產品描述: | MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity |
靶點: |
VEGFR2:10 nM (IC50);c-Met:29 nM (IC50);Apoptosis;?VEGFR;?c-Met/HGFR |
體內研究: |
MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice. MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and Cmax (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg). MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) |
參考文獻: |
1. Claridge S, et al. Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.932 ml |
9.66 ml |
19.32 ml |
5 mM |
0.386 ml |
1.932 ml |
3.864 ml |
10 mM |
0.193 ml |
0.966 ml |
1.932 ml |
50 mM |
0.039 ml |
0.193 ml |
0.386 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |