产品描述: PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively. |
靶点:
PI3Kα:0.13 nM (Ki);PI3Kγ:0.111 nM (Ki);PI3Kδ:0.122 nM (Ki);mTOR:1.42 nM (Ki);PI3K; mTOR |
体外研究:
PF-04979064 is tested against human class I PI3K isoforms PI3Kα, PI3Kγ, and PI3Kδ, with PI3Kα Ki of 0.13 nM, PI3Kγ Ki of 0.111 nM, and PI3Kδ Ki of 0.122 nM |
体内研究:
PF-04979064 is progressed to rat in vivo PK studies and exhibits robust PK profile: Vdss=5.23 L/kg, Cl=19.3 mL/min/kg, T1/2=1.85 h, and F%=61% |
参考文献:
1. Cheng H et al. Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett, 2012 Nov 7, 4(1):91-7. |
溶解性:
soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.24 ml |
11.198 ml |
22.396 ml |
5 mM |
0.448 ml |
2.24 ml |
4.479 ml |
10 mM |
0.224 ml |
1.12 ml |
2.24 ml |
50 mM |
0.045 ml |
0.224 ml |
0.448 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。 |