PF-04691502 Inhibitor CAS No. 1013101-36-4

Cat. No.	Name	Size	Price
KI1215	PF-04691502	5 mg	$176
	PF-04691502	10 mg	$270
	PF-04691502	50 mg	$850
	PF-04691502	200 mg	$3000

Chemical Characteristic

Product Name	PF-04691502
CAS No.	1013101-36-4
Molecular Weight	425.48
Formula	C₂₂H₂₇N₅O₄
Chemical Name	2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
Smiles	c1(nc2c(c(n1)C)cc(c(=O)n2C1CC[C@@H](CC1)OCCO)c1cnc(cc1)OC)N
Chemical Structure

Biological activities

PF-04691502 is an ATP-competitive PI3K/mTOR dual inhibitor. PF-04691502 inhibits human PI3K isoforms α, β, δ, γ and mTOR with Ki of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively. PF-04691502 potently inhibits AKT phosphorylation on S473 in all the cancer cell lines BT20, SKOV3 and U87MG with IC50s of 20, 7.4 and 3.8 nM, respectively. PF-04691502 inhibits the activation of PI3K and mTOR downstream effectors including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP. PF-04691502 induces cell cycle G1 arrest, concomitant with upregulation of p27 Kip1 and reduction of Rb. In vivo, PF-04691502 shows robust antitumor activity in 4 NSCLC xenograft models, NCI-H1650 and A549, NCI-H1975 and NCI-H460. ^[1] PF-04691502 inhibits tumor growth at 7 days by 72%. PF-04691502 inhibits dramatically tissue biomarkers of PI3K/mTOR pathway activity, p-AKT (S473), and p-RPS6 (S240/244). The combination of PF-04691502 with PD-0325901 leads to dramatic tumor regression and long-term survival of tumor-bearing mice. ^[2]

Protocols

PF-04691502 is prepared in 0.5% methylcellulose. ^[2]

References

[1] Kinross KM, et al. In vivo activity of combined PI3K/mTOR and MEK inhibition in a Kras (G12D); Pten deletion mouse model of ovarian cancer. Mol Cancer Ther. 2011, 10(8): 1440-1449. [2] Yuan J, et al. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol Cancer Ther. 2011, 10(11): 2189-2199

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