S80919 |
OSI-930 |
源叶(MedMol) | 99% |
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- 产品描述: OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity
- 靶点: KDR:9 nM (IC50);Flt-1:8 nM (IC50);Kit:80 nM (IC50);PDGFRβ:6900 nM (IC50);PDGFRα:3408 nM (IC50);CSF-1R:15 nM (IC50);c-Raf:41 nM (IC50);Flt-3:1303 nM (IC50);Lck:22 nM (IC50);Abl:4738 nM (IC50);Apoptosis;c-Fms;Raf;VEGFR;FLT;CSF-1R;Src;c-Kit
- 体内研究:
OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models
- 参考文献:
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.
- 溶解性: DMSO : 50 mg/mL (112.75 mM; Need ultrasonic)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.255 ml 11.275 ml 22.55 ml 5 mM 0.451 ml 2.255 ml 4.51 ml 10 mM 0.226 ml 1.128 ml 2.255 ml 50 mM 0.045 ml 0.226 ml 0.451 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)