Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0RLOBQ
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| ADC Name |
GsADC 3b
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| Synonyms |
gsADC 3b
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| Organization |
School of Pharmaceutical Science and Technology, Hangzhou Institute of Advanced Study, Hangzhou 310024, China; State Key Laboratory of Drug Research, Center for Biotherapeutics Discovery Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, No.555 Zuchongzhi Rd, Pudong, Shanghai 201203, China; University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing 100049, China; Shanghai Biomedical Co., Ltd. Zhangjiang, Pudong, Shanghai 201203, China.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
2
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| Structure |
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| Antibody Name |
SAC 1
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Antibody Info | ||||
| Antigen Name |
Tumor-associated calcium signal transducer 2 (TACSTD2)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Undisclosed
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| Conjugate Type |
Divinylsulfonamide-mediated disulfide re-bridging.
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General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.011 nM | High TROP2 expression (TROP2 +++) | ||
| Method Description |
The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % FBS-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37 °C in a 5 % CO2 cell incubator. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.
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| In Vitro Model | Lung papillary adenocarcinoma | NCI-H441 cells | CVCL_1561 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.056 nM | High TROP2 expression (TROP2 +++) | ||
| Method Description |
The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % FBS-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37 °C in a 5 % CO2 cell incubator. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.073 nM | High TROP2 expression (TROP2 +++) | ||
| Method Description |
The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % FBS-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37 °C in a 5 % CO2 cell incubator. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.233 nM | High TROP2 expression (TROP2 +++) | ||
| Method Description |
The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % FBS-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37 °C in a 5 % CO2 cell incubator. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.
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| In Vitro Model | Hypopharyngeal squamous cell carcinoma | FaDu cells | CVCL_1218 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 2.592 nM | High TROP2 expression (TROP2 +++) | ||
| Method Description |
The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % FBS-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37 °C in a 5 % CO2 cell incubator. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.
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| In Vitro Model | Breast acantholytic squamous cell carcinoma | HCC-1806 cells | CVCL_1258 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 100 nM | Negative TROP2 expression (TROP2-) | ||
| Method Description |
The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % FBS-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37 °C in a 5 % CO2 cell incubator. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.
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| In Vitro Model | Lung adenocarcinoma | Calu-6 cells | CVCL_0236 | ||
References