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Submit ReviewMK 2206 dihydrochloride is a potent and selective allosteric Akt inhibitor (IC50 values are 5 nM, 12 nM, and 65 nM for Akt1, Akt2, and Akt3, respectively). MK 2206 requires the Pleckstrin homology domain for its activity, and exhibits no inhibitory activity in a panel of 250 tested protein kinases. MK 2206 induces growth inhibition of different cancer cell lines (IC50 in the range 3.4 and 28.6 μmol/L) and enhances antitumor efficacy of a range of standard chemotherapeutics. It synergistically inhibits cell proliferation of human lung and breast cancer cells in combination with Erlotinib (Cat. No. 7194) by suppressing both the Ras/Erk and PI 3-K pathways in vitro and in vivo. MK 2206 can be used to block the IL-22 - Akt signaling pathway for studying paneth cell differentiation.
分子量 | 480.39 |
公式 | C25H21N5O.2HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1032350-13-2 |
PubChem ID | 46930998 |
InChI Key | HWUHTJIKQZZBRA-UHFFFAOYSA-N |
Smiles | O=C1NN=C2C3=C(C=CN12)N=C(C4=CC=C(C5(CCC5)N)C=C4)C(C6=CC=CC=C6)=C3.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 24.02 | 50 |
以下数据基于产品分子量 480.39。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.16 mL | 20.82 mL | 41.63 mL |
2.5 mM | 0.83 mL | 4.16 mL | 8.33 mL |
5 mM | 0.42 mL | 2.08 mL | 4.16 mL |
25 mM | 0.08 mL | 0.42 mL | 0.83 mL |
参考文献是支持产品生物活性的出版物。
He et al (2022) Optimized human intestinal organoid model reveals interleukin-22-dependency of paneth cell formation. Cell Stem Cell 29 1333 PMID: 36002022
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 PMID: 20571069
Li et al (2009) Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. AACR Annual Meeting 69
If you know of a relevant reference for MK 2206 dihydrochloride, please let us know.
关键词: MK 2206 dihydrochloride, MK 2206 dihydrochloride supplier, MK2206, dihydrochloride, 2HCl, MK-2206, potent, selective, allosteric, AKT1, AKT2, AKT3, kinase, inhibitor, antitumor, Akt, (Protein, Kinase, B), 7850, Tocris Bioscience
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