Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0GCXCC
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| ADC Name |
4C9-DM1
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| Synonyms |
4C9-SMCC-DM1
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Small cell lung cancer [ICD11:2C25]
Investigative
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| Drug-to-Antibody Ratio |
2.16
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| Structure |
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| Antibody Name |
Anti-KIT mAb 4C9
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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 | ||||
| Conjugate Type |
Random conjugation through nucleophilic lysines.
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| Combination Type |
Emtansine
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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) | ≈ 40.00% (Day 14) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 1 mg/kg twice at day 0 and day 7.
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| In Vivo Model | Small cell lung cancer CDX model | ||||
| In Vitro Model | Small cell lung cancer | Small cell lung cancer cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 45.00% (Day 14) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 3 mg/kg twice at day 0 and day 7.
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| In Vivo Model | Small cell lung cancer CDX model | ||||
| In Vitro Model | Small cell lung cancer | Small cell lung cancer cells | Homo sapiens | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 59.00% (Day 14) | Positive KIT expression (KIT+++/++) | ||
| Method Description |
In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 5 mg/kg twice at day 0 and day 7.
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| In Vivo Model | Small cell lung cancer CDX model | ||||
| In Vitro Model | Small cell lung cancer | Small cell lung cancer cells | Homo sapiens | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.16 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
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| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.32 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
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| In Vitro Model | Lung small cell carcinoma | NCI-H889 cells | CVCL_1598 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 4.08 nM | Positive KIT expression (KIT+++/++) | ||
| Method Description |
C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
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| In Vitro Model | Lung small cell carcinoma | NCI-H1048 cells | CVCL_1453 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 16.58 nM | Negative KIT expression (KIT-) | ||
| Method Description |
C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
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| In Vitro Model | Lung small cell carcinoma | NCI-H446 cells | CVCL_1562 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 35.50 nM | Negative KIT expression (KIT-) | ||
| Method Description |
C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
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| In Vitro Model | Lung squamous cell carcinoma | NCI-H2170 cells | CVCL_1535 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 47.63 nM | Negative KIT expression (KIT-) | ||
| Method Description |
C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
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| In Vitro Model | Amelanotic melanoma | MDA-MB-435 cells | CVCL_0417 | ||
References
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