Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0WWBCV
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| ADC Name |
Anti-KIT 20376?SMCC-DM1
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| Synonyms |
Anti-KIT-20376?SMCC-DM1
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| Organization |
Novartis AG
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| Drug Status |
Investigative
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| Indication |
In total 3 Indication(s)
Acute myeloid leukaemia [ICD11:2A60]
Investigative
Melanoma [ICD11:2C30]
Investigative
Small cell lung cancer [ICD11:2C25]
Investigative
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| Drug-to-Antibody Ratio |
3.8
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| Antibody Name |
Anti-KIT mAb 20376
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Antibody Info | ||||
| Antigen Name |
Mast/stem cell growth factor receptor Kit (KIT)
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Antigen Info | ||||
| Payload Name |
Mertansine DM1
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
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Linker Info | ||||
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 43.00% (Day 23) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).
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| In Vivo Model | NCI-H1048 CDX model | ||||
| In Vitro Model | Lung small cell carcinoma | NCI-H1048 cells | CVCL_1453 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 49.00% (Day 40) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).
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| In Vivo Model | GIST-T1 CDX model | ||||
| In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 91.00% (Day 40) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).
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| In Vivo Model | GIST-T1 CDX model | ||||
| In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.00% (Day 40) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).
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| In Vivo Model | GIST-T1 CDX model | ||||
| In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.00% (Day 40) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).
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| In Vivo Model | GIST-T1 CDX model | ||||
| In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 54.00% | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Gastrointestinal stromal tumor | GIST430 cells | CVCL_7040 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 69.00% | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 69.00% | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Gastrointestinal stromal tumor | GIST882 cells | CVCL_7044 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 79.00% | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Acute myeloid leukemia | Kasumi-6 cells | CVCL_0614 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 95.00% | Negative KIT expression (KIT-) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 97.00% | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Lung small cell carcinoma | NCI-H1048 cells | CVCL_1453 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 99.00% | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 100.00% | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Myeloid leukemia with maturation | Kasumi-1 cells | CVCL_0589 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.04 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Gastrointestinal stromal tumor | GIST430 cells | CVCL_7040 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.05 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Gastrointestinal stromal tumor | GIST-T1 cells | CVCL_4976 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.07 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.00 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Gastrointestinal stromal tumor | GIST882 cells | CVCL_7044 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.33 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Myeloid leukemia with maturation | Kasumi-1 cells | CVCL_0589 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.34 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Lung small cell carcinoma | NCI-H1048 cells | CVCL_1453 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.51 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Acute myeloid leukemia | Kasumi-6 cells | CVCL_0614 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.69 nM | Negative KIT expression (KIT-) | ||
| Method Description |
Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
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