Merck-22-6

Names

[ Name ]:
Merck-22-6

Biological Activity

[Description]:

Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Caspase

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[Target]

Akt1:138 nM (IC50)

Akt2:212 nM (IC50)

Akt3:7.2 mM (IC50)

Caspase-3

[In Vitro]

Akt1/Akt2-IN-2 (compound 7) 对 LnCaP，HT29，MCF7，A2780 细胞有细胞毒性[1]。 Akt1/Akt2-IN-2 (2 μM, 4 μM) 分别在2 μM和4 μM时，诱导 LnCaP 细胞中 caspase-3 的活性增加 3 倍或 6.6 倍[1]。

[References]

[1]. Zhao Z, et al. Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity. Bioorg Med Chem Lett. 2008 Jan 1;18(1):49-53.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₀H₄₃N₇O₂

[ Molecular Weight ]:
653.81500

[ Exact Mass ]:
653.34800

[ PSA ]:
102.90000

[ LogP ]:
7.44050

Synthetic Route

Click to get detail synthetic route

Related Compounds

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