Molecular Formula | C49H60ClN9O7S2 |
Molar Mass | 986.65 |
Density | 1.39±0.1 g/cm3(Predicted) |
Solubility | 10 mM in DMSO |
pKa | 13.61±0.46(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.014 ml | 5.068 ml | 10.135 ml |
5 mM | 0.203 ml | 1.014 ml | 2.027 ml |
10 mM | 0.101 ml | 0.507 ml | 1.014 ml |
5 mM | 0.02 ml | 0.101 ml | 0.203 ml |
biological activity | ARV-771 is an effective pan-(bromodomain and extra-terminal)BET degradation agent, A new BET-PROTAC (protein-targeting chimera), for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) have Kd values of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM, respectively. |
Target | Value |
BRD2-BD2 (Cell-free assay) | 4.7 nM(Kd) |
BRD3-BD2 (Cell-free assay) | 7.6 nM(Kd) |
BRD4-BD2 (Cell-free assay) | 7.6 nM(Kd) |
BRD3-BD1 (Cell-free assay) | 8.3 nM(Kd) |
BRD4-BD1 (Cell-free assay) | 9.6 nM(Kd) |
Use | an effective BET degradant of the PROTAC class. |