PF 04691502

Pricing Availability Delivery Time Qty
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
Reviews
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.

Compound Libraries

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

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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

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

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


If you know of a relevant reference for PF 04691502, please let us know.

View Related Products by Target

View Related Products by Product Action

View all PI 3-kinase Inhibitors

Keywords: PF 04691502, PF 04691502 supplier, PF04691502, phosphoinositide, 3-kinases, PI, 3-K/mTOR, mammalian, Target, Rapamycin, FRAP, FK506, binding, protein, 12, FKBP12, rapamycin, associated, cell, cycle, antitumor, 3-Kinase, mTOR, 4820, Tocris Bioscience

Citations for PF 04691502

Citations are publications that use Tocris products.

Currently there are no citations for PF 04691502. Do you know of a great paper that uses PF 04691502 from Tocris? Please let us know.

Reviews for PF 04691502

There are currently no reviews for this product. Be the first to review PF 04691502 and earn rewards!

Have you used PF 04691502?

Submit a review and receive an Amazon gift card.

$10US/$10CAN/€7/£6 gift card for a review without an image

$25US/$25CAN/€18/£15 gift card for a review with an image

*Offer only valid in the USA / Canada, UK and Europe

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Kinases

Kinases Product Listing

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

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling