| Identification | Back Directory | [Name]
MK-2206 2HCl | [CAS]
1032350-13-2 | [Synonyms]
MK-2206
MK-2206 2HCl
MK-2206 Dihydrochloride
MK 2206 (hydrochloride)
8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one
8-[4-(1-AMinocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one Hydrochloride
8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride MK-2206
MK-2206 8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride | [Molecular Formula]
C25H21N5O | [MDL Number]
MFCD14584463 | [MOL File]
1032350-13-2.mol | [Molecular Weight]
407.467 |
| Chemical Properties | Back Directory | [Melting point ]
>255°C (dec.) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 10 mg/ml with warming) | [form ]
Yellow powder. | [color ]
Yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Usage]
A highly selective inhibitor of Akt. Akt1, IC50=8 nM; Akt2, IC50=12 nM; Akt3, IC50=65 nM. | [Usage]
AZD 6244 and MK 2206 are targeted small-molecule drugs that inhibit MEK and AKT responses. The combination of AZD6244 and MK2206 has a significant synergistic effect on tumor growth in vitro and in vi
vo and leads to increased survival rates in mice bearing highly aggressive human lung tumors. Antitumor agents. | [Description]
MK-2206 (CAS 1032350-13-2) is a potent and selective allosteric inhibitor of Akt (IC50’s: Akt1 = 5 nM, Akt2 = 12 nM, Akt3 = 65 nM) that enhances the?in vitro?and?in vivo?antitumor efficacy of several standard chemotherapeutic agents.1?It was able to decrease insulin-stimulated glucose uptake, glycogen synthesis and glycogen synthase activity in rat muscle.2?MK-2206 induced G1-phase cycle arrest and sensitized HepG2 hepatocellular carcinoma cells to TRAIL-induced apoptosis.3 | [Uses]
A highly selective inhibitor of Akt. Akt1, IC50=8 nM; Akt2, IC50=12 nM; Akt3, IC50=65 nM. | [Uses]
AZD 6244 and MK 2206 are targeted small-molecule drugs that inhibit MEK and AKT responses. The combination of AZD6244 and MK2206 has a significant synergistic effect on tumor growth in vitro and in vi
vo and leads to increased survival rates in mice bearing highly aggressive human lung tumors. Antitumor agents. | [in vivo]
Both MK-2206 dihydrochloride (MK-2206 (2HCl)) doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. No other obvious toxicity is observed in mice[2].
MK-2206 dihydrochloride (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth in 3-5 week old athymic nude mice with GEO colon carcinoma cells[3].
| Animal Model: | Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts[2] | | Dosage: | 240 mg/kg and 480 mg/kg | | Administration: | Oral gavage; 240 mg/kg for three times a week; 480 mg/kg for once a week; for 2 weeks | | Result: | Both doses inhibited the growth of human CNE-2 xenografts in nude mice. |
| [target]
Akt1 | [IC 50]
Akt1: 8 nM (IC50); Akt2: 12 nM (IC50); Akt3: 65 nM (IC50) | [storage]
-20°C | [References]
1) Hirai?et al.?(2010),?MK-2206, an Allosteric Akt inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular targeted Drugs In vitro and In vivo; Mol. Cancer Ther.?9?1956
2) Lai?et al.?(2012),?A novel PKB/Akt inhibitor, MK-2206, effectively inhibits insulin-stimulated glucose metabolism and protein synthesis in isolated rat skeletal muscle; Biochem. J.?447?137
3) Jiao?et al.?(2013),?MK-2206 induces cell cycle arrest and apoptosis in HepG2 cells and sensitizes TRAIL-mediated cell death; Mol. Cell Biochem.?382?217 |
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