Product Information
Kinase Inhibitor Name TAK-733
FormulaC17H15F2IN4O4
SolubilityDMSO ≥101 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
CAS No.1035555-63-5
Biological ActivityTAK-733 is highly potent and selective novel MEK allosteric site inhibitor with an IC50 of 3.2 nM. TAK-733 selectively binds to and inhibits the activity of MEK1/2. Subseqently, TAK-733 prevents the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often up-regulated in a variety of tumor cell types. TAK-733 has potent anticancer activity in various mouse xenograft models. TAK-733 showed potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. [1][2]
M.W.504.23
ReferencesDiscovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Dong Q et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9
MEK inhibitor TAK-733 http://cn.termwiki.com/EN:MEK_inhibitor_TAK-733
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.