化学性质:
规格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg |
CAS | 952021-60-2 |
别名 |
|
化学名 | (R)-2-amino-2-cyclohexyl-N-(2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-4H-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide |
分子式 | C22H25N7O2 |
分子量 | 419.48 |
溶解度 | ≥ 5.2mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
PF-477736 is a potent, selective ATP-competitive and small-molecule inhibitor of Chk1 with a Ki of 0.49±0.29nM for the in vitro kinase activity of Chk1 [1].
PF-477736 has shown a selective inhibition of Chk1 with the IC50 values of 0.49nM, 9.9μM and 47nM for Chk1, CDK1 and Chk2, respectively. In a dot-blot assay, PF-477736 has been reported to inhibit camptothecin-induced G2 arrest with the EC50 values of 45nM, 38nM and 42nM in P53-mutated human lymphoma CA46 cells, HeLa cells and HT29 cells. Apart from these, PF-477736 has been found to selectively target p53-defective cancer cells while having minimal cytotoxic effects on normal (p53-competent) cells. In addition, PF-00477736 has been revealed to dose-dependently enhance the antitumor activity of a MTD of gemcitabine with no apparent exacerbation of systemic toxicity as assessed by monitoring body weight in the Colo205 xenograft [1].
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
标签:PF-477736
联系人:高小姐
手 机:13585831301
Q Q:3004967995
座 机:021-59541103
传 真:021-60443211
地 址:上海嘉定区嘉罗公路1661