TAK733
发布者：信康 浏览次数：
产品名称:TAK733CAS:1035555-63-5别名：英文名：TAK-733
[] - 生物活性TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1， AKT3， c-RAF， CamK1， CDK2及c-Met等活性。Phase 1。
- 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.
