| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京