Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0KWPXB
|
|||||
|---|---|---|---|---|---|---|
| ADC Name |
Tras (C4)-Cp
|
|||||
| Synonyms |
Tras (C4)-Cp
Click to Show/Hide
|
|||||
| Organization |
Technical University of Darmstadt.; University of Bielefeld.; Lantern Pharma Inc.; The University of Tennessee.; Technical University of Darmstadt.
|
|||||
| Drug Status |
Investigative
|
|||||
| Drug-to-Antibody Ratio |
3
|
|||||
| Structure |
|
|||||
| Antibody Name |
Trastuzumab (C4)
|
Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
|
Antigen Info | ||||
| Payload Name |
Cryptophycin-uD[Dap (Me)]
|
Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
|
Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
|
Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
|
|||||
ADC-specific functional property(2027 Update)
Binding Affinity
| Dissocation Constant (Kd) | Binding Target | Description | Reference |
|---|---|---|---|
| 3.2 nM |
SK-BR-3 cells (HER2)
|
EC50 values of the affinity of the ADCs binding to SK-BR-3 cells.
|
[1]
|
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
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 | Half Maximal Effective Concentration (EC50) | 30 pM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 515𫐫 pM | Moderate HER2 expression (HER2++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
|
||||
| In Vitro Model | Bladder carcinoma | RT112 cells | CVCL_1670 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 982𫛫 pM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
|
||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
References