Molecular Formula | C25H28N6O |
Molar Mass | 428.53 |
Density | 1.31±0.1 g/cm3(Predicted) |
Boling Point | 657.6±65.0 °C(Predicted) |
Solubility | 10 mM in DMSO |
pKa | 8.70±0.60(Predicted) |
Storage Condition | -20℃ |
In vitro study | AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC 50 s of 3 nM and 1 nM, respectively. AZ6102 alao has 100-fold selectivity against other PARP family enzymes, with IC 50 s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively. AZ6102 shows Wnt pathway inhibition in DLD-1 cells. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.334 ml | 11.668 ml | 23.336 ml |
5 mM | 0.467 ml | 2.334 ml | 4.667 ml |
10 mM | 0.233 ml | 1.167 ml | 2.334 ml |
5 mM | 0.047 ml | 0.233 ml | 0.467 ml |
biological activity | AZ6102 is a potent dual inhibitor of TNKS1 and tnks2, the IC50 values were 3 nM and 1 nM, and the selectivity was 100 times higher than that for other PARP family proteins. The IC50 values for PARP1,PARP2 and PARP6 were 2.0 μm, 0.5 M and> 3 M. |