Molecular Formula | C17H15F2IN4O4 |
Molar Mass | 504.23 |
Density | 1.91±0.1 g/cm3(Predicted) |
Boling Point | 530.5±60.0 °C(Predicted) |
pKa | 13.72±0.20(Predicted) |
Storage Condition | -20℃ |
In vitro study | TAK-733 is a highly potent and selective allosteric site inhibitor of MEK with an IC50 of 3.2 nM. TAK-733 exhibited potent enzymatic and cellular activity with an EC50 of 1.9 nM for ERK phosphorylation in cells. |
In vivo study | TAK-733 demonstrated broad-spectrum antitumor activity in mouse xenograft models of human tumors, including melanoma, colorectal, NSCLC, pancreatic, and breast cancers. TAK-733 has good pharmacokinetic and pharmacodynamic tolerability and can be administered orally once daily to humans. The maximum effective dose of TAK-733 is 10 mg/kg once daily. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.983 ml | 9.916 ml | 19.832 ml |
5 mM | 0.397 ml | 1.983 ml | 3.966 ml |
10 mM | 0.198 ml | 0.992 ml | 1.983 ml |
5 mM | 0.04 ml | 0.198 ml | 0.397 ml |