Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0GCLJQ
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| ADC Name |
Trastuzumab-C239I-SG3600
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| Drug Status |
Investigative
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| Indication |
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
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| Drug-to-Antibody Ratio |
1.89
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| Structure |
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| Antibody Name |
Engineered trastuzumab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
N10-beta-glucuronide SG3200
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Payload Info | ||||
| Therapeutic Target |
Human Deoxyribonucleic acid (hDNA)
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Target Info | ||||
| Linker Name |
Mal-PEG8-Val-Ala-PABC
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Linker Info | ||||
| Conjugate Type |
Coupling of cysteine sulfhydryl groups in antibodies with maleimide.
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| Combination Type |
SG3600
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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) | ≈ 62.20% (Day 50) | Low HER2 expression (HER2+) | ||
| Method Description |
The antitumor activity of trastuzumab-C239i-SG3600 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
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| In Vivo Model | Gastric cancer CDX model | ||||
| In Vitro Model | Gastric cancer | Gastric cancer cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 65.10% (Day 50) | Negative expression (HER2-) | ||
| Method Description |
The antitumor activity of trastuzumab-C239i-SG3600 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast cancer | Breast cancer cells | Homo sapiens | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 50) | Low HER2 expression (HER2+) | ||
| Method Description |
The antitumor activity of trastuzumab-C239i-SG3600 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 3 mg/kg was chosen for both ADCs to observe any difference in activity.
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| In Vivo Model | Gastric cancer CDX model | ||||
| In Vitro Model | Gastric cancer | Gastric 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) | 16.10 ng/mL | Low HER2 expression (HER2+) | ||
| Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 24.10 ng/mL | Low HER2 expression (HER2+) | ||
| Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
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| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 33.90 ng/mL | Low HER2 expression (HER2+) | ||
| Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative expression (HER2-) | ||
| Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative expression (HER2-) | ||
| Method Description |
The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
References
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