Molecular Formula | C18H18N4O2 |
Molar Mass | 322.36 |
Density | 1.30±0.1 g/cm3(Predicted) |
Solubility | DMSO : 6.8 mg/mL (21.09 mM; Need ultrasonic and warming) |
pKa | 12.13±0.43(Predicted) |
Storage Condition | -20°C |
In vitro study | Takinib is an inhibitor of both auto-phosphorylated and non-phosphorylated TAK1 and binds to the ATP binding pocket of TAK1 to slow down the rate-limiting step in the activation of tak1. Takinib has significant inhibitory activity against six threonine/serine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2 and MINK1 at a concentration of 10 μm, TAK1/MAP3K7 was the most efficiently inhibited kinase with an IC50 of 9.5 nM. Treatment with Takinib induces TNF-α dependent apoptosis in RA cell models and metastatic breast cancer. Takinib does not inhibit MAP2Ks or MAP3Ks family members such as MKK6/MAP2K6, MEKK1/ MAP3K1, MKK1/MAP2K1. Takinib also had no inhibitory effect on MAP3K5/ASK1. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.102 ml | 15.511 ml | 31.021 ml |
5 mM | 0.62 ml | 3.102 ml | 6.204 ml |
10 mM | 0.31 ml | 1.551 ml | 3.102 ml |
5 mM | 0.062 ml | 0.31 ml | 0.62 ml |