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噻爾非尼OSI-930是Kit,KDR和CSF-1R的抑制劑,IC50分別為80 nM,9 nM和15 nM,對Flt-1,c-Raf和Lck有接近的抑制性,但對 PDGFRα/β,F(xiàn)lt-3和Abl抑制性較弱。
[1]. Garton AJ, et al. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006, 66(2):1015-1024.
[2]. Lin HL, et al. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011, 39(2), 345-350.
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