PF 04691502

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Cat.No. 4820 - PF 04691502 | C22H27N5O4 | CAS No. 1013101-36-4
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)
Datasheet
Citations
Literature

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
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1013101-36-4
PubChem ID 6741
InChI Key VHRSUDSXCMQTMA-PJHHCJLFSA-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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 425.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.35 mL 11.75 mL 23.5 mL
5 mM 0.47 mL 2.35 mL 4.7 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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Product Datasheets

Safety Datasheet

References

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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Citations for PF 04691502

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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Pathways for PF 04691502

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