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Omipalisib

产品编号 T1861 CAS 1086062-66-9

别名: GSK458, GSK2126458

Omipalisib (GSK2126458) 是一种磷脂酰肌醇 3-激酶(PI3K) 的小分子吡啶磺酰胺抑制剂，具有抗肿瘤活性。它抑制 p110α/β/δ/γ，mTORC1/2 的活性，Ki 值分别为 0.019 nM/0.13 nM/0.024 nM/0.06 nM 和 0.18 nM/0.3 nM。

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Omipalisib, CAS 1086062-66-9

规格	价格/CNY	货期
1 mg	￥ 179	现货
5 mg	￥ 398	现货
10 mg	￥ 657	现货
25 mg	￥ 1,270	现货
50 mg	￥ 2,320	现货
100 mg	￥ 3,460	现货
1 mL * 10 mM (in DMSO)	￥ 446	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Omipalisib (GSK2126458) is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
靶点活性	p110α:0.019 nM(Ki), p110γ:0.06 nM(Ki), mTORC1:0.18 nM(Ki), p110δ:0.024 nM(Ki), p110β:0.13 nM(Ki)
体外活性	在BT474人类移植瘤模型,GSK2126458（300 μg /kg）能够以剂量依赖的方式抑制肿瘤细胞生长.在临床试验中,GSK2126458 在小鼠、大鼠、犬、和猴中具有口服生物活性,并且有良好的血液清除能力.
体内活性	在T47D细胞（IC50=0.41 nM）和BT474 细胞（ IC50=0.18 nM）中,GSK2126458降低pAKT-S473水平,使细胞在G1期停滞,抑制细胞增殖。
激酶实验	HTRF In vitro Profiling Assays for PI3K Inhibition : Compounds are serially diluted (3-fold in 100% DMSO) across a 384-well polypropylene mother plate from column 1 to column 12 and column 13 to column 24, to yield 11 concentrations for GSK2126458. Columns 6 and 18 contain only DMSO. Once titrations are made, 0.05μL is transferred to a 384-well low-volume assay plate. This assay plate contains three pharmacological controls (known PI3K inhibitors) and 3 assay controls: (1) Enzyme without inhibitor; (2) Buffer minus enzyme, and (3) Buffer minus enzyme plus native PIP3. DMSO is stamped into all wells of columns 6 and 18. PIP3 is added at 40 μM in 1X Reaction buffer (1μL of 200 μM PIP3) to alternating rows of column 18 (wells 18 B, D, F, H, J, L, N, P). The no-enzyme control reactions are run in wells 18 A, C, E, G, I, K, M, O (0.1μL of 100% DMSO). The PI3-Kinase profiling assay is optimized using the HTRF kit. The assay kit contains seven reagents: 1) 4X Reaction Buffer; 2) native PIP2 (substrate); 3) Stop A (EDTA); 4) Stop B (Biotin-PIP3); 5) Detection Mix A (Streptavidin-APC); 6) Detection Mix B (Eu-labeled Anti-GST plus GST-tagged PHdomain); 7) Detection Mix C (KF). PI3Kinase Reaction Buffer is prepared by diluting the stock 1:4 with de-ionized water. Freshly prepared DTT is added at a final concentration of 5 mM on the day of use. Enzyme addition and compound pre-incubation are initiated by the addition of 2.5μL of PI3K (at twice its final concentration) in 1X reaction buffer to all wells using a Multidrop Combi. Plates are incubated at room temperature for 15 minutes. Reactions are initiated by addition of 2.5μL of 2X substrate solution (PIP2 and ATP in 1X reaction buffer) using a Multidrop Combi. Plates are incubated at room temperature for one hour. Reactions are quenched by the addition of 2.5μL of stop solution (Stop A and Stop B pre-mixed at a ratio of 5:1, respectively) to all wells using the Multidrop Combi.The quenched reactions are then processed to detect product formation by adding 2.5μL of Detection Solution to all wells using the Mulitdrop Combi (Detection mix C, Detection mix A, and Detection mix B combined together in an 18:1:1 ratio, i.e.: for a 6000 μL total volume, mix 5400 μL Detection mix C, 300μL Detection mix A, and 300 μL Detection mix B. Note: this solution should be prepared 2 hours prior to use). Following a one hour incubation in the dark, the HTRF signal is measured on the Envision plate reader set for 330 nM excitation and dual emission detection at 620 nM (Eu) and 665 nM (APC).
细胞实验	BT474, HCC1954 and T-47D (human breast) are cultured in RPMI-1640 containing 10% fetal bovine serum at 37 °C in 5% CO2 incubator. Cells are split into T75 flask two to three days prior to assay set up at density which yields approximately 70-80% confluence at time of harvest for assay. Cells are harvested using 0.25% trypsin-EDTA. Cell counts are performed on cell suspension using Trypan Blue exclusion staining. Cells are then plated in 384 well black flat bottom polystyrene in 48 μL of culture media per well at 1,000 cells/well. All plates are placed at 5% CO2, 37 °C overnight and GSK2126458 is added the following day. One plate is treated with CellTiter-Glo for a day 0 (t=0) measurement and read as described below. GSK2126458 is prepared in clear bottom polypropylene 384 well plates with consecutive two fold dilutions. 4 μL of these dilutions are added to 105 μL culture media, after mixing the solution, 2 μL of these dilutions are added into each well of the cell plates. The final concentration of DMSO in all wells is 0.15%. Cells are incubated at 37 °C, 5% CO2 for 72 hours. Following 72 hours of incubation with GSK2126458 each plate is developed and read. CellTiter-Glo reagent is added to assay plates using a volume equivalent to the cell culture volume in the wells. Plates are shaken for approximately two minutes and incubated at room temperature for approximately 30 minutes and chemiluminescent signal is read on the Analyst GT reader. Results are expressed as a percent of the t=0 and plotted against the GSK2126458 concentration. Cell growth inhibition is determined for GSK2126458 by fitting the dose response with a 4 or 6 parameter curve fit using XLfit software and determining the concentration that inhibits 50% of the cell growth (gIC50) with the Y min as the t=0 and Y max as the DMSO control. Value from wells with no cells is subtracted from all samples for background correction.(Only for Reference)

别名	GSK458, GSK2126458
分子量	505.5
分子式	C25H17F2N5O3S
CAS No.	1086062-66-9

存储

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

溶解度

DMSO: 100 mg/mL (197.82 mM)

Ethanol: < 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	1.9782 mL	9.8912 mL	19.7824 mL	49.456 mL
	5 mM	0.3956 mL	1.9782 mL	3.9565 mL	9.8912 mL
	10 mM	0.1978 mL	0.9891 mL	1.9782 mL	4.9456 mL
	20 mM	0.0989 mL	0.4946 mL	0.9891 mL	2.4728 mL
	50 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9891 mL
	100 mM	0.0198 mL	0.0989 mL	0.1978 mL	0.4946 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Knight SD, et al. ACS Med. Chem. Lett. 2010, 1 (1), 39–43. 2. Greger JG, et al. Mol Cancer Ther. 2012, 11(4), 909-920.

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

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+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

Omipalisib 1086062-66-9 Autophagy PI3K/Akt/mTOR signaling PI3K mTOR Inhibitor inhibit GSK 2126458 Mammalian target of Rapamycin GSK 458 GSK-2126458 GSK458 Phosphoinositide 3-kinase GSK2126458 GSK-458 inhibitor

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Omipalisib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords