Product Name

PF04691502

General description

PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor.

Synonym

2-amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one; PF 04691502; PF-04691502

Purity

≥98%(HPLC)

CAS Number

1013101-36-4

Formula

C²²H²⁷N⁵O⁴

Molecular Weight

425.489

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White or Off-white solid

Solubility(25℃)

DMSO

≥10mg/mL

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol   Actions

PF-04691502 is a potent dual mTOR/PI3K inhibitor with Ki values of 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI 3-K δ, α, β, γ, and mTOR, respectively, with no significant inhibitory activity at more than 80 other protein kinases, including PI 3-K downstream kinases, and MAPK family members. PF-04691502 showed antitumor activity in several non-small cell lung carcer (NSCLC) xenografts and ovarian cancer cell lines. PF-04691502 is currently in clinical trials.

Application

PF-04691502 has been used in trials studying the treatment of Cancer, Breast Neoplasms, Early Breast Cancer (Phase 2), and Advanced Breast Cancer (Phase 1b).

l  Packaging & Storage

Packaging

5mg;  25mg; 100mg

Storage temp.

0-5℃

l  Precautions and Disclaimer

This   product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov