PF-05212384

Phosphatidylinositol-3-kinases (PI3Ks) act in concert with mTOR complexes to regulate signaling pathways that have critical roles in cancer and other diseases. PF-05212384 is a potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kalpha and PI3Kgamma, respectively, and 1.6 nM for mTOR). It is active both in vitro and in vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously. PF-05212384 blocks the proliferation of liver cancer stem cells, and this effect is enhanced in combination therapy with the multikinase inhibitor BAY-43-9006 (Cay-10009644). PF-05212384 action also enhances the effectiveness of cetuximab or radiation therapy in human head and neck cancer models.Formal Name: N-[4-[[4-(dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]-urea. CAS Number: 1197160-78-3. Synonyms: PK-1587, PKI-587. Molecular Formula: C32H41N9O4. Formula Weight: 615.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1.5 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 1 mg/ml. lambdamax: 228, 303 nm. SMILES: O=C(N1CCC(N(C)C)CC1)C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=NC(N6CCOCC6)=N4)C=C3)=O)C=C2. InChi Code: InChI=1S/C32H41N9O4/c1-38(2)27-11-13-39(14-12-27)29(42)24-5-9-26(10-6-24)34-32(43)33-25-7-3-23(4-8-25)28-35-30(40-15-19-44-20-16-40)37-31(36-28)41-17-21-45-22-18-41/h3-10,27H,11-22H2,1-2H3,(H2,33,34,43). InChi Key: DWZAEMINVBZMHQ-UHFFFAOYSA-N.