PF 04691502

Cat. No. 4820

PF 04691502 C22H27N5O4 [1013101-36-4]

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Chemical Name: 2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one

Biological Activity

Potent and selective dual ATP-competitive PI 3-K/mTOR inhibitor (Ki values are 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI 3-K δ, α, γ, β, and mTOR, respectively). Displays no significant inhibitory activity at more than 80 protein kinases (concentration ≥ 10 μM) including hVps34, PI 3-K downstream kinases, and MAPK family members. Orally available. Induces robust cell cycle arrest at the G1 phase in U87MG cancer cells and antitumor activity in SKOV3 ovarian cancer xenograft models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
425.48
Formula:
C22H27N5O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1013101-36-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Yuan et al (2011) PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol.Cancer Ther. 10 2189. PMID: 21750219.

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Keywords: PF 04691502, supplier, PF04691502, phosphoinositide, 3-kinases, PI, 3-K/mTOR, mammalian, Target, Rapamycin, FRAP, FK506, binding, protein, 12, FKBP12, rapamycin, associated, protein, cell, cycle, antitumor, Tocris Bioscience, PI 3-kinase Inhibitor products

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