharmacokinetic parameters for DP303c, Dose escalation 3.0 mg/kg, n=6.
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[1] |
| Clearance (CL) | 0.0224 | L/h |
Pharmacokinetic parameters for DP303c, Dose escalation 4.0 mg/kg, n=6.
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[1] |
| Clearance (CL) | 0.0321 | L/h |
Pharmacokinetic parameters for DP303c, Dose expansion 3.0 mg/kg, n=72.
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[1] |
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor-associated calcium signal transducer 2 (TACSTD2) | . . . | |||
| Patients Enrolled |
Eligibility requires age ≥18 with ECOG 0-1, HER2+ advanced solid tumors, prior anti-HER2 therapy, and adequate organ function. Key exclusions: LVEF<40%, grade ≥3 neuropathy, active hepatitis/HIV, recent CYP3A modulators (14 days), anthracycline overexposure, or uncontrolled CNS metastases. Contraception mandated for 6 months post-treatment.
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| Administration Dosage |
DP303c injection, 3.0 mg/kg, every 3 weeks.
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| Related Clinical Trial | |||||
| NCT Number | NCT05810103 | Clinical Status | PHASE1 | ||
| Clinical Description | A Multi-center, Single-arm, Phase I Study of DP303c in Patients With HER2-positive Advanced Solid Tumors | ||||
| Primary Endpoint |
Primary pharmacokinetic endpoints include Cmax, AUC0-last, AUC0-inf, and Tmax of the investigational drug measured during multiple dosing cycles (21-day cycles) in patients with HER2-positive advanced solid tumors.
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| Other Endpoint |
Secondary endpoints assess safety (AE incidence over 12 months), efficacy (ORR, DCR, DoR over 12 months), and immunogenicity (ADA/Nab incidence measured during treatment cycles) in this phase I clinical trial.
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| Experiment 2 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Progression Free Survival |
4.44 months
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| Patients Enrolled |
Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, ≥Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure ≥360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.
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| Administration Dosage |
.
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| Related Clinical Trial | |||||
| NCT Number | NCT04146610 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors | ||||
| Primary Endpoint |
Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
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| Other Endpoint |
Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
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| Experiment 3 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
42.90%
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| Patients Enrolled |
Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, ≥Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure ≥360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.
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| Administration Dosage |
.
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| Related Clinical Trial | |||||
| NCT Number | NCT04146610 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors | ||||
| Primary Endpoint |
Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
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| Other Endpoint |
Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
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| Experiment 4 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Disease control rate (DCR) |
68.10%
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| Patients Enrolled |
Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, ≥Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure ≥360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.
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| Administration Dosage |
.
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| Related Clinical Trial | |||||
| NCT Number | NCT04146610 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors | ||||
| Primary Endpoint |
Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
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| Other Endpoint |
Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
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| Experiment 5 Reporting the Activity Date of This ADC | [4] | ||||
| Patients Enrolled |
Inclusion: HER2+ breast cancer patients (IHC 3+ or IHC 2+/ISH+) aged 18-75 with ≥2 prior anti-HER2 lines (including trastuzumab), measurable disease, ECOG 0-1, LVEF≥50%, and adequate organ function. Exclusion: Prior DP303c treatment, active CNS metastases, LVEF<40% history, uncontrolled comorbidities, recent anticancer therapies (4w chemo/2w endocrine), active infections (HBV/HCV), or CYP3A modulator use within 14 days. Contraception required for 6 months post-treatment.
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| Administration Dosage |
DP303c injection, 3.0 mg/kg, every 3 weeks.
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| Related Clinical Trial | |||||
| NCT Number | NCT05334810 | Clinical Status | PHASE2 | ||
| Clinical Description | A Multi-center, Open-lable, Single-arm Phase II Study to Evaluate the Efficacy and Safety of DP303c in Patients With HER2-positive Unresectable Locally Advanced, Relapsed, or Metastatic Breast Cancer | ||||
| Primary Endpoint |
Primary endpoint is ORR assessed by IRC per RECIST v1.1 with tumor evaluations every 6 weeks from baseline.
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| Other Endpoint |
Secondary endpoints include DOR and PFS measured at 6-week intervals from baseline until progression.
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| Experiment 6 Reporting the Activity Date of This ADC | [5] | ||||
| Patients Enrolled |
Inclusion: HER2+ breast cancer patients (IHC 3+/ISH+) aged ≥18 with ≥2 prior systemic therapies, measurable disease, ECOG 0-1, adequate organ function. Exclusion: Pregnancy, recent anticancer treatments (28d systemic/14d TCM therapy), active CNS metastases, LVEF<40%, severe comorbidities (cardiopulmonary/neuropathic/ocular), active infections (HBV/HCV/HIV), or CYP3A modulator use. Contraception required during study participation.
