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PF-477736

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Chemical Structure| 952021-60-2 同义名 : PF-00477736;PF-736
CAS号 : 952021-60-2
货号 : A464575
分子式 : C22H25N7O2
纯度 : 98%+
分子量 : 419.48
MDL号 : MFCD16038847
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:

2% DMSO+40% PEG 300+water 5 mg/mL

生物活性
靶点
  • Chk1

    Chk1, Ki:0.49 nM

描述 PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes and shows ~100-fold selectivity for Chk1 than Chk2.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.92mL

2.38mL

1.19mL

23.84mL

4.77mL

2.38mL

参考文献

[1]Chakraborty J, Banerjee S, et al. Gain of cellular adaptation due to prolonged p53 impairment leads to functional switchover from p53 to p73 during DNA damage in acute myeloid leukemia cells. J Biol Chem. 2010 Oct 22;285(43):33104-12.

[2]Blasina A, Hallin J, et al. Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol Cancer Ther. 2008 Aug;7(8):2394-404.