MK-2206 dihydrochloride
(HB5934)
Product overview
Name | MK-2206 dihydrochloride |
Description | Highly selective, pan-Akt inhibitor. Autophagy and apoptosis inducer. Orally bioavailable. |
Alternative names | MK-2206 2HCl |
Purity | >98% |
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Biological Data
Biological description | Highly selective, allosteric pan-Akt inhibitor (IC50 values are 8, 12 and 65 nM at Akt1, Akt2 and Akt3 respectively) which shows no inhibitory activity at 250 other protein kinases. Orally bioavailable and blood brain barrier permeable. Binds to Akt and inhibits it in a non-ATP competitive manner. Shows anti-cancer (antineoplastic) antiproliferative and anti-tumor activity. Synergistically inhibits cell proliferation of human cancer cell lines to enhance anti-tumor efficacy when used in combination with other anticancer agents. Induces cell cycle arrest, autophagy and apoptosis. |
Solubility & Handling
Storage instructions | -20°C |
Solubility overview | Soluble in DMSO (100 mM) |
Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use |
Chemical Data
Purity | >98% |
Chemical name | 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride |
Molecular Weight | 480.4 |
Chemical structure | |
Molecular Formula | C25H21N5O.2HCl |
CAS Number | 1032350-13-2 |
PubChem identifier | 46930998 |
SMILES | C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl |
InChi | 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 |
InChiKey | HWUHTJIKQZZBRA-UHFFFAOYSA-N |
References for MK-2206 dihydrochloride
References are publications that support the biological activity of the product
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eEF-2 kinase dictates cross-talk between autophagy and apoptosis induced by Akt Inhibition, thereby modulating cytotoxicity of novel Akt inhibitor MK-2206.
Cheng Y et al (2011) Cancer research 71 : 2654-63 -
MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo.
Hirai H et al (2010) Molecular cancer therapeutics 9 : 1956-67 -
Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor
Yan Li (2009) New Drugs on the Horizon 1 69 : 9_supplement