PF-04979064 |
| カタログ番号GC19283 |
PF-04979064 は、強力で選択的な PI3K/mTOR デュアル キナーゼ阻害剤であり、PI3Kα と mTOR の Kis はそれぞれ 0.13 nM と 1.42 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1220699-06-8
Sample solution is provided at 25 µL, 10mM.
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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.
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[1].
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%[1].
References:
[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.
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