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PF-04691502
Cat No.
CEI-0138
Description
PF-04691502 inhibits PI3K-alpha, PI3K-beta, PI3K-delta, PI3K-gamma, and mTOR with Ki of 1.8 nM, 2.1 nM, 1.6 nM, and 1.9 nM and 16 nM.
CAS No.
1013101-36-4
Molecular Weight
425.48
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
PI3K, mTOR
Molecular Formula
C22H27N5O4
Chemical Name
2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
Solubility
DMSO 14 mg/mL Water
In vitro
PF-04691502 is an ATP-competitive, selective inhibitor of Class I PI3K and mTOR. PF-04691502 inhibits PI3K-alpha, PI3K-beta, PI3K-delta, PI3K-gamma, and mTOR with Ki of 1.8 nM, 2.1 nM, 1.6 nM, and 1.9 nM and 16 nmol/L. PF-04691502 inhibits PI3K/mTOR signaling and induces cell cycle arrest in cancer cell. PF-04691502 can induce cell cycle arrest at the G1 phase in a dose-dependent manner in U87MG cells. Besides above, PF-04691502 can modestly increase caspase 3/7 activities ( 3-fold) in a dose-dependent manner in U87MG cells. For cell linePF-04691502 inhibits cell proliferation of BT20, SKOV3, and U87MG with IC 50 values of 313 nM, 188 nM, and 179 nM.
In vivo
In a U87MG xenograft model, treatment with 10 mg/kg PF-04691502 resulted in a significant reduction of P-AKT(S473) levels at 1 hour postdosing, and persistent inhibition was observed for 8 hours PF-04691502 also shows robust antitumor activity in ovarian cancer and NSCLC models. The effect of PF-04691502 was also measured in a time-dependent manner at 1, 7, and 24 hours post 10 mg/kg dose. Phosphorylation of AKTS473, PRAS40, 4EBP1, and S6RP was inhibited up to 7 hours after dosing.
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