TAK-733 (C007B-298954)

InformationTAK-733 is a potent and selectiveMEKallosteric site inhibitor for MEK1 withIC50of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.In vitroTAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells.In vivoTAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg.Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥96%. Specification: 10mM in DMSO Molecular Formula: C17H15F2IN4O4 Molecular Weight: 504.23