TAK-733 1035555-63-5
TAK733
分子式:C17H15F2IN4O4 分子量:504.23
产品描述
TAK-733 是有效的,选择性MEK 变构抑制剂,作用于 MEK1,IC50为3.2 nM,抑制Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met等活性。
靶点
MEK1/2
IC50
3.2 nM
体外研究
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.
体内研究
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
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO