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CAS No.: 1047644-62-1

Afuresertib Catalog No. CSN17427

Synonyms: GSK2110183

Afuresertib is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively.

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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 Akt1

Ki:0.08nM Akt2

Ki:2nM Akt3

Ki:2.6nM
描述AKT is the central node of PI3K/AKT/mTOR pathway. The PH domain and ATP-competitive site are the main target site for research of new compound^[2]. Afuresertib （GSK2110183） is an ATP-competitive inhibitor of AKT1/2/3 with Ki value of 0.08nM, 2nM and 2.6nM (measured by a filter binding assay), respectively. Treatment of Afuresertib on concentration of 1-10uM can induce G1-arrest and decrease the phosphorylation level of multiple AKT substrate including PRAS40, FOXO and Caspase 9 in BT474 and LNCaP cell lines in a concentration-dependent manner, accompanied by feedback increase in AKT phosphorylation. Afuresertib has more potent anti-proliferative effects on a variety of hematological malignancies (65% were sensitive to Afuresertib with EC50<1uM)). Among solid tumor cell lines, 21% had EC50<1uM in response to Afuresertib. Treatment with Afuresertib at 10, 30 and 100mg/kg, daily for 7 days, can decrease PRAS40 phosphorylation by 8%, 37% and 61% in mice bearing BT474 tumors, which showed the good pharmacodynamics of Afuresertib^[1]. Single-agent Afuresertib shows clinical activity against hematologic malignancies, including multiple myeloma^[3].
作用机制Afuresertib is an ATP-competitive AKT inhibitor.^[1]
动物研究
剂量
Mice: min = 10 mg/kg, max = 100 mg/kg^[1]

给药途径
p.o.
临床研究

动物研究
剂量	Mice: min = 10 mg/kg, max = 100 mg/kg^[1]
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02040480	Cancer	Phase 1	Completed	-	Australia, New South Wales ... more >> GSK Investigational Site Randwick, New South Wales, Australia, 2031 Collapse <<
NCT02380313	Cancer	Phase 1	Withdrawn(Study cancelled With... more >>drawn before enrollment of any participants) Collapse <<	May 2017	-
NCT01827644	Cancer	Phase 1	Completed	-	Australia, Victoria ... more >> GSK Investigational Site Melbourne, Victoria, Australia, 3004 Collapse <<

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
- 2.3401 mL
- 11.7007 mL
- 23.4015 mL
- 5 mM
- 0.4680 mL
- 2.3401 mL
- 4.6803 mL
- 10 mM
- 0.2340 mL
- 1.1701 mL
- 2.3401 mL

技术信息

CAS号

1047644-62-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H17Cl2FN4OS

运输

蓝冰

分子量

427.32

别名

GSK2110183

溶解度

DMSO	50.0 mg/mL (117.0 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02040480	Cancer	Phase 1	Completed	-	Australia, New South Wales ... more >> GSK Investigational Site Randwick, New South Wales, Australia, 2031 Collapse <<
NCT02380313	Cancer	Phase 1	Withdrawn(Study cancelled With... more >>drawn before enrollment of any participants) Collapse <<	May 2017	-
NCT01827644	Cancer	Phase 1	Completed	-	Australia, Victoria ... more >> GSK Investigational Site Melbourne, Victoria, Australia, 3004 Collapse <<
NCT02240212	Cancer	Phase 1	Completed	-	Korea, Republic of ... more >> Novartis Investigative Site Seoul, Korea, Republic of, 110-774 Novartis Investigative Site Seoul, Korea, Republic of, 120/752 Novartis Investigative Site Seoul, Korea, Republic of, 135-710 Taiwan Novartis Investigative Site Taipei, Taiwan, 100 Novartis Investigative Site Taipei, Taiwan, 112 Collapse <<
NCT02177682	Neoplasms, Haematologic	Phase 1	Active, not recruiting	December 28, 2018	Japan ... more >> Novartis Investigative Site Aichi, Japan, 467-8602 Novartis Investigative Site Fukuoka, Japan, 811-1395 Novartis Investigative Site Miyagi, Japan, 980-8574 Novartis Investigative Site Niigata, Japan, 951-8566 Novartis Investigative Site Tokyo, Japan, 104-0045 Collapse <<
NCT02235740	Cancer	Phase 1	Terminated	-	United States, North Carolina ... more >> Novartis Investigative Site Cary, North Carolina, United States, 27518 Collapse <<

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

Afuresertib Catalog No. CSN17427

靶点选择性

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