Chemical Structure : PF-06843195
CAS No.: 2067281-51-8
Catalog No.: PC-49021Not For Human Use, Lab Use Only.
PF-06843195 is a potent, selective PI3Kα inhibitor with Ki value of <0.018 nM, IC50 of 18 nM (RAT1 PI3Kα), with cellular isoform selectivity of 20-fold over PI3Kβ and 9-fold over PI3Kδ.
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PF-06843195 is a potent, selective PI3Kα inhibitor with Ki value of <0.018 nM, IC50 of 18 nM (RAT1 PI3Kα), with cellular isoform selectivity of 20-fold over PI3Kβ and 9-fold over PI3Kδ.
PF-06843195 also demonstrated high selectivity over mTOR.
PF-06843195 is a potent inhibitor of both PI3Kα (Ki< 0.018 nM) and PI3Kδ (Ki< 0.28 nM), but found to be 9-fold selective for PI3Kα over PI3Kδ in cell assays.
PF-06843195 is selective over two other members of the class I catalytic PI3K kinase group, PI3Kβ and PI3Kγ, >100- and >10 000-fold, respectively, in biochemical assays and 20-fold selective over PI3Kβ in cell assays.
M.Wt | 498.467 | |
Formula | C20H25F3N8O4 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
2,2-difluoroethyl (3S)-3-{[2'-amino-5-fluoro-2-(morpholin-4-yl)-4,5'-bipyrimidin-6-yl]amino}-3-(hydroxymethyl)pyrrolidine-1-carboxylate |
1. Cheng H, et al. J Med Chem. 2021 Jan 14;64(1):644-661.
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