- MK-2206 2HCl
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- $30.00
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2023-09-07
- CAS:1032350-13-2
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 1000t/year
- MK-2206 2HCl
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- $2.00
-
2019-07-06
- CAS:1032350-13-2
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 100kg
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| | MK-2206 2HCl Basic information |
| Product Name: | MK-2206 2HCl | | Synonyms: | 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;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 | | CAS: | 1032350-13-2 | | MF: | C25H22ClN5O | | MW: | 443.94 | | EINECS: | | | 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. | | InChIKey | LFYOZCBFOSSLNJ-UHFFFAOYSA-N | | SMILES | O=C1NN=C2C3=CC(C4C=CC=CC=4)=C(C4C=CC(C5(CCC5)N)=CC=4)N=C3C=CN12.Cl |
| | 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 thein vitroandin vivoantitumor efficacy of several standard chemotherapeutic agents.1It was able to decrease insulin-stimulated glucose uptake, glycogen synthesis and glycogen synthase activity in rat muscle.2MK-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] HIROSHI HIRAI. MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo.[J]. Molecular Cancer Therapeutics, 2010, 9 7: 1956-1967. DOI:10.1158/1535-7163.mct-09-1012
[2] YU-CHIANG LAI. A novel PKB/Akt inhibitor, MK-2206, effectively inhibits insulin-stimulated glucose metabolism and protein synthesis in isolated rat skeletal muscle.[J]. Biochemical Journal, 2012, 447 1: 137-147. DOI:10.1042/bj20120772
[3] PENG JIAO. MK-2206 induces cell cycle arrest and apoptosis in HepG2 cells and sensitizes TRAIL-mediated cell death.[J]. Molecular and Cellular Biochemistry, 2013, 382 1-2: 217-224. DOI:10.1007/s11010-013-1737-0 |
| | MK-2206 2HCl Preparation Products And Raw materials |
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