Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0ZZHUS
|
|||||
|---|---|---|---|---|---|---|
| ADC Name |
aU2023279443A1 Example A6
|
|||||
| Synonyms |
AU2023279443A1 Example A6
Click to Show/Hide
|
|||||
| Organization |
UBE CORPORATION
|
|||||
| Drug Status |
Investigative
|
|||||
| Drug-to-Antibody Ratio |
8
|
|||||
| Antibody Name |
Trastuzumab
|
Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
|
Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
|
Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
|
Target Info | ||||
| Linker Name |
AU2023279443A1, Example A6, Linker
|
Linker Info | ||||
| Conjugate Type |
site formylglycine residue random conjugation
|
|||||
| Combination Type |
Exemplification A3-6
|
|||||
ADC-specific functional property(2027 Update)
Payload Release Efficiency
| Incubation Time | 24hr | Release | 78% | Reference |
[1]
|
|---|---|---|---|---|---|
| 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, MMAE released from the Example A6 into the reaction solution was quantified by LC-MS/MS.
Click to Show/Hide
|
||||
| Incubation Time | 24hr | Release | 67% | Reference |
[1]
|
| 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, MMAE released from the Example A6 into the reaction solution was quantified by LC-MS/MS.
Click to Show/Hide
|
||||
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 lnhibition value (TGl) |
> 100
|
%
|
Undisclosed | Undisclosed |
Revealed Based on the Cell Line Data
| Standard Type | Value | Units | Cell Line | Disease Model |
|---|---|---|---|---|
| Cell growth inhibition rate (%) |
> 14
|
%
|
CVCL_1603
|
Gastric tubular adenocarcinoma
|
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 lnhibition value (TGl) | > 100% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.
Click to Show/Hide
|
||||
| In Vivo Model | NCI-N87 female BALB/c-nu/nu mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | 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.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||