PF 05212384

• Supplier: Tocris Bioscience
• Catalog: 5790
• Prices: $255.00
• Sizes: 10 mg
• Function Type: Inhibitor
• Cas Number: 1197160-78-3
• Chemical Name: N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]urea
• Formula: C32H41N9O4
• Molecular Weight: 615.73
• Purity: >98 %
• Description: Potent and selective dual inhibitor of PI 3-kinase/mTOR (IC 50 values are 0.4, 1.6 and 5.4 nM for PI 3-K α , mTOR and PI 3-K γ respectively). Exhibits selectivity over 234 other protein kinases (IC 50 >10 μ M). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC 50 < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models.

Product References

Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate - Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate

Venkatesan AM, Dehnhardt CM, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham RT, Chaudhary I, Mansour TS. J Med Chem. 2010 Mar 25;53(6):2636-45.

Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. - Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor.

Mallon R, Feldberg LR, Lucas J, Chaudhary I, Dehnhardt C, Santos ED, Chen Z, dos Santos O, Ayral-Kaloustian S, Venkatesan A, Hollander I. Clin Cancer Res. 2011 May 15;17(10):3193-203.