GSK2636771

For research use only. Not for use in humans.

目录号:S8002

GSK2636771 Chemical Structure

CAS No. 1372540-25-4

GSK2636771是一种口服生物有效的PI3Kβ选择性抑制剂,其对PI3Kβ的选择性比对PI3Kα/PI3Kγ高900倍以上,比对PI3Kδ的选择性大10倍以上。对PTEN缺失细胞系敏感。

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客户使用Selleck生产的GSK2636771发表文献14篇:

客户使用该产品的4个实验数据:

  • Cells were treated as indicated. Medium and drug were refreshed every 2 to 3 days, and protein lysates were analyzed as above.

    Clin Cancer Res, 2017, 23(11):2795-2805. GSK2636771 purchased from Selleck.

  • PI3K inhibitor GSK2636771 demonstrated to be effective on ALL-SIL cells, showed an IC50 in the lower micromolar range.

    Dr. Antonino Maria Spartà from University of Bolog. GSK2636771 purchased from Selleck.

  • Effect of GSK2636771 on phosphorylation of Akt and integrin b1 in DU145 cells. Levels of p-integrin b1, integrin b1, p-Akt, Akt, and b-actin in DU145 cells treated with different concentrations of GSK2636771 were determined by Western blot analysis and quantified by ImageJ software.

    FASEB J, 2018, doi:10.1096/fj.201800183R. GSK2636771 purchased from Selleck.

  • Activity of LY2784544 and GSK2636771 at GPR39 and 11 additional understudied GPCRs.

    Mol Pharmacol, 2016, 90(6):726-737. GSK2636771 purchased from Selleck.

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 GSK2636771是一种口服生物有效的PI3Kβ选择性抑制剂,其对PI3Kβ的选择性比对PI3Kα/PI3Kγ高900倍以上,比对PI3Kδ的选择性大10倍以上。对PTEN缺失细胞系敏感。
靶点
PI3Kβ [1]
体外研究

GSK-2636771对PTEN缺失细胞系(人前列腺癌PC-3和乳腺癌HCC70)具有选择性抑制活性,EC50分别为36 nM 和 72 nM。[1]

体内研究 GSK-2636771处理这些移植瘤模型,降低磷酸化的蛋白激酶Akt(Ser473)水平。GSK-2636771(100 mg/kg) 处理小鼠,不增加葡萄糖/胰岛素水平。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[2]

- 合并
  • Cell lines: p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines.
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are plated in 96-well microtiter plates at densities ranging from 1,500 to 15,000 cells/well, optimized for untreated control cells to be 80-90% confluent at the endpoint of the experiment. After 24 h, cells are treated with serial dilutions (100pM to 10μM) of GSK2636771. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration requires for survival of 50% of cells relative to untreated cells (surviving fraction 50, SF50) is determined using GraphPad Prism version 5.0d. Cell lines that fails to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (i.e. 10μM). At least three independent experiments in triplicate per cell line targeted drug are performed. Association between a mutation and response to a targeted agent is determined using a Fisher’s exact test (GraphPad Prism), and a two-tailed P value <0.05 is considered statistically significant.


    (Only for Reference)
动物实验:

[3]

- 合并
  • Animal Models: Balb-c nude mice
  • Dosages: 100 mg/kg
  • Administration: oral administration
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 28 mg/mL (64.6 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 433.42
化学式

C22H22F3N3O3

CAS号 1372540-25-4
储存条件 粉状
溶于溶剂
别名 N/A

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Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03131908 Active not recruiting Drug: GSK2636771|Drug: Pembrolizumab Melanoma and Other Malignant Neoplasms of Skin|Metastatic Melanoma M.D. Anderson Cancer Center|National Cancer Institute (NCI)|National Institutes of Health (NIH)|Merck Sharp & Dohme Corp.|GlaxoSmithKline July 17 2017 Phase 1|Phase 2
NCT02215096 Completed Drug: GSK2636771|Drug: Enzalutamide Neoplasms GlaxoSmithKline November 13 2014 Phase 1
NCT01458067 Completed Drug: GSK2636771 Cancer GlaxoSmithKline November 10 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID