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Merck
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文件

A6730

Sigma-Aldrich

Akt1/2激酶抑制剂

≥98% (HPLC)

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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About This Item

经验公式（希尔记法）:
C34H29N7O · xC2HF3O2 · yH2O
CAS号:
616871-83-1
分子量:
551.64 (anhydrous free base basis)
MDL號碼:
MFCD08705407
分類程式碼代碼:
12352200
PubChem物質ID:
24891133
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

yellow

溶解度

DMSO: ≥10 mg/mL

起源

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

儲存溫度

2-8°C

SMILES 字串

[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 密鑰

CRRPFKCJZALCLQ-UHFFFAOYSA-N

應用

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。

生化／生理作用

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.

特點和優勢

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析证书(COA)

输入产品批号来搜索 分析证书(COA) 。批号可以在产品标签上"批“ （Lot或Batch）字后找到。

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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
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
Bo Hu et al.
Journal of Cancer, 10(17), 3914-3925 (2019-08-17)
Sorafenib, a multikinase inhibitor, is a new standard treatment for patients with advanced hepatocellular carcinoma (HCC). However, resistance to this regimen is frequently observed in clinical practice, and the molecular basis of this resistance remains largely unknown. Herein, the antitumor
Z Lu et al.
Cell death and differentiation, 21(8), 1275-1289 (2014-04-29)
The process of autophagy has been described in detail at the molecular level in normal cells, but less is known of its regulation in cancer cells. Aplasia Ras homolog member I (ARHI; DIRAS3) is an imprinted tumor suppressor gene that
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.
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