Omipalisib (GSK2126458)

别名: GSK458

Omipalisib (GSK2126458, GSK458)是一种高选择性的,有效的p110α/β/γ/δ和 mTORC1/2抑制剂,无细胞试验中Ki分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。Omipalisib 可诱导自噬。Phase 1。

Omipalisib (GSK2126458) Chemical Structure

Omipalisib (GSK2126458) Chemical Structure

CAS: 1086062-66-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 3095.01 现货
2mg RMB 1387.54 现货
5mg RMB 2224.11 现货
10mg RMB 3034.97 现货
1g RMB 39900 现货
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客户使用Selleck的Omipalisib (GSK2126458)发表文献53

产品质控

批次: 纯度: 99.46%
99.46

Omipalisib (GSK2126458)相关产品

相关信号通路图

PI3K抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 0.01 μM. 26819001
Bel7404 Cytotoxicity assay 72 hrs Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay, IC50 = 0.01 μM. 26819001
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 0.13 μM. 26819001
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.14 μM. 27448924
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 0.154 μM. 27448924
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.537 μM. 27448924
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.6 μM. 26819001
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Omipalisib (GSK2126458, GSK458)是一种高选择性的,有效的p110α/β/γ/δ和 mTORC1/2抑制剂,无细胞试验中Ki分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。Omipalisib 可诱导自噬。Phase 1。
靶点
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
mTORC1 [1]
(Cell-free assay)
点击更多
0.019 nM(Ki) 0.024 nM(Ki) 0.06 nM(Ki) 0.13 nM(Ki) 0.18 nM(Ki)
体外研究(In Vitro)
体外研究活性 GSK2126458有效抑制人类癌细胞中发现的p110α(E542K, E545K, 和H1047R)常见激活突变型,Ki 分别为 8 pM, 8 pM 和 9 pM。GSK2126458作用于T47D和BT474 细胞,显著降低pAKT-S473水平,IC50分别为 0.41 nM 和 0.18 nM。 而且, GSK2126458作用于多种细胞系,包括T47D 和 BT474乳腺癌细胞系,导致细胞周期停在G1期,且抑制细胞增殖,IC50分别为3 nM 和2.4 nM。[1]
激酶实验 体外均相时间分辨荧光技术(HTRF)测定 PI3K 抑制
在384孔聚丙烯母板上,化合物 (3倍溶于100% DMSO) 从1列到12列,和13列到24列连续稀释,获得11种浓度 GSK2126458。6列和18列只含DMSO。滴定后,0.05μL 立即转移到384孔低容量实验板上。 实验板中含3种药物对照(PI3K 抑制剂)和3组实验对照: (1) 不含抑制剂的酶实验;(2) 去酶buffer, 和 (3)去酶加 PIP3的buffer。DMSO加到6列和18列的所有孔中。40 μM PIP3加到 1X 反应 buffer (1μL 200 μM PIP3)中, 交替 18列的行数 ( B, D, F, H, J, L, N, P)。不含酶的对照实验在 A, C, E, G, I, K, M, O孔中 (0.1μL 100% DMSO)中进行。使用 HTRF试剂盒优化PI3K 实验 。实验试剂盒中含7种试剂: 1) 4X 反应Buffer; 2) PIP2 (底物); 3) Stop A (EDTA); 4) Stop B (生物素-PIP3); 5) 检测混合物A (链霉亲和素-APC); 6)检测混合物 B (Eu-标记的抗-GST抗体和 GST标记的 PH域); 7) 检测混合物 C (KF)。通过使用去离子水按1:4稀释而制备PI3K反应 Buffer。加入新鲜制备的 DTT,终浓度为5 mM。加入酶,使用Multidrop Combi 在1X反应 buffer中加入2.5μL PI3K,加到每孔中 ,开始预温育化合物。实验板在室温下温育15分钟。 使用Multidrop Combