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CAS No.: 1047645-82-8

Afuresertib HCl Catalog No. CSN15693

Synonyms: GSK2110183 hydrochloride;GSK-2110183 HCl;Afuresertib (hydrochloride)

Afuresertib HCl is a potent pan-Akt inhibitor with Ki values of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Akt2

Ki:2nM Akt3

Ki:2.6nM Akt1

Ki:0.08nM
描述Akt (protein kinase B) is a master regulator of cell survival in response to growth factors. In human cancers, Akt plays a pivotal role in cell growth, apoptosis inhibition, protein synthesis, and glucose and fatty acid metabolism by phosphorylating its substrates, including CDK2, FOXO, GSK-3beta, S6 kinase, and mTOR^[2]. Afuresertib, a thiophenecarboxamide derivative, is a catalytic ATP‐competitive inhibitor of AKT1, AKT2, AKT3 with Ki values of 0.08 nM, 2 nM, and 2.6 nM^[3]. Afuresertib, an ATP‐competitive specific Akt inhibitor, exerted tumor‐specific effects on MPM cells. Afuresertib significantly increased caspase‐3 and caspase‐7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Moreover, Afuresertib strongly arrested the cell cycle in the G1 phase^[2]. Cells treated with Afuresertib show decreased phosphorylation of several substrates downstream of AKT. Afuresertib at 5 μmol/L for 24h clearly suppressed the migration of ACC-MESO-4 and MSTO-211H cells^[3]. In a phase IIa study of Afuresertib, patients were treated with oral Afuresertib (125 mg/d) for over 28 weeks, it was showed that Afuresertib had clinical activity in some patients with newly diagnosed and advanced LCH^[4].
动物研究
剂量
Mice: 10 mg/kg - 100 mg/kg^[1] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 10 mg/kg - 100 mg/kg^[1] (p.o.)
给药途径	p.o.

[1] Dumble M, Crouthamel MC, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880.
[2] Yamaji M, Ota A, Wahiduzzaman M, Karnan S, Hyodo T, Konishi H, Tsuzuki S, Hosokawa Y, Haniuda M. Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. doi: 10.1002/cam4.1179. Epub 2017 Sep 27. PMID: 28960945; PMCID: PMC5673922.
[3] Dumble M, Crouthamel MC, Zhang SY, Schaber M, Levy D, Robell K, Liu Q, Figueroa DJ, Minthorn EA, Seefeld MA, Rouse MB, Rabindran SK, Heerding DA, Kumar R. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880. doi: 10.1371/journal.pone.0100880. PMID: 24978597; PMCID: PMC4076210.
[4] Arceci RJ, Allen CE, Dunkel IJ, Jacobsen E, Whitlock J, Vassallo R, Morris SR, Portnoy A, Reedy BA, Smith DA, Noble R, Murnane A, Cornfeld M, Rodriguez-Galindo C, Heaney ML, McClain K, Vaiselbuh S. A phase IIa study of afuresertib, an oral pan-AKT inhibitor, in patients with Langerhans cell histiocytosis. Pediatr Blood Cancer. 2017 May;64(5). doi: 10.1002/pbc.26325. Epub 2016 Nov 2. PMID: 27804235.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1562 mL
- 10.7809 mL
- 21.5618 mL
- 5 mM
- 0.4312 mL
- 2.1562 mL
- 4.3124 mL
- 10 mM
- 0.2156 mL
- 1.0781 mL
- 2.1562 mL

技术信息

CAS号

1047645-82-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H18Cl3FN4OS

运输

蓝冰

分子量

463.78

别名

GSK2110183 hydrochloride;GSK-2110183 HCl;Afuresertib (hydrochloride);GSK-2110183;Afuresertib;Afuresertib HCl

溶解度

DMSO	52.0 mg/mL (112.1 mM)

动物实验配方

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靶点	Description	IC50
Akt2		Ki:2nM
Akt3		Ki:2.6nM
Akt1		Ki:0.08nM

Afuresertib HCl Catalog No. CSN15693

靶点选择性

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