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| Administration Dosage |
Eligible patients will be treated with trastuzumab IV on day 1 and oral capecitabine twice daily on days 1-14 every 3 weeks, or patients will be treated with trastuzumab IV on day 1 and vinorelbine IV over on days 1 and 8 every 3 weeks.
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| Related Clinical Trial | |||||
| NCT Number | NCT05901935 | Clinical Status | PHASE3 | ||
| Clinical Description | A Multicentre, Randomized, Open-label, Controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of DP303cversus Trastuzumab Combined With Vinorelbine/Capecitabine in of HER2-positive Advanced Breast Cancer | ||||
| Primary Endpoint |
Primary endpoint is PFS assessed by BIRC per RECIST v1.1 with follow-up up to 5 years.
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| Other Endpoint |
Secondary endpoints include investigator-assessed PFS, OS, ORR, DoR (all evaluated per RECIST v1.1 over 5 years), and AE incidence/severity monitoring throughout the study period.
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| Experiment 7 Reporting the Activity Date of This ADC | [6] | ||||
| Patients Enrolled |
Inclusion: HER2+ (IHC3+/ISH+) breast cancer patients ≥18 years with prior trastuzumab/taxane treatment, ECOG 0-2, adequate organ function. Exclusion: Prior HER2-ADC therapy, active CNS metastases, uncontrolled effusions, Grade≥2 neuropathy, recent anticancer therapies (4w immunotherapy/2w chemotherapy), ocular/cardiopulmonary comorbidities, or active infections requiring IV treatment.
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| Administration Dosage |
DP303c injection, 3.0 mg/kg, Q3W.
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| Related Clinical Trial | |||||
| NCT Number | NCT06313086 | Clinical Status | PHASE3 | ||
| Clinical Description | A Multicentre, Randomized, Open-label, Controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of DP303c Versus Trastuzumab Emtansine in Patients With HER2-positive Advanced Breast Cancer | ||||
| Primary Endpoint |
Primary endpoint is BIRC-assessed PFS per RECIST v1.1 with 4-year follow-up in HER2+ advanced/metastatic breast cancer patients.
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| Other Endpoint |
Secondary endpoints include investigator-assessed PFS, OS, ORR, DoR (all per RECIST v1.1) and AE monitoring over 4 years, evaluating both efficacy and safety outcomes.
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| Experiment 8 Reporting the Activity Date of This ADC | [7] | ||||
| Patients Enrolled |
Eligibility requires age 18-75 with progressed gastric cancer after 1-2 prior therapies (including platinum/fluorouracil), measurable lesions, and organ function adequacy. Key exclusions: trastuzumab intolerance, uncontrolled effusions, active CNS metastases, ≥Grade 2 neuropathy, recent CYP3A4/UGT1A1 modulator use, or significant ocular/cardiovascular comorbidities.
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| Administration Dosage |
DP303c injection, dose level 1, intravenous drip, Q3W + simmitinib tablets, dose level 1, oral, QD, taken for 3 weeks, discontinued for 1 week, Q4W
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| Related Clinical Trial | |||||
| NCT Number | NCT06577376 | Clinical Status | PHASE1|||PHASE2 | ||
| Clinical Description | A Multicenter, Open-label Phase I/II Clinical Study to Evaluate the Safety and Efficacy of Simmitinib or Irinotecan Liposomes Combined With DP303c Injection in the Treatment of HER2 Expressing Gastric Adenocarcinoma or Gastroesophageal Junction Adenocarcinoma | ||||
| Primary Endpoint |
Primary endpoints include DLT occurrence/incidence, AE/SAE monitoring, and ORR per RECIST 1.1 assessed over 36 months in HER2-positive (IHC 1+/2+/3+) gastric/GEJ adenocarcinoma patients.
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| Other Endpoint |
Secondary outcomes comprise efficacy measures (DCR, DoR, PFS, OS) and pharmacokinetic evaluations (DP303c/simmitinib concentrations, ADA incidence, HER2 expression) tracked for 36 months.
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| Experiment 9 Reporting the Activity Date of This ADC | [8] | ||||
| Patients Enrolled |
Inclusion: Age 18-75 with histologically confirmed advanced gastric cancer, ECOG 0-1, adequate organ function, measurable lesions (RECIST v1.1), and progression after platinum/taxane-based therapy (HER2-positive cohorts require prior trastuzumab). Exclusion: Active CNS metastases, uncontrolled effusions, ≥Grade 2 neuropathy, cardiac dysfunction (LVEF<50%), recent CYP3A4 modulators, or prior HER2-ADC therapy. Contraception required for 6 months post-treatment.
