PF-04691502

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: C₂₂H₂₇N₅O_4.
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.