Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0WIMOQ
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| ADC Name |
aU2023279443A1 Example 7
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| Synonyms |
AU2023279443A1 Example 7
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| Organization |
UBE CORPORATION
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
7.9
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| Antibody Name |
Trastuzumab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
U-031
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Payload Info | ||||
| Payload Name |
U-033
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Payload Info | ||||
| Linker Name |
AU2023279443A1, Example 4, Linker
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
Exemplification 3-7
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ADC-specific functional property(2027 Update)
Payload Release Efficiency
| Incubation Time | 24hr | Release | 112% | Reference |
[1]
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| Description |
Metabolism test using human liver lysosomal fraction. To a reaction composition solution in which human liver lysosome (corresponding to 0.125 mg of protein) was suspended and distilled water (10 uL) was added 1.2 uM test compound (25 uL) dissolved in PBS to prepare a reaction solution. After the reaction solution was incubated at 37 °C for 24 hours, U-031 released from the Example 7 into the reaction solution was quantified by LC-MS/MS.
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| Incubation Time | 24hr | Release | 106% | Reference |
[1]
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| Description |
Metabolism test using human liver lysosomal fraction. To a reaction composition solution in which human liver lysosome (corresponding to 0.125 mg of protein) was suspended and distilled water (10 uL) was added 1.2 uM test compound (25 uL) dissolved in PBS to prepare a reaction solution. After the reaction solution was incubated at 37 °C for 24 hours, U-033 released from the Example 7 into the reaction solution was quantified by LC-MS/MS.
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| Incubation Time | 24hr | Release | 139% | Reference |
[1]
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| Description |
Metabolism test using human liver Cathepsin B. To human liver Cathepsin B (corresponding to 400 Unit/mL) (5 pL), X10 Catabolic Buffer (10 uL), 2.5 mM Bovine Serum Albumin (5 uL), and distilled water (55 uL) was added 1.2 uM test compound (25 uL) dissolved in PBS to prepare a reaction solution. After the reaction solution was incubated at 37°C for 24 hours, U-031 released from the Example 7 into the reaction solution was quantified by LC-MS/MS.
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| Incubation Time | 24hr | Release | 121% | Reference |
[1]
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| Description |
Metabolism test using human liver Cathepsin B. To human liver Cathepsin B (corresponding to 400 Unit/mL) (5 pL), X10 Catabolic Buffer (10 uL), 2.5 mM Bovine Serum Albumin (5 uL), and distilled water (55 uL) was added 1.2 uM test compound (25 uL) dissolved in PBS to prepare a reaction solution. After the reaction solution was incubated at 37°C for 24 hours, U-033 released from the Example 7 into the reaction solution was quantified by LC-MS/MS.
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General Information of The Activity Data Related to This ADC
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 | Cell growth inhibition rate (%) | < 10% | Negative HER2 expression (HER2-) | ||
| Method Description |
Growth inhibition test of HER2-negative human breast cancer cell line (MDA-MB-231). The cells were seeded at 1000 cells / 100 pL / well. The cells were cultured at 37 0 C overnight, then the medium was exchanged with new one (95 uL/well), and the cells were treated with a test compound, which was adjusted to 2 ug/mL with PBS , at 5 uL/well (treatment concentration: 100 ng/mL). The cells were cultured for 6 days, then CellTiter-Glo was added thereto at 100 uL/well, and the luminescence amount of each well was measured.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | 107% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||