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PKI-402 is an inhibitor of PI3K that is somewhat selective for p110α; it also inhibits mTORC1/2. PKI-402 exhibits anticancer chemotherapeutic activity, inhibiting cell proliferation in vitro and suppressing tumor growth induced by a variety of cancer cells in vitro, such as breast cancer, glioma, and pancreatic cancer.
| Cas No. | 1173204-81-3 |
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| Purity | ≥98% |
| Formula | C29H34N10O3 |
| Formula Wt. | 570.65 |
| IUPAC Name | 1-[4-(3-ethyl-7-morpholin-4-yltriazolo[4,5-d]pyrimidin-5-yl)phenyl]-3-[4-(4-methylpiperazine-1-carbonyl)phenyl]urea |
| Solubility | DMSO 0.4 mg/mL (0.7 mM) Water Insoluble Ethanol Insoluble |
| Appearance | Off-white Powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet | |
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Mallon R, Hollander I, Feldberg L, et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84. PMID: 20371716.
Dehnhardt CM, Venkatesan AM, Delos Santos E, et al. Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402. J Med Chem. 2010 Jan 28;53(2):798-810. PMID: 19968288.