MK-2206 2HCl
MK-2206 2HCl Basic information
- Product Name:
- MK-2206 2HCl
- Synonyms:
-
- MK-2206
- MK-2206 Dihydrochloride
- 8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
- MK 2206 2HCL;MK2206 2HCL
- CS-260
- MK2206; MK-2206; MK 2206; MK2206 DIHYDROCHLORIDE; MK2206 HCL.
- 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
- CAS:
- 1032350-13-2
- MF:
- C25H22ClN5O
- MW:
- 443.94
- Product Categories:
-
- Inhibitor
- PI3K/Akt/mTOR
- Inhibitors
- Akt
- mTOR
- PI3K
- Amines
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 1032350-13-2.mol
MK-2206 2HCl Chemical Properties
- 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.
MK-2206 2HCl Usage And Synthesis
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 vivo and leads to increased survival rates in mice bearing highly aggressive human lung tumors. Antitumor agents. Potent AKT inhibitor.
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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