S80704 |
Dovitinib (TKI-258, CHIR-258) |
源叶(MedMol) | 99% |
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- 产品描述: Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity
- 靶点: FLT3:1 nM (IC50);c-Kit:2 nM (IC50);FGFR1:8 nM (IC50);FGFR3:9 nM (IC50);VEGFR3:8 nM (IC50);VEGFR1:10 nM (IC50);VEGFR2:13 nM (IC50);PDGFRβ:27 nM (IC50);PDGFRα:210 nM (IC50);CSF-1R:36 nM (IC50);VEGFR;FGFR;FLT;PDGFR;c-Kit
- 体内研究:
Dovitinib (CHIR-258; 10-60 mg/kg/day; gavage; for 21 days) has a significant antitumor effect. Dovitinib (50 and 75 mg/kg) results in 97% and 98% tumor growth inhibition, respectively, and the maximal efficacy is at 50 mg/kg.
- 参考文献:
1. Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948. 2. Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56(3), 595-601. 3. Lee Y, et al. A Receptor Tyrosine Kinase Inhibitor, Dovitinib (TKI-258), Enhances BMP-2-Induced Osteoblast Differentiation In Vitro. Mol Cells. 2016 May 31;39(5):389-94 4. Chon HJ, et al. Traf2- and Nck-interacting kinase (TNIK) is involved in the anti-cancer mechanism of dovitinib in human multiple myeloma IM-9 cells. Amino Acids. 2016 Jul;48(7):1591-9.
- 溶解性: DMSO : 25 mg/mL (63.71 mM; Need ultrasonic and warming)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.548 ml 12.741 ml 25.482 ml 5 mM 0.51 ml 2.548 ml 5.096 ml 10 mM 0.255 ml 1.274 ml 2.548 ml 50 mM 0.051 ml 0.255 ml 0.51 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)