MK-2206 (hydrochloride)

无

An allosteric Akt inhibitor

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.1,2 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).3 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.3 At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.4

480.4

≥98%

8-[4-(1-氨基环丁基)苯基]-9-苯基-1,2,4-三唑并[3,4-F][1,6]萘啶-3(2H)-酮二盐酸盐≥98%，杂质≤2%

NC1(CCC1)C(C=C2)=CC=C2C(C(C3=CC=CC=C3)=C4)=NC5=C4C(N6C=C5)=NNC6=O.Cl.Cl

C25H21N5O • 2HCl

1032350-13-2

≥ 4 years

DMF: 0.2 mg/ml DMF:PBS (pH 7.2)(1:3): 0.2 mg/ml DMSO: 2 mg/ml

1.Manning, B.D. and Cantley, L.C. AKT/PKB signaling: Navigating downstream. Cell 129, 1261-1274 (2007).
2.Yuan, T.L. and Cantley, L.C. PI3K pathway alterations in cancer: Variations on a theme. Oncogene 27(41), 5497-5510 (2008).
3.Hirai, H.,Sootome, H.,Nakatsuru, Y., et al. MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo. Molecular Cancer Therapeutics 9(7), 1956-1967 (2010).
4.Kurosu, T.,Nagao, T.,Wu, N., et al. Inhibition of the PI3K/Akt/GSK3 pathway downstream of BCR/ABL, Jak2-V617F, or FLT3-ITD downregulates DNA damage-induced Chk1 activation as well as G₂/M arrest and prominently enhances induction of apoptosis. PLoS One 8(11), (2013).