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Background Information:
PF-04691502 is a potent, selective and orally active ATP-competitive PI3K/mTOR inhibitor with Ki values of 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI3K δ, α, γ, β, and mTOR, respectively, displaying no significant inhibitory activity towards more than 80 protein kinases (concentration ≥ 10 μM) including hVps34, PI3K downstream kinases, and MAPK family members, and inducing robust cell cycle arrest at the G1 phase in U87MG cancer cells and antitumor activity in SKOV3 ovarian cancer xenograft models.
Reference:
1. Cheng, H., et al, “Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design”, Med. Chem. Commun., (2010), 1, 139 -144.
APIM050225: PF-04691502
CAS No.: 1013101-36-4.
Molecular Formula: C22H27N5O4.
Molecular Weight: 425.5.
Purity: >99% (HPLC at 214 and 254 nm).
QC: MS, 1HNMR, HPLC, and Microanalysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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