TAK-733  1035555-63-5

TAK733
分子式：C17H15F2IN4O4   分子量：504.23
 
產(chǎn)品描述
TAK-733 是有效的，選擇性MEK 變構(gòu)抑制劑，作用于 MEK1，IC50為3.2 nM，抑制Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met等活性。
靶點(diǎn)
MEK1/2
         
IC50
3.2 nM
         
體外研究
TAK-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.
體內(nèi)研究
TAK-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.
溶解性
DMSO 101 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO