NVP-BAG956

NVP-BAG956 is a dual inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1, IC50 = 245 nM) and class I phosphatidylinositol 3-kinase catalytic subunits (PI3Ks, IC50s = 56, 446, 35, and 117 nM for p110alpha, p110beta, p110delta, and p110gamma, respectively). It inhibits phosphorylation of T308-PKB (IC50 = 45 nM) in and proliferation of U87MG cells (EC50 = 143 nM). NVP-BAG956 decreases cell viability in a panel of human leukemia cell lines (IC50s = 1 phase in MOLM-14 cells and reduces colony formation by patient-derived acute myeloid leukemia (AML) cells. NVP-BAG956 (75 mg/kg) reduces tumor burden in mice injected with 32D.p210-luc+cells when administered in combination with everolimus (Cay-11597).Formal Name: alpha,alpha-dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile. CAS Number: 853910-02-8. Synonyms: BAG956. Molecular Formula: C28H21N5. Formula Weight: 427.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 20 mg/ml. SMILES: CC1=NC2=C(N1C3=CC=C(C(C)(C)C#N)C=C3)C4=CC(C#CC5=CC=CN=C5)=CC=C4N=C2. InChi Code: InChI=1S/C28H21N5/c1-19-32-26-17-31-25-13-8-20(6-7-21-5-4-14-30-16-21)15-24(25)27(26)33(19)23-11-9-22(10-12-23)28(2,3)18-29/h4-5,8-17H,1-3H3. InChi Key: GVPAGJWVBUZHNQ-UHFFFAOYSA-N.