Omipalisib (Synonyms: GSK2126458; GSK458)

目录号: HY-10297 纯度: 99.91%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Omipalisib (GSK2126458) 是一种口服有效的，高选择性的 PI3K 抑制剂，抑制 p110α/β/δ/γ，mTORC1/2 的活性，K_i 值分别为 0.019 nM/0.13 nM/0.024 nM/0.06 nM 和 0.18 nM/0.3 nM。Omipalisib 具有抗癌活性。

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Omipalisib Chemical Structure

CAS No. : 1086062-66-9

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2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥556	In-stock
1 mg	￥250	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
50 mg	￥2800	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 17 篇科研文献

Omipalisib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PI3K 亚型特异性产品:

查看所有亚型

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 mTOR 亚型特异性产品:

查看所有亚型

mTOR mTORC1 mTORC2

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with K_is of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity^[1]^[2]^[3].

IC₅₀ & Target^[1]

p110α

0.019 nM (Ki)

p110α-E545K

0.008 nM (Ki)

p110α-E542K

0.008 nM (Ki)

p110α-H1047R

0.009 nM (Ki)

p110β

0.13 nM (Ki)

p110δ

0.024 nM (Ki)

p110γ

0.06 nM (Ki)

mTORC1

0.18 nM (Ki)

mTORC2

0.3 nM (Ki)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.6 μM Compound: GSK2126458	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26819001]
A549	IC₅₀	0.86 μM Compound: Omipalisib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
A549	IC₅₀	140 nM Compound: GSK-2126458	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 27448924]
A549	GI₅₀	26.6 nM Compound: GSK; GSK-2126458	Growth inhibition of human A549 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human A549 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
BEL-7404 tumor cell line	IC₅₀	0.01 μM Compound: GSK2126458	Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay	[PMID: 26819001]
DU-145	GI₅₀	16.3 nM Compound: GSK; GSK-2126458	Growth inhibition of human DU-145 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human DU-145 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
HCT-116	IC₅₀	0.01 μM Compound: GSK2126458	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26819001]
HCT-116	IC₅₀	0.14 μM Compound: Omipalisib	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
HCT-116	IC₅₀	154 nM Compound: GSK-2126458	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 27448924]
HT-29	GI₅₀	19.9 nM Compound: GSK; GSK-2126458	Growth inhibition of human HT-29 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human HT-29 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
MCF7	IC₅₀	0.03 μM Compound: Omipalisib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
MDA-MB-231	IC₅₀	0.13 μM Compound: GSK2126458	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 26819001]
NCI-H1975	GI₅₀	14.4 nM Compound: GSK; GSK-2126458	Growth inhibition of human NCI-H1975 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human NCI-H1975 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
PC-3	GI₅₀	0.25 μM Compound: 3; GSK2126458	Growth inhibition of human PC3 cells after 72 hrs by sulforhodamine B assay Growth inhibition of human PC3 cells after 72 hrs by sulforhodamine B assay	[PMID: 33561608]
PC-3	GI₅₀	197 nM Compound: GSK; GSK-2126458	Growth inhibition of human PC-3 cells harboring PTEN inactivation measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human PC-3 cells harboring PTEN inactivation measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
U-87MG ATCC	GI₅₀	0.22 μM Compound: 3; GSK2126458	Growth inhibition of human U87MG cells after 72 hrs by sulforhodamine B assay Growth inhibition of human U87MG cells after 72 hrs by sulforhodamine B assay	[PMID: 33561608]
U-87MG ATCC	IC₅₀	537 nM Compound: GSK-2126458	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 27448924]

体外研究
(In Vitro)

Omipalisib (GSK2126458) 有效抑制人类癌症中常见的 p110α 激活突变体 (E542K、E545K 和 H1047R) 的活性，K_i 分别为 8 pM、8 pM 和 9 pM。Omipalisib 显著降低 pAkt-S473 的水平，在 T47D 和 BT474 细胞中具有显著的效力，IC₅₀ 分别为 0.41 nM 和 0.18 nM。此外，Omipalisib (GSK2126458) 导致 G1 细胞周期停滞，并对大量细胞系的细胞增殖产生抑制作用，包括 T47D 和 BT474 乳腺癌细胞系，IC₅₀ 分别为 3 nM，2.4 nM^[1]。Omipalisib 或 GSK1120212 与 Omipalisib 的组合增强细胞生长抑制并降低 A375 BRAF (V600E) 和 YUSIT1 BRAF (V600K) 黑色素瘤细胞系的耐药克隆中的 S6 核糖体蛋白磷酸化^[2]。Omipalisib (GSK2126458) 增强结直肠癌细胞系中 DDR1-IN-1 的抗增殖活性^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

在 BT474 人肿瘤异种移植模型中，Omipalisib (GSK2126458) 处理导致 pAkt-S473 水平呈剂量依赖性降低，并在 300 μg/kg 的低剂量下表现出剂量依赖性肿瘤生长抑制。此外，Omipalisib (GSK2126458) 在四种临床前动物 (小鼠、大鼠、狗和猴) 中表现出低血液清除率和良好的口服生物利用度^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

505.50

Formula

C₂₅H₁₇F₂N₅O₃S

CAS 号

1086062-66-9

性状

固体

颜色

Off-white to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (98.91 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9782 mL	9.8912 mL	19.7824 mL
5 mM	0.3956 mL	1.9782 mL	3.9565 mL
10 mM	0.1978 mL	0.9891 mL	1.9782 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.95 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.93%

选择批次：

Data Sheet (653 KB) SDS (252 KB)

COA (200 KB) LCMS (97 KB) 元素分析报告 (217 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Knight SD, et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1 (1), 39-43. [Content Brief]

[2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20. [Content Brief]

[3]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. [Content Brief]

Cell Assay ^[1]	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 Omipalisib (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. Omipalisib (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 Omipalisib 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 Omipalisib (GSK2126458) concentration. Cell growth inhibition is determined for Omipalisib (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.. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Knight SD, et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1 (1), 39-43. [Content Brief] [2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20. [Content Brief] [3]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. [Content Brief]

Cell Assay
^[1]

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 Omipalisib (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. Omipalisib (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 Omipalisib 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 Omipalisib (GSK2126458) concentration. Cell growth inhibition is determined for Omipalisib (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..

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Knight SD, et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1 (1), 39-43. [Content Brief]

[2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20. [Content Brief]

[3]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. [Content Brief]

Omipalisib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9782 mL	9.8912 mL	19.7824 mL	49.4560 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
	15 mM	0.1319 mL	0.6594 mL	1.3188 mL	3.2971 mL
	20 mM	0.0989 mL	0.4946 mL	0.9891 mL	2.4728 mL
	25 mM	0.0791 mL	0.3956 mL	0.7913 mL	1.9782 mL
	30 mM	0.0659 mL	0.3297 mL	0.6594 mL	1.6485 mL
	40 mM	0.0495 mL	0.2473 mL	0.4946 mL	1.2364 mL
	50 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9891 mL
	60 mM	0.0330 mL	0.1649 mL	0.3297 mL	0.8243 mL
	80 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6182 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Omipalisib1086062-66-9GSK2126458 GSK458GSK 2126458GSK-2126458GSK458GSK 458GSK-458PI3KmTORAutophagyPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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Omipalisib (Synonyms: GSK2126458; GSK458)

Customer Review

MCE 顾客使用本产品发表的 17 篇科研文献

Omipalisib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PI3K 亚型特异性产品:

查看 mTOR 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Omipalisib 相关分类

完整储备液配制表

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Omipalisib (Synonyms: GSK2126458; GSK458)

Customer Review

Omipalisib 相关抗体

MCE 顾客使用本产品发表的 17 篇科研文献

Omipalisib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PI3K 亚型特异性产品:

查看 mTOR 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Omipalisib 相关抗体:

摩尔计算器

稀释计算器

Omipalisib 相关分类

完整储备液配制表

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您最近查看的产品:

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