Home>>Signaling Pathways>> PI3K/Akt/mTOR Signaling>> PDK-1>>GSK2334470

GSK2334470 Sale

目录号 : GC12275

A selective PDK1 inhibitor

GSK2334470 Chemical Structure

Cas No.:1227911-45-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥893.00
现货
10mg
¥756.00
现货
25mg
¥1,502.00
现货
50mg
¥2,289.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

U87 cells and fibroblasts

Preparation method

The solubility of this compound in DMSO is >23.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

3 μM, 1 μM

Applications

In U87 glioblastoma cells that lack PTEN expression, GSK2334470 (3μM) only partially inhibited Thr308 phosphorylation or Akt activation ~3-fold. GSK2334470 (1 μM) effectively inhibited SGK1 activity. In MEF (mouse embryonic fibroblast) cells, 1 μM GSK2334470 inhibited Akt Thr308 phosphorylation and activity, and also inhibited activation of S6K1 as well as SGK1.

Animal experiment [2]:

Animal models

MM xenograft model established in immunodeficient mice

Dosage form

5 days of GSK-470 (40 mg/kg/d), 5 days of PP242 (20 mg/kg/d), or 5 days of GSK-470 combined with PP242; intraperitoneal injection; once every day

Application

In multiple myeloma xenograft immunodeficient mice, compared with untreated mice, GSK-470 (GSK2334470) or PP242 produced a modest tumor volume reduction. Combination treatment with GSK-470 and PP242 significantly inhibited tumor growth.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Najafov A, Sommer E, Axten J, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem. J, 2011, 433: 357-369.

[2]. Yang C, Huang X, Liu H, et al. PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242. Oncotarget. 2017 Jun 13;8(24):39185-39197.

产品描述

GSK2334470 is a highly specific inhibitor of 3-phosphoinositide-dependent protein kinase 1(PDK1) with IC50 value of ~10nM [1].

GSK2334470 prevents PDK1 from activating full-length Akt1or mutant Akt1 lacking the PH domain. It also inhibits phosphorylation of the PDKtide peptide substrate. GSK2334470 shows no significant inhibitory effect on 93 other protein kinases (including 13 AGC-kinases) and 15 lipid kinases. GSK2334470 markedly inhibits the IGF1-induced T-loop phosphorylation of SGK1, SGK2 and SGK3 overexpressed in HEK293 cells. GSK2334470 is also reported to suppress the activity of S6K1. It inhibits the phosphorylation of both hydrophobic motif and T-loop of S6K1. To Akt1, GSK2334470 exerts same effects on the phosphorylation of T-loop but has no significant inhibition of hydrophobic motif phosphorylation. In PDK1K465E/K465E knock-in ES cells, GSK2334470 is more potent to inhibit Akt activation than in PDK1+/+ ES cells. Moreover, the inhibition of Akt activation shows to recede in U87 glioblastoma cells lack PTEN expression [1].

References:
[1] Najafov A, Sommer E, Axten J, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem. J, 2011, 433: 357-369.

Chemical Properties

Cas No. 1227911-45-6 SDF
化学名 (3S,6R)-1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl]-N-cyclohexyl-6-methylpiperidine-3-carboxamide
Canonical SMILES CC1CCC(CN1C2=NC(=NC(=C2)C3=CC4=C(C=C3)C(=NN4)N)NC)C(=O)NC5CCCCC5
分子式 C25H34N8O 分子量 462.59
溶解度 ≥ 46.3mg/mL in DMSO 储存条件 Store at -20°C
General tips 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.1617 mL 10.8087 mL 21.6174 mL
5 mM 0.4323 mL 2.1617 mL 4.3235 mL
10 mM 0.2162 mL 1.0809 mL 2.1617 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置