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GSK-690693
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK-690693图片
CAS NO:937174-76-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
GSK-690693 是一种 ATP 竞争型的泛Akt抑制剂,对Akt1Akt2Akt3IC50分别为 2 nM,13 nM,9 nM。GSK-690693 也是一种AMPK的抑制剂,影响 ULK1 的活性,并能显著抑制 STING 依赖的 IRF3 的激活。
生物活性

GSK-690693 is an ATP-competitivepan-Aktinhibitor withIC50s of 2 nM, 13 nM, 9 nM forAkt1,Akt2andAkt3, respectively. GSK-690693 is also anAMPKinhibitor, affects Unc-51-likeautophagyactivating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation[1][2][3].

IC50& Target[1]

Akt1

2 nM (IC50)

Akt3

9 nM (IC50)

Akt2

13 nM (IC50)

PKCη

2 nM (IC50)

PKCθ

2 nM (IC50)

PrkX

5 nM (IC50)

PAK6

6 nM (IC50)

PAK4

10 nM (IC50)

PKCδ

14 nM (IC50)

PKCβ1

19 nM (IC50)

PKCε

21 nM (IC50)

PKA

24 nM (IC50)

PKG1β

33 nM (IC50)

AMPK

50 nM (IC50)

PAK5

52 nM (IC50)

DAPK3

81 nM (IC50)

Autophagy

 

体外研究
(In Vitro)

GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations >100 nM in both LNCaP and BT474 cells[1]. Consistent with the role of AKT in cell survival, GSK690693 induces apoptosis in sensitive ALL cell lines[2].

体内研究
(In Vivo)

A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day[1]. GSK690693 exhibits efficacy irrespective of the mechanism of Akt activation involved. GSK690693 is most effective in delaying tumor progression in Lck-MyrAkt2 mice expressing a membrane-bound, constitutively active form of Akt[3].

Clinical Trial
分子量

425.48

性状

Solid

Formula

C21H27N7O3

CAS 号

937174-76-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 20 mg/mL(47.01 mM;ultrasonic and warming and heat to 60℃)

H2O : 5 mg/mL(11.75 mM;ultrasonic and adjust pH to 5 with HCl)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3503 mL11.7514 mL23.5029 mL
5 mM0.4701 mL2.3503 mL4.7006 mL
10 mM0.2350 mL1.1751 mL2.3503 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 20%HP-β-CD/10 mM citrate pH 2.0

    Solubility: 10 mg/mL (23.50 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.88 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: 2 mg/mL (4.70 mM); Clear solution; Need ultrasonic

    此方案可获得 2 mg/mL (4.70 mM) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2 mg/mL (4.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2 mg/mL (4.70 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。