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Apitolisib

Apitolisib

产品编号 T1916   CAS 1032754-93-0
别名: RG 7422, GNE 390, GDC-0980

Apitolisib (RG 7422) 是一种口服有效的 PI3K 和 mTOR(TORC1/2) 激酶抑制剂,抑制 PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ的活性,IC50值为 5 nM/27 nM/7 nM/14 nM,抑制 mTOR,Ki 为 17 nM。它用于乳腺癌、前列腺癌、肾细胞癌和子宫内膜癌等实体癌的试验研究 。

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Apitolisib Chemical Structure
Apitolisib, CAS 1032754-93-0
规格 价格/CNY 货期 数量
1 mg ¥ 359 现货
2 mg ¥ 517 现货
5 mg ¥ 913 现货
10 mg ¥ 1,330 现货
25 mg ¥ 2,370 现货
50 mg ¥ 3,820 现货
100 mg ¥ 5,520 现货
500 mg ¥ 11,300 现货
1 mL * 10 mM (in DMSO) ¥ 931 现货
产品目录号及名称: Apitolisib (T1916)
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纯度: 99.52%
纯度: 98.28%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.
靶点活性 p110α:5 nM, p110γ:14 nM, p110δ:7 nM
体外活性 在PC-3和MCF-7 neo/HER2异种移植模型中,GDC-0980(1 mg/kg)能够抑制肿瘤生长.在小鼠中,静脉给药 GDC-0980(1 mg/kg).
体内活性 在PC3(IC50=307 nM)和MCF7细胞(IC50=255 nM)中,GDC-0980明显抑制的细胞增殖。对于I类PI3K和mTOR激酶,GDC-0980的选择性抑制作用显著,对mTOR的(Ki=17 nM),对于PI3Kα(IC50=5 nM),β(IC50=27 nM),δ(IC50=7 nM),和γ(IC50=14 nM)。
激酶实验 Enzymatic activity: Enzymatic activity of the Class I PI3K isoforms is measured using a fluorescence polarization assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labeled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarization signal as the labeled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. PI3K isoforms are assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl2, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, 2% (v/v) DMSO at the following concentrations for each isoform: PI3Kα,β at 60 ng/mL; PI3Kγ at 8 ng/mL; PI3Kδ at 45 ng/mL. After assay for 30 minutes at 25°C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarization on an Envision plate reader. IC50s are calculated from the fit of the dose?response curves to a 4-parameter equation.Human recombinant mTOR(1360?2549) is expressed and purified from insect cells and assayed using a Lanthascreen fluorescence resonance energy transfer format in which phosphorylation of recombinant green fluorescent protein (GFP)-4-EBP1 is detected using a terbium-labeled antibody to phospho-threonine 37/46 of 4-EBP1. Reactions are initiated with ATP and conducted in the presence of 50 mM Hepes (pH 7.5), 0.25 nM mTOR, 400 nM GFP-4E-BP1, 8 μM ATP, 0.01% (v/v) Tween 20, 10 mM MnCl2, 1 mM EGTA, 1 mM dithiothreitol, and 1% (v/v) DMSO. Assays are conducted under initial rate conditions at room temperature for 30 minutes before terminating the reaction and detecting product in the presence of 2 nM Tb-anti-p4E-BP1 antibody and 10 mM EDTA.Dose?response curves are fit to an equation for competitive tight-binding inhibition and apparent Ki' s are calculated using the determined Km for ATP of 6.1 μM.
细胞实验 Antiproliferative cellular assays are conducted using PC3 and MCF7.1 human tumor cell lines. MCF7.1 is an in vivo selected line and originally derived from the parental human MCF7 breast cancer cell line. Cell lines are cultured in RPMI supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 μg/mL streptomycin, 10 mM HEPES, and 2 mM glutamine at 3°C under 5% CO2. MCF7.1 cells or PC3 cells are seeded in 384-well plates in media at 1000 cells/well or 3000 cells/well, respectively, and incubated overnight prior to the addition of GDC-0980 to a final DMSO concentration of 0.5% v/v. MCF7.1 cells and PC3 cells are incubated for 3 days and 4 days, respectively, prior to the addition of CellTiter-Glo reagen and reading of luminescence using an Analyst plate reader. For antiproliferative assays, a cytostatic agent such as aphidicolin and a cytotoxic agent such as staurosporine are included as controls. Dose?response curves are fit to a 4-parameter equation and relative IC50s are calculated using Assay Explorer software.(Only for Reference)
别名 RG 7422, GNE 390, GDC-0980
分子量 498.6
分子式 C23H30N8O3S
CAS No. 1032754-93-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 16 mg/mL (32.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0056 mL 10.0281 mL 20.0562 mL 50.1404 mL
5 mM 0.4011 mL 2.0056 mL 4.0112 mL 10.0281 mL
10 mM 0.2006 mL 1.0028 mL 2.0056 mL 5.014 mL
20 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.507 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Sutherlin DP, et al. J Med Chem, 2011, 54(21), 7579-7587. 2. Wallin JJ, et al. Mol Cancer Ther, 2011, 10(12), 2426-2436. 3. Makhov PB, et al. 2012. doi: 10.1158/1535-7163. MCT-11-0907.
Tetramethylcurcumin PROTAC-O4I2 Lexatumumab Pivanex Tubulin polymerization-IN-43 Moexipril hydrochloride AKT inhibitor VIII Ro-3306

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 抗癌细胞代谢库 抗肺癌化合物库 抗衰老化合物库 神经再生化合物库 糖酵解化合物库 抗癌化合物库 抗代谢疾病化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Apitolisib 1032754-93-0 Apoptosis PI3K/Akt/mTOR signaling PI3K mTOR GNE-390 RG 7422 inhibit GNE 390 GDC-0980 Inhibitor RG-7422 GDC0980 Phosphoinositide 3-kinase GNE390 GDC 0980 Mammalian target of Rapamycin RG7422 inhibitor

 

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