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Description: MK-2206 dihydrochloride (2HCl) is a novel, potent, orally bioavailable and highly selective allosteric inhibitor of the serine/threonine protein kinase Akt1/2/3 with potential anticancer activity. It inhibits Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; it has no/little inhibitory activities against 250 other protein kinases observed. MK-2206 has potential anticancer activity by inhibiting the phosphorylation of Thr308 and Ser 473 of Akt. MK-2206 suppresses Akt signalling pathway and promoting cancer cell death as a single agent as well as in combination with other chemotherapeutic agents. MK-2206 enhance the sensitivity to through apoptosis and enhance the sensitivity to rapamycin via reactive oxygen species.
Solubility: Soluble in DMSO (up to 10 mg/ml with warming)References: Mol Cancer Ther. 2010 Jul;9(7):1956-67; Cancer Res. 2011 Apr 1;71(7):2654-63.Related CAS: 1032349-77-1 (HCl); 1032350-13-2 (2HCl); 1032349-93-1 (free base);
Attribute [Chem Name] MK-2206 2HCl [Synonym] 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride; MK2206 diHCl; MK-2206; MK 2206; MK2206 dihydrochloride; MK2206 HCl; MK2206; [CAS No.] 1032350-13-2 [Formula] C25H21N5O.2HCl [Molecular] 480.39 [MDL No.] MFCD14584463 [Form] Yellow powder [Risk Codes] GHS07
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