| 产品描述： | R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence |
| 靶点： |
KDR:10 nM (IC50);FGFR1:28 nM (IC50);VEGFR;FGFR;FLT;PDGFR |
| 体内研究： |
R1530 (1.56, 25, and 50 mg/kg; p.o.; daily, for 28 days.) has notable antitumor activity across a broad range of human xenograft models, with minimal toxicity. Animal Model: Human tumor xenograft models Dosage: 1.56, 25 and 50 mg/kg Administration: Oral administration; daily, for 28 days. Result: Inhibited tumor growth in all models, with regression observed in all models tested at a 50 mg/kg dose. |
| 参考文献： |
1. Jin-Jun Liu, et al. Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors. ACS Med Chem Lett. 2013 Feb 14; 4(2): 259–263. 2. Christian Tovar, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.803 ml |
14.014 ml |
28.028 ml |
| 5 mM |
0.561 ml |
2.803 ml |
5.606 ml |
| 10 mM |
0.28 ml |
1.401 ml |
2.803 ml |
| 50 mM |
0.056 ml |
0.28 ml |
0.561 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