Payload Information
General Information of This Payload
| Payload ID | PAY0XXLAE |
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| Name | Monomethyl auristatin E+Monomethyl auristatin F |
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| Synonyms |
Monomethyl auristatin E+Monomethyl auristatin F
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| Target(s) | Microtubule (MT) | |||||
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
ADC MMAE/F 4+2 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.50% (Day 24) | Low HER2 expression (HER2+) | ||
| Method Description |
HCC1954-TDR breast tumor model shows very low HER2 expression with intratumor heterogeneity,representing refractory breast tumors. The HCC1954-TDR cell line was established by continuous treatment with T-DM1 for 8 months. Once tumors reached an average volume of 125mm3,mice were administered with a single dose of the MMAE/F 4+2 ADC (1 mg/kg).
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast cancer | Breast cancer cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.10% (Day 24) | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
The in vivo validated model was a xenograft model of human breast tumor consisting of HER2-positive JIMT-1 cells and HER2-negative MDA-MB-231 cells (4:1 ratio) transferred into immunodeficient mice. This admixed tumor grew aggressively and reached a palpable size (100-150 mm 3 ) in most mice 7 days after orthotopic transplantation. Tumor-bearing mice were treated with each ADC at 3 mg/kg.
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells/MDA-MB-231 cells | CVCL_2077/CVCL_0062 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.02 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.02 nM
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Low HER2 expression (HER2+) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.18 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
ADC MMAE/F 2+4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 87.60% (Day 24) | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
The in vivo validated model was a xenograft model of human breast tumor consisting of HER2-positive JIMT-1 cells and HER2-negative MDA-MB-231 cells (4:1 ratio) transferred into immunodeficient mice. This admixed tumor grew aggressively and reached a palpable size (100-150 mm 3 ) in most mice 7 days after orthotopic transplantation. Tumor-bearing mice were treated with each ADC at 3 mg/kg.
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells/MDA-MB-231 cells | CVCL_2077/CVCL_0062 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.02 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.03 nM
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Low HER2 expression (HER2+) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.23 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
ADC MMAE/F 2+2 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.03 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.05 nM
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Low HER2 expression (HER2+) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.34 nM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
ADCs were evaluated in vitro cytotoxicity in HER2-positive (KPL-4,JIMT-1,and SKBR-3) and -negative (MDA-MB-231) breast cancer cell lines,human embryonic kidney 293 (HEK293) cells,and human hepatocyte carcinoma (HepG2) cells. All cells were cultured at 37°C under 5% CO2 and passaged before becoming fully confluent up to 20 passages.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
References
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