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| Administration Dosage |
Patients with HER2-positive advanced or metastatic gastric cancer after receiving 1st-line treatment will be treated with DP303c injection at 2.0 mg/kg,2.5 mg/kg or 3.0 mg/kg every 3 weeks to determine the recommended dose.
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| Related Clinical Trial | |||||
| NCT Number | NCT04826107 | Clinical Status | PHASE2 | ||
| Clinical Description | An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With Unresectable Locally Advanced, Recurrent or Metastatic Gastric Cancer With HER2 Expression | ||||
| Primary Endpoint |
Primary endpoint is ORR (CR+PR rate) assessed over 2.5 years in HER2-positive/low-expression gastric/GEJ adenocarcinoma patients with progression after ≥1 prior therapy.
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| Other Endpoint |
Secondary endpoints include PFS, OS, DCR, DoR (all measured over 2.5 years) and AE/SAE monitoring, evaluating both efficacy and safety outcomes in this multicenter trial.
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| Experiment 10 Reporting the Activity Date of This ADC | [9] | ||||
| Patients Enrolled |
Inclusion: Women aged 18-75 with ECOG 0-2, measurable lesions (RECIST v1.1), adequate organ function, and HER2 IHC 1+/2+/3+ status. Exclusion: Active CNS metastases, ≥Grade 2 neuropathy, LVEF<50%, uncontrolled effusions, recent CYP3A4 modulators (28 days), prior HER2-ADC therapy, or anthracycline exposure >500mg/m2 doxorubicin equivalent. Contraception required for 6 months post-treatment.
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| Administration Dosage |
Part1:Patients with HER2-expressing advanced ovarian cancer will be treated with DP303c injection at 2.0 mg/kg or 3.0 mg/kg every 3 weeks (Q3W) to determine the recommended phase 2 dose (RP2D).Part2a:Patients with HER2-overexpressing advanced ovarian cancer will be treated with DP303c injection at RP2D.Part2b:Patients with HER2-lowexpressing advanced ovarian cancer will be treated with DP303c injection at RP2D.
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| Related Clinical Trial | |||||
| NCT Number | NCT04828616 | Clinical Status | PHASE2 | ||
| Clinical Description | An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With HER2-expressing Advanced Ovarian Cancer | ||||
| Primary Endpoint |
Primary endpoint is ORR (CR+PR rate) assessed over 3 years in HER2-positive/low-expressing ovarian/tubal/peritoneal cancer patients with prior platinum therapy.
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| Other Endpoint |
Secondary endpoints include PFS, OS, DoR (3-year follow-up), AE/SAE monitoring (NCI-CTCAE v5.0), PK parameters (Cmax/Tmax/AUC of DP303c), and ADA incidence in this phase I/II study.
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| Experiment 11 Reporting the Activity Date of This ADC | [10] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04826107 | Clinical Status | Phase 2 | ||
| Clinical Description | An open-label, multicentre, phase 2 study of DP303c injection in patients with unresectable locally advanced, recurrent or metastatic gastric cancer with HER2 expression. | ||||
| Experiment 12 Reporting the Activity Date of This ADC | [11] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04828616 | Clinical Status | Phase 2 | ||
| Clinical Description | An open-label, multicentre, phase 2 study of DP303c injection in patients with HER2-expressing advanced ovarian cancer. | ||||
| Experiment 13 Reporting the Activity Date of This ADC | [12] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05334810 | Clinical Status | Phase 2 | ||
| Clinical Description | A multi-center, open-lable, single-arm phase 2 study to evaluate the efficacy and safety of DP303c in patients with HER2-positive unresectable locally advanced, relapsed, or metastatic breast cancer. | ||||
| Experiment 14 Reporting the Activity Date of This ADC | [13] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04146610 | Clinical Status | Phase 1 | ||
| Clinical Description | A phase 1a, multicenter, open and dose-increasing study of DP303c to evaluate the safety , pharmacokinetics, immunogenicity and antitumor activity of subjects with HER2-positive advanced solid tumors. | ||||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 7.60% | Moderate HER2 expression (HER2++) | ||
| Method Description |
DP001 (10 mg/kg).
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| In Vivo Model | JIMT -1 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 16.20% | Moderate HER2 expression (HER2++) | ||
| Method Description |
T-DM1 (10 mg/kg).
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| In Vivo Model | JIMT -1 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 28.47% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP001 (10 mg/kg).
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| In Vivo Model | SK-OV-3 cell line xenograft model | ||||
| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 33.60% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP001 (10 mg/kg).
