PF 04691502

Name: PF 04691502
Brand: Tocris Bioscience
SKU: 4820

Tocris Bioscience a Bio-Techne Brand

Catalog # 4820

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Key Product Details

Description:	Potent and selective dual PI 3-K/mTOR inhibitor
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
Purity:	≥98% (HPLC)
Molecular Weight:	425.48

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Biological Activity for PF 04691502

PF 04691502 is a potent and selective dual ATP-competitive PI 3-K/mTOR inhibitor (K_i 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 bioavailable. 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.

Compound Libraries for PF 04691502

PF 04691502 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 04691502

M. Wt	425.48
Formula	C₂₂H₂₇N₅O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1013101-36-4
PubChem ID	25033539
InChi Key	XDLYKKIQACFMJG-UHFFFAOYSA-N
Smiles	O=C2C(C4=CC=C(OC)N=C4)=CC1=C(C)N=C(N)N=C1N2[C@@H]3CC[C@@H](OCCO)CC3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 04691502

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	42.55	100

Preparing Stock Solutions for PF 04691502

The following data is based on the product molecular weight 425.48.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.35 mL	11.75 mL	23.50 mL
5 mM	0.47 mL	2.35 mL	4.70 mL
10 mM	0.24 mL	1.18 mL	2.35 mL
50 mM	0.05 mL	0.24 mL	0.47 mL

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References for PF 04691502

References are publications that support the biological activity of the product.

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

Citations for PF 04691502

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