MK-2206 (hydrochloride)

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBalpha, beta, gamma) modulate cell proliferation, metabolism, and survival as well as angiogenesis. MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM). In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines. At 5 µM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.Formal Name: 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one, dihydrochloride. CAS Number: 1032350-13-2. Molecular Formula: C25H21N5O . 2HCl. Formula Weight: 480.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.2 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.2 mg/ml, DMSO: 2 mg/ml. lambdamax: 210, 257, 357 nm. SMILES: NC1(CCC1)C(C=C2)=CC=C2C(C(C3=CC=CC=C3)=C4)=NC5=C4C(N6C=C5)=NNC6=O.Cl.Cl. InChi Code: InChI=1S/C25H21N5O.2ClH/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31,,/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31),2*1H. InChi Key: HWUHTJIKQZZBRA-UHFFFAOYSA-N.