| 产品描述： | KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities |
| 靶点： |
PDGFRβ:520 nM (Kd);PDGFRα:300 nM (Kd);B-Raf;c-Raf;FLT3:52 nM (Kd);KIT:170 nM (Kd);Raf; FLT; PDGFR; c-Kit |
| 体外研究： |
KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) and endothelial cells viability with EC50 values of 0.59 μM and 0.54 μM, respectively. Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259. KG5 (Compound 6) inhibits only PDGFRα and β with Kds of 300 and 520 nM, respectively, and Flt3 and KIT at 52 and 170 nM, respectively. KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK and ERK in endothelial cells stimulated with bFGF or VEGF |
| 体内研究： |
KG5 (Compound 6; 100 mg/kg; oral administration; daily; for 26 days) treatment prevents tumor growth in an orthotopic renal cell carcinoma model. KG5 (Compound 6; 50 mg/kg; i.p.; twice daily) treatment completely blocks angiogenesis relative to vehicle control in mice (injected with Matrigel containing bFGF). Pharmacokinetic analysis of the dose and formulation of KG5 used indicated a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an area under the concentration time curve (AUC0-12h) of 14.7 μg•h/mL. KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis. Animal Model: Male Nu/Nu mice injected with SN12C-RFP cells Dosage: 100 mg/kg Administration: Oral administration; daily; for 26 days Result: Prevented tumor growth in an orthotopic renal cell carcinoma model. |
| 参考文献： |
1. Eric A Murphy, et al. Disruption of angiogenesis and tumor growth with an orally active drug that stabilizes the inactive state of PDGFRbeta/B-RAF. Proc Natl Acad Sci U S A. 2010 Mar 2;107(9):4299-304. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.177 ml |
10.883 ml |
21.765 ml |
| 5 mM |
0.435 ml |
2.177 ml |
4.353 ml |
| 10 mM |
0.218 ml |
1.088 ml |
2.177 ml |
| 50 mM |
0.044 ml |
0.218 ml |
0.435 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