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OSI-930
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
OSI-930图片
CAS NO:728033-96-3
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
OSI-930 是 Kit、KDR 和 CSF-1R (c-Fms) 的口服选择性抑制剂，IC50 分别为 80 nM、9 nM 和 15 nM。 OSI-930 还适度抑制 Flt-1、c-Raf、Lck 和对 PDGFRα/β、Flt-3 和 Abl 的低活性。 OSI-930 具有抗肿瘤活性。
Cas No.728033-96-3
别名噻尔非尼
化学名3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide
Canonical SMILESC1=CC=C2C(=C1)C(=CC=N2)CNC3=C(SC=C3)C(=O)NC4=CC=C(C=C4)OC(F)(F)F
分子式C22H16F3N3O2S
分子量443.44
溶解度≥ 22.15mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

OSI-930 is a novel, potent inhibitor of Flt1, kinase insert domain receptor (KDR), CSF-1R, Lck, c-Raf and activated receptor tyrosine kinases Kit with IC50 values of 8, 9, 15, 22, 41 and 80 nM, respectively [1].

OSI-930 has been demonstrated to inhibit proliferation and induce apoptosis in the HMC-1 cell line which is highly dependent on Kit signaling for survival. On the contrary, OSI-930 revealed no growth inhibition of COLO-205 cell line under normal culture conditions [1].

OSI-930 has shown to time- and concentration-dependently inactivate P450 3A4. Additionally, OSI-930 could reduce CO difference spectra of P450 3A4 [2].

References:
[1] Garton AJ1, Crew AP, Franklin M, Cooke AR, Wynne GM, Castaldo L, Kahler J, Winski SL, Franks A, Brown EN, Bittner MA, Keily JF, Briner P, Hidden C, Srebernak MC, Pirrit C, O'Connor M, Chan A, Vulevic B,Henninger D, Hart K, Sennello R, Li AH, Zhang T, Richardson F, Emerson DL, Castelhano AL, Arnold LD,Gibson NW. 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 Jan 15;66(2):1015-24.
[2] Lin HL1, Zhang H, Medower C, Hollenberg PF, Johnson WW. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011 Feb;39(2):345-50.