A PI3Kα, -β, -δ, -γ, and mTOR inhibitor
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PF-04691502

Item No. 15017

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
1013101-36-4
Synonyms
  • HNC-VP-L
  • PF-502
Molecular Formula
C22H27N5O4
Formula Weight
425.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
222, 302, 353 nm
SMILES
O=C1N([C@H]2CC[C@H](OCCO)CC2)C3=NC(N)=NC(C)=C3C=C1C4=CN=C(OC)C=C4
InChi Code
InChI=1S/C22H27N5O4/c1-13-17-11-18(14-3-8-19(30-2)24-12-14)21(29)27(20(17)26-22(23)25-13)15-4-6-16(7-5-15)31-10-9-28/h3,8,11-12,15-16,28H,4-7,9-10H2,1-2H3,(H2,23,25,26)/t15-,16-
InChi Key
XDLYKKIQACFMJG-WKILWMFISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    PF-04691502 is an inhibitor of PI3Kα, -β, -δ, and -γ and mammalian target of rapamycin (mTOR; Kis = 1.8, 2.1, 1.6, 1.9, and 16 nM, respectively, for the human enzymes).1 It decreases the proliferation of BT-20 breast cancer, SKOV3 ovarian cancer, and U87MG glioblastoma cells (IC50s = 313, 188, and 179 nM, respectively). PF-04691502 (2.5 and 5 µM) inhibits capillary tube formation by, and migration of, human umbilical vein endothelial cells (HUVECs).2 It induces cell cycle arrest at the G1 phase in U87MG cells when used at concentrations of 500 and 1,000 nM.1 PF-04691502 (10 mg/kg per day) decreases tumor volume in NCI H1650 and H1975 non-small cell lung cancer (NSCLC) mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yuan, J., Mehta, P.P., Yin, M.J., et al. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol. Cancer Ther. 10(11), 2189-2199 (2011).

    2. Wang, F.-Z., Peng-Jiao, Yang, N.-N., et al. PF-04691502 triggers cell cycle arrest, apoptosis and inhibits the angiogenesis in hepatocellular carcinoma cells. Toxicol. Lett. 220(2), 150-156 (2013).