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Merck
CN

A6730

Akt1/2激酶抑制剂

≥98% (HPLC), Akt1/2 kinase inhibitor, powder

别名:

1,3-二氢-1-（1-（（4-（6-苯基-1H-咪唑[4,5-g）喹喔啉-7-基）苯基）甲基）-4-哌啶基）-2H-苯并咪唑-2-酮 三氟乙酸盐 水合物, Akti-1/2 三氟乙酸盐 水合物, Akt抑制剂八 三氟乙酸盐 水合物

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关于此项目

经验公式（希尔记法）:
C34H29N7O · xC2HF3O2 · yH2O
化学文摘社编号:
616871-83-1
分子量:
551.64 (anhydrous free base basis)
UNSPSC Code:
12352200
PubChem Substance ID:
24891133
NACRES:
NA.77
MDL number:
MFCD08705407

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产品名称

Akt1/2激酶抑制剂, ≥98% (HPLC)

SMILES string

[H]O[H].OC(=O)C(F)(F)F.O=C1Nc2ccccc2N1C3CCN(CC3)Cc4ccc(cc4)-c5nc6cc7nc[nH]c7cc6nc5-c8ccccc8

InChI

1S/C34H29N7O.C2HF3O2.H2O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33;3-2(4,5)1(6)7;/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42);(H,6,7);1H2

InChI key

CRRPFKCJZALCLQ-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

yellow

solubility

DMSO: ≥10 mg/mL

originator

Merck & Co., Inc., Kenilworth, NJ, U.S.

storage temp.

2-8°C

Quality Level

100

相关类别

Application

Akt在细胞增殖、凋亡、血管生成和糖尿病的信号转导途径中发挥作用。Akt1和Akt2双激酶抑制剂能够使肿瘤细胞对某些凋亡刺激敏感，并抑制体内Akt磷酸化。造血细胞中Akt1激酶的活性及其受细胞体内外信号因子的调节表明，AKT1的激活涉及激酶从胞质溶胶到膜的胞内易位。

Biochem/physiol Actions

Akt1/2激酶抑制剂；同工酶对Akt1有选择性。
同工酶选择性Akt1/2激酶抑制剂。在体外激酶试验中，Akt1/2激酶抑制剂显示IC50 = 58 nM、210 nM和2.12 mM，分别针对Akt1、Akt2和Akt3，抑制作用似乎是多重同源（酸碱度）结构域依赖性的，Akt1/2激酶抑制剂对酸碱度结构域缺失的Akts或其他密切相关的AGC家族激酶、PKA、PKC和SGK没有抑制作用，即使浓度高达50 & # 956；M.

Features and Benefits

该化合物由Merck & Co., Inc.（美国新泽西州Kenilworth）开发。想要浏览其他由制药公司开发的化合物以及已批准药物/候选药物清单， 请单击此处。
这种化合物是激酶磷酸酶生物学研究的特色产品。点击此处发现更多特色激酶磷酸酶生物产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000223096
0000223096
0000190470
0000190470
0000143305

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Jenny Sandström et al.
Archives of toxicology, 93(6), 1649-1664 (2019-04-18)
Brain susceptibility to a neurotoxic insult may be increased in a compromised health status, such as metabolic syndrome. Both metabolic syndrome and exposure to trimethyltin (TMT) are known to promote neurodegeneration. In combination the two factors may elicit additive or
X Zhang et al.
Leukemia research, 21(9), 849-856 (1997-12-11)
AKT1 is the human homolog of the v-akt oncogene. AKT1 has two distinct protein domains, one serine/threonine kinase domain and one pleckstrin homology (PH) domain. We studied the expression and activity of AKT1 in hematopoietic cell lines. The expression of
Zhijian Zhao et al.
Bioorganic & medicinal chemistry letters, 15(4), 905-909 (2005-02-03)
This letter describes the discovery of a novel series of dual Akt1/Akt2 kinase inhibitors, based on a 2,3,5-trisubstituted pyridine scaffold. Compounds from this series, which contain a 5-tetrazolyl moiety, exhibit more potent inhibition of Akt2 than Akt1.
Brad Larson et al.
Assay and drug development technologies, 7(6), 573-584 (2010-01-12)
Kinases continue to be one of the most important targets in today's drug discovery efforts. Following the identification of lead compounds through screening efforts, it is important to profile these leads against other kinases within that family, as well as
Vanessa Desplat et al.
Journal of enzyme inhibition and medicinal chemistry, 25(2), 204-215 (2010-03-13)
Attenuation of protein kinases by selective inhibitors is an extremely active field of activity in anticancer drug development. Therefore, Akt, a serine/threonine protein kinase, also known as protein kinase B (PKB), represents an attractive potential target for therapeutic intervention. Recent
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