Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0RANRT
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| ADC Name |
Hu-Alpha-EGFR-172
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| Synonyms |
Hu-alpha-EGFR 172
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Melanoma [ICD11:2C30]
Investigative
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
Cetuximab
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Antibody Info | ||||
| Antigen Name |
Epidermal growth factor receptor (EGFR)
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Antigen Info | ||||
| Payload Name |
IMSA172
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Payload Info | ||||
| Therapeutic Target |
Stimulator of interferon genes protein (STING1)
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Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
A mutant version of cetuximab hu-alphaEGFR(ACVC), provides four cysteines (heavy chain A114C and light chain V205C)on each antibody and was used for site-specific conjugation.
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
| Standard Type | Value | Units | Cell Line | Disease Model |
|---|---|---|---|---|
| Tumor Growth Inhibition value (TGI) |
90.3
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%
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B16-F10 cells
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Mouse melanoma
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Revealed Based on the Cell Line Data
| Standard Type | Value | Units | Cell Line | Disease Model |
|---|---|---|---|---|
| Half Maximal Inhibitory Concentration (IC50) |
> 10
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uM
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THP1-Lucia ISG cells
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Acute monocytic leukemia
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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) | 90.30% (Day 18) | High EGFR expression (EGFR+++) | ||
| Method Description |
To test the effect of STING ADCs in vivo, we used a mouse tumor model in which the C57BL/6J mice were implanted subcutaneously with B16F10 melanoma cells stably expressing human EGFR (B16-EGFR). After the tumors grew to ~100 mm 3 , STING ADCs were administered to the mice through intraperitoneal injection three times (200 g each time on day 5, 8, and 11 after tumor cell inoculation).
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| In Vivo Model | Melanoma CDX model | ||||
| In Vitro Model | Mouse melanoma | B16-F10 cells | CVCL_0159 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 uM | Negative EGFR expression (EGFR-) | ||
| Method Description |
Serial dilutions of IMSA172 or its conjugates with the indicated antibodies (ADCs) were incubated with THP1-ISG-Luc or this cell line stably expressing human EGFR (THP1-ISG-luc-EGFR; B and D) for 16 h, and the interferon response was measured by luciferase assay.
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| In Vitro Model | Acute monocytic leukemia | THP1-Lucia ISG cells | CVCL_X587 | ||
References
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