| 产品描述： | Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity |
| 靶点： |
VEGFR2:2.2 nM (IC50);Braf:7.0 nM (IC50);VEGFR |
| 体内研究： |
Takeda-6D (compound 6d) (10 mg/kg, Orally, once) shows sufficient oral bioavailability (F = 70.5%) in rats. Takeda-6D (0-10 mg/kg, Orally, once) significantly decreases phosphorylation levels of ERK1/24 h after oral administration in an A375 (BRAFV600E mutant) human melanoma xenograft model in rats. Takeda-6D (10 mg/kg, Orally, twice daily for 2 weeks) shows tumor regression with T/Cof −7.0% without severe toxicity, and this tumor regression should include the efficacy based on the antiangiogenesis potency and BRAF inhibitory activity |
| 参考文献： |
1. Okaniwa M, et al. Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds. J Med Chem. 2012 Apr 12;55(7):3452-78. |
| 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 |
1.825 ml |
9.124 ml |
18.249 ml |
| 5 mM |
0.365 ml |
1.825 ml |
3.65 ml |
| 10 mM |
0.182 ml |
0.912 ml |
1.825 ml |
| 50 mM |
0.036 ml |
0.182 ml |
0.365 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