现货,PF-04217903,CAS号:956905-27-4 ,美国进口,受体酪氨酸激酶(RTK) , c-Met ,c-Met 抑制剂和化合物,目录号S1094

信号转导通路: 受体酪氨酸激酶(RTK) >> c-Met >> c-Met 抑制剂和化合物 >> PF-04217903http://selleck.cn/pf-04217903-S1094.html

技术数据:

分子量(MW): 372.38

化学式:

C19H16N8O

 

溶解度: DMSO ≥75mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 956905-27-4

生物活性

 

 

PF-04217903 is an orally bioavailabe, small-molecule MET tyrosine kinase inhibitor with potential antineoplastic activity. [1]

PF-04217903 demonstrates exquisite kinase selectivity. Inhibition studies of the c-Met mutants show that PF-04217903 is more susceptible to oncogenic mutations that attenuate potency than PF-02341066. [1]

PF-04217903 was evaluated against multiple kinase selectivity screening panels: Invitrogen Inc. (125 kinases), Millipore/Upstate Ltd. (105 kinases), University ofDundee (51 kinases), and Pfizer in-house (48 kinases) (Supporting Information). On the basis of the percent inhibition or IC50 values generated from each of these screens, PF-04217903 was estimated to be>1000-fold selective for c-Met compared with each of the other kinases included in these collective screening assays. [1]

 

 

 

参考文献

Enzymatic Characterization of c-Met Receptor Tyrosine Kinase Oncogenic Mutants and Kinetic Studies with Aminopyridine and Triazolopyrazine Inhibitors Sergei L. Timofeevski, Michele A. McTigue, et al. Biochemistry 2009;48:5339–5349

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