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PF-04691502 Chemical Structure

PF-04691502

Data Sheet For research use only. Not for human use.
Cat. No. :BCP02895CAS No. :1013101-36-4Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 1013101-36-4 Cat. No. BCP02895
Name PF-04691502
Synonyms PF 04691502;PF04691502;
SMILES
Chemical Name
Formula C22H27N5O4 M. Wt 425.48
Purity 98% Storage Store at 4-8°C
Description PF-04691502 potently inhibits recombinant class I PI3K and mTOR in biochemical assays and suppresses transformation of avian fibroblasts mediated by wild-type PI3K γ, δ, or mutant PI3Kα. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF-04691502 reduces phosphorylation of AKT T308 and AKT S473 (IC(50) of 7.5-47 nM and 3.8-20 nM, respectively) and inhibits cell proliferation (IC(50) of 179-313 nM). PF-04691502 inhibits mTORC1 activity in cells as measured by PI3K-independent nutrient stimulated assay, with an IC(50) of 32 nM and inhibits the activation of PI3K and mTOR downstream effectors including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP. Short-term exposure to PF-04691502 predominantly inhibits PI3K, whereas mTOR inhibition persists for 24 to 48 hours. PF-04691502 induces cell cycle G(1) arrest, concomitant with upregulation of p27 Kip1 and reduction of Rb.
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