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| In Vivo Model | NCI-N87 xenograft model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 39% | Moderate HER2 expression (HER2++) | ||
| Method Description |
DP303c (0.3 mg/kg).
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| In Vivo Model | JIMT -1 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 45.26% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (1 mg/kg).
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| In Vivo Model | SK-OV-3 cell line xenograft model | ||||
| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 54.40% | Moderate HER2 expression (HER2++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 0.1 mg/kg.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 82.10% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 83.94% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (3 mg/kg).
|
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| In Vivo Model | SK-OV-3 cell line xenograft model | ||||
| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.48% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP001 (15 mg/kg).
|
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| In Vivo Model | HCC1954 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 91.60% | High HER2 expression (HER2+++/++) | ||
| Method Description |
T-DM1 (10 mg/kg).
|
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| In Vivo Model | NCI-N87 xenograft model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (10 mg/kg).
|
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| In Vivo Model | NCI-N87 xenograft model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (5 mg/kg).
|
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| In Vivo Model | NCI-N87 xenograft model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (2.5 mg/kg).
|
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| In Vivo Model | NCI-N87 xenograft model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.10% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.
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|
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.16% | High HER2 expression (HER2+++/++) | ||
| Method Description |
T-DM1 (10 mg/kg).
|
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| In Vivo Model | SK-OV-3 cell line xenograft model | ||||
| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 17 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.30% | High HER2 expression (HER2+++/++) | ||
| Method Description |
T-DM1 (15 mg/kg).
|
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| In Vivo Model | HCC1954 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 18 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (3 mg/kg).
|
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| In Vivo Model | HCC1954 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 19 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (10 mg/kg).
|
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| In Vivo Model | HCC1954 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 20 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (15 mg/kg).
|
||||
| In Vivo Model | HCC1954 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 21 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.10% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.
Click to Show/Hide
|
||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 22 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.50% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.
Click to Show/Hide
|
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 23 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.50% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 2.5 mg/kg.
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|
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 24 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.80% | Moderate HER2 expression (HER2++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.
Click to Show/Hide
|
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 25 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.80% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.
Click to Show/Hide
|
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 26 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.80% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 5 mg/kg.
Click to Show/Hide
|
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 27 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.50% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.
Click to Show/Hide
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 28 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.54% | High HER2 expression (HER2+++/++) | ||
| Method Description |
DP303c (10 mg/kg).
|
||||
| In Vivo Model | SK-OV-3 cell line xenograft model | ||||
| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 29 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.80% | Moderate HER2 expression (HER2++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.
Click to Show/Hide
|
||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 30 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.10% | High HER2 expression (HER2+++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 15 mg/kg.
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|
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 31 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.90% | Moderate HER2 expression (HER2++) | ||
| Method Description |
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.
Click to Show/Hide
|
||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 32 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Moderate HER2 expression (HER2++) | ||
| Method Description |
DP303c (10 mg/kg).
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| In Vivo Model | JIMT -1 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 33 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Moderate HER2 expression (HER2++) | ||
| Method Description |
DP303c (3 mg/kg).
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| In Vivo Model | JIMT -1 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 34 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Moderate HER2 expression (HER2++) | ||
| Method Description |
DP303c (1 mg/kg).
|
||||
| In Vivo Model | JIMT -1 cell line xenograft model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.07 nM | Moderate HER2 expression (HER2++; HER2 MFI=157,231) | ||
| Method Description |
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.07 nM | High HER2 expression (HER2+++) | ||
| Method Description |
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.08 nM | High HER2 expression (HER2+++; HER2 MFI=987,353) | ||
| Method Description |
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.08 nM | Negative HER2 expression (HER2-; HER2 MFI=256) | ||
| Method Description |
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.15 nM | High HER2 expression (HER2+++) | ||
| Method Description |
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.15 nM | High HER2 expression (HER2+++) | ||
| Method Description |
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.22 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
|
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| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.22 nM | High HER2 expression (HER2+++) | ||
| Method Description |
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
|
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| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.23 nM | High HER2 expression (HER2+++; HER2 MFI=804,573) | ||
| Method Description |
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
|
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.23 nM | High HER2 expression (HER2+++; HER2 MFI=892,333) | ||
| Method Description |
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
|
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 3.39 nM | High HER2 expression (HER2+++) | ||
| Method Description |
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
|
||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 3.39 nM | Moderate HER2 expression (HER2++) | ||
| Method Description |
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
|
||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 50 nM | High HER2 expression (HER2+++; HER2 MFI=1,106,494) | ||
| Method Description |
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [14] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | High HER2 expression (HER2+++; HER2 MFI=765,629) | ||
| Method Description |
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
|
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
References