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PF-04691502 inhibits PI3K and mTORC1/2, exhibiting anticancer chemotherapeutic and anti-angiogenic activities. In nasopharyngeal carcinoma cells, PF-04691502 induces G0/G1 cell cycle arrest and apoptosis, inhibiting proliferation. In similar animal models, PF-04691502 decreases tumor volume and weight. Additionally, PF-04691502 decreases tumor growth of bladder cancer tumors in vivo and decreases VEGF secretion and cell proliferation in vitro.
| Purity | ≥98% |
|---|---|
| Formula | C22H27N5O4 • 2H2O |
| Formula Wt. | 461.51 |
| Solubility | DMSO 14 mg/mL (32.9 mM) Water Insoluble Ethanol Insoluble |
| Appearance | Yellow Powder |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet | |
| Brochures |
Cirone P, Andresen CJ, Eswaraka JR, et al. Patient-derived xenografts reveal limits to PI3K/mTOR- and MEK-mediated inhibition of bladder cancer. Cancer Chemother Pharmacol. 2014 Mar;73(3):525-38. PMID: 24442130.
Wong CH, Loong HH, Hui CW, et al. Preclinical evaluation of the PI3K-mTOR dual inhibitor PF-04691502 as a novel therapeutic drug in nasopharyngeal carcinoma. Invest New Drugs. 2013 Dec;31(6):1399-408. PMID: 23975511.
Yuan J, Mehta PP, Yin MJ, et al. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol Cancer Ther. 2011 Nov;10(11):2189-99. PMID: 21750219.