GSK-690693 | Akt Inhibitor | AmBeed-信号通路专用抑制剂

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GSK-690693 {[allProObj[0].p_purity_real_show]}

货号：A111141

GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes.

GSK-690693 化学结构
CAS号：937174-76-0

GSK-690693 3D分子结构
CAS号：937174-76-0

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GSK-690693 纯度/质量文件产品仅供科研

货号：A111141 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

Akt 亚型比较

产品名称	Akt ↓ ↑	Akt1 ↓ ↑	Akt2 ↓ ↑	Akt3 ↓ ↑	其他靶点	纯度
Honokiol	✔				MEK	98%
PF-04691502	++++ P-Akt (S473), IC50: 3.8 nM P-Akt (T308), IC50: 7.5 nM					98+%
PHT-427	+ Akt, Ki: 2.7 μM					99%+
Deguelin	✔				PI3K	99%+
TIC10 isomer	✔				ERK	98+%
Perifosine	+ Akt, IC50: 4.7 μM					98%
Miltefosine	✔				PI3K,PKC	98%
Triciribine	+ Akt, IC50: 130 nM					99%+
Uprosertib		+ Akt1, IC50: 180 nM	+ Akt2, IC50: 328 nM	++ Akt3, IC50: 38 nM		99%+
Afuresertib		++++ Akt1, Ki: 0.08 nM	++++ Akt2, Ki: 2 nM	++++ Akt3, Ki: 2.6 nM		99%+
Miransertib		++++ Akt1, IC50: 5 nM	++++ Akt2, IC50: 4.5 nM	++ Akt3, IC50: 16 nM		98+%
GSK-690693		++++ Akt1, IC50: 2 nM	+++ Akt2, IC50: 13 nM	+++ Akt3, IC50: 9 nM		99%+
AT7867		++ Akt1, IC50: 32 nM	++ Akt2, IC50: 17 nM	++ Akt3, IC50: 47 nM	PKA	99%+
AKT inhibitor VIII		++ Akt1, IC50: 58 nM	+ Akt2, IC50: 210 nM	+ Akt3, IC50: 2119 nM		98+%
MK-2206 2HCl		+++ Akt1, IC50: 8 nM	+++ Akt2, IC50: 12 nM	+ Akt3, IC50: 65 nM		99%+
Ipatasertib		++++ Akt1, IC50: 5 nM	++ Akt2, IC50: 18 nM	+++ Akt3, IC50: 8 nM		99%+
AT13148		++ Akt1, IC50: 38 nM	+ Akt2, IC50: 402 nM	++ Akt3, IC50: 50 nM	PKA	98+%
Capivasertib		++++ Akt1, IC50: 3 nM	+++ Akt2, IC50: 8 nM	+++ Akt3, IC50: 8 nM		99%+
A-674563 HCl		+++ Akt1, Ki: 11 nM			PKA	98%
CCT128930			+++ Akt2, IC50: 6 nM		PKA	98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GSK-690693 生物活性

靶点	Akt3 Akt3, IC50:9 nM Akt1 Akt1, IC50:2 nM Akt2 Akt2, IC50:13 nM
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^[1]. GSK690693 is an ATP-competitive pan AKT inhibitor with IC50 values of 2, 13 and 9nM for AKT 1, 2, and 3, respectively. Treatment with GSK690693 on concentration of 0.01-10uM cause decreased phosphorylation level of GSK3, p70S6K, and PRAS40 in BT474 breast tumor cells in a dose-dependent manner. GSK690693 can induce accumulation of the FOXO3A, an Akt downstream substrate, in the nucleus at concentration >1uM. In growth inhibition studies, cell lines with higher level of p-AKT showed more sensitivity to GSK690693, such as HCC1954, ZR-75-1, BT474 and LNCaP, etc.. In vivo studies showed maximal tumor growth inhibition of 58% to 75% at the end of dosing period with 30mg/kg/day dose of GSK690693 (i.p.) for 21 days in mice bearing established SKOV-3 ovarian, LNCaP prostate, BT474 and HCC-1954 breast carcinoma xenografts^[2].
作用机制	GSK690693 is an ATP-competitive AKT inhibitor^[2].

GSK-690693 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HFF cells		Cytotoxic assay		Cytotoxicity against HFF cells, IC50=16.3 μM	18800763
human BT474 cells		Proliferation assay		Antiproliferative activity against human BT474 cells, IC50=50 nM	18800763
human LNCaP cells		Proliferation assay		Antiproliferative activity against human LNCaP cells, IC50=20 nM	18800763
human NCI-H460 cells		Growth inhibition assay	72 h	Growth inhibition of human NCI-H460 cells after 72 hrs by coulter counter method, IC50=5.4 μM	24900862

GSK-690693 动物研究

Dose

Mice^[3]: 30 mg/kg (i.p,)

Administration

i.p.

Pharmacokinetics

Animal	Rats^[4]	Dogs^[4]	Monkeys
Dose	10.6 mg/kg	4.2 mg/kg	4.3 mg/kg
Administration	i.v.	i.v.	i.v.
C_max	2.13 ± 0.19 μg/ml	1.30 ± 0.11 μg/ml	1.50 ± 0.10 μg/ml
T_1/2	8.92 ± 1.03 h	3.50 ± 0.33 h	5.52 ± 0.43 h
Protein binding (free drug %)	j
AUC_0→t	3.15 ± 0.32 (μg·h)/ml (0-inf)	2.01 ± 0.11 (μg·h)/ml (0-inf)	3.25 ± 0.67 (μg·h)/ml (0-inf)
CL	56.7 ± 5.5 (ml·min)/kg	34.6 ± 2.0 (ml·min)/kg	22.5 ± 4.3 (ml·min)/kg
Vss	15.2 ± 1.3 L/kg	5.29 ± 0.24 L/kg	6.54 ± 0.89 L/kg

GSK-690693 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00493818	Cancer	Phase 1	Terminated	-	United States, Indiana ... 展开 >> GSK Investigational Site Indianapolis, Indiana, United States, 46202 United States, Michigan GSK Investigational Site Detroit, Michigan, United States, 48201 United States, North Carolina GSK Investigational Site Durham, North Carolina, United States, 27710 收起 <<
NCT00666081	Cancer	Phase 1	Withdrawn(Study Cancelled befo... 展开 >>re enrollment) 收起 <<	December 2009	-

GSK-690693 参考文献

[1]Huck BR, Mochalkin I, et al. Recent progress towards clinically relevant ATP-competitive Akt inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2838-2848.

[2]Rhodes N, Heerding DA, et al. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res. 2008 Apr 1;68(7):2366-74.

[3]Altomare DA, Zhang L, et al. GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt. Clin Cancer Res. 2010 Jan 15;16(2):486-96.

[4]Heerding DA, Rhodes N, et al. Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J Med Chem. 2008 Sep 25;51(18):5663-79.

GSK-690693 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.75mL

2.35mL

1.18mL

23.50mL

4.70mL

2.35mL

GSK-690693 技术信息

CAS号	937174-76-0
分子式	C₂₁H₂₇N₇O₃
分子量	425.484

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 18 mg/mL(42.3 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 5 mg/mL(11.75 mM)，配合低频超声，并调节pH至5

动物实验配方

5% DMSO+40%PEG300+5% tween80+50% water 3 mg/mL

GSK-690693 {[allProObj[0].p_purity_real_show]}

GSK-690693 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GSK-690693 质控信息

GSK-690693 生物活性

GSK-690693 细胞研究

GSK-690693 动物研究

GSK-690693 临床研究

GSK-690693 参考文献

GSK-690693 实验方案

GSK-690693 技术信息

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GSK-690693 {[allProObj[0].p_purity_real_show]}

GSK-690693 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK-690693 质控信息

GSK-690693 生物活性

GSK-690693 细胞研究

GSK-690693 动物研究

GSK-690693 临床研究

GSK-690693 参考文献

GSK-690693 实验方案

GSK-690693 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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GSK-690693 纯度/质量文件产品仅供科研