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MK-2206 dihydrochloride 目录号 GC16304

Akt1/2/3 inhibitor

规格 价格 库存 购买数量
10mg
¥693.00
现货
50mg
¥1,649.00
现货
100mg
¥2,247.00
现货
500mg
¥9,020.00
现货
1g
¥16,233.00
现货

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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Cell experiment:[1]

Cell lines

Endometriotic stromal cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

100 nM, 2h

Applications

Inhibiting AKT with MK-2206 or MEK1/2 with U0126 for 24 hours in the absence of R5020 increased total and nuclear PRA and PRB protein levels in OSIS but not in eutopic endometrial stromal cells from disease-free patients from disease-free patients. MK-2206 and R5020 decreased OSIS viability and increased apoptosis. Trends toward decreased volumes of sc grafted endometriosis tissues were demonstrated with MK-2206 and progesterone.

Animal experiment:[1]

Animal models

5-week-old CD-1 nude mice

Dosage form

360 mg/kg/d, 15 days, oral Gavage

Applications

No significant interaction between MK-2206 and progesterone (P=0.628). Trends toward decreased tumor volume were noted with MK-2206 (P=0.077) and progesterone (P=0.087). Treatment with MK-2206 decreased levels of Ki67. Levels of cleaved caspase-3 (CC3) were very low in E and E +P-treated grafts, whereas MK-2206 increased CC3 levels, especially in the presence of P.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Eaton JL1, Unno K, Caraveo M et al. Increased AKT or MEK1/2 activity influences progesterone receptor levels and localization in endometriosis. J Clin Endocrinol Metab. 2013 Dec;98(12):E1871-9.

MK-2206 dihydrochloride Dilution Calculator

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化学数据

Cas No. 1032350-13-2 SDF
别名 MK-2206,MK2206,MK 2206
化学名 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride
Canonical SMILES C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
分子式 C25H21N5O.2HCl 分子量 480.39
溶解度 ≥12.01mg/mL in DMSO 储存条件 Store at -20°C
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。溶液形式可以在-20℃下储存几个月。
运输条件 所有可选规格:常温运输或根据产品储存温度要求用蓝冰运输。

产品描述

MK-2206 dihydrochloride is a selective inhibitor of Akt1/2/3. MK-2206 inhibites the phosphorylation of Thr308 and Ser 473 of Akt. MK-2206 suppresses Akt signalling pathway and promoting cancer cell death as a single agent as well as in combination with other chemotherapeutic agents. MK-2206 enhance the sensitivity to through apoptosis and enhance the sensitivity to rapamycin via reactive oxygen species. Combination of MK-2206 with etoposide or rapamycin significantly increase antitumor growth effect.

References
1. Pant A, Lee II, Lu Z, Rueda BR, Schink J, Kim JJ.Inhibition of AKT with the Orally Active Allosteric AKT Inhibitor, MK-2206, Sensitizes Endometrial Cancer Cells to Progestin.PLoS One. 2012;7(7):e41593. Epub 2012 Jul 24.
2. First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors. TA Yap, L Yan, A Patnaik, I Fearen.  Journal of Clinical Oncology  2011