NVP-BGT226

NVP-BGT226 is an orally bioavailable dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR). It inhibits class I PI3Ks with EC50 values of 4, 63, and 38 nM for PI3Kalpha, beta, and gamma isoforms, respectively, in a filter binding assay. It binds to both class I and class III PI3Ks in a quantitative ELISA assay with EC50 values of 55.8 and 7.03 nM, for HsPI3Kbeta and HsVps34, respectively. It decreases protein levels of phosphorylated mTOR and Akt, a downstream target of PI3K signaling. NVP-BGT226 inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (Cay-13119) with IC50 values of 7.4-27.8, 22.6, and 30.1 nM, respectively. It halts the cell cycle at the G0/G1 phase and induces autophagy. NVP-BGT226 (2.5 and 5 mg/kg daily for three weeks) inhibits tumor growth in a FaDu head and neck cancer mouse xenograft model.Formal Name: 1,3-dihydro-8-(6-methoxy-3-pyridinyl)-3-methyl-1-[4-(1-piperazinyl)-3-(trifluoromethyl)phenyl]-2H-imidazo[4,5-c]quinolin-2-one, (2Z)-2-butenedioate. CAS Number: 1245537-68-1. Molecular Formula: C28H25F3N6O2 . C4H4O4. Formula Weight: 650.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml. lambdamax: 273 nm. SMILES: COC(N=C1)=CC=C1C2=CC3=C(C=C2)N=CC4=C3N(C5=CC=C(N6CCNCC6)C(C(F)(F)F)=C5)C(N4C)=O.OC(/C=C\C(O)=O)=O. InChi Code: InChI=1S/C28H25F3N6O2.C4H4O4/c1-35-24-16-33-22-6-3-17(18-4-8-25(39-2)34-15-18)13-20(22)26(24)37(27(35)38)19-5-7-23(21(14-19)28(29,30)31)36-11-9-32-10-12-36,5-3(6)1-2-4(7)8/h3-8,13-16,32H,9-12H2,1-2H3,1-2H,(H,5,6)(H,7,8)/b,2-1-. InChi Key: YUXMAKUNSXIEKN-BTJKTKAUSA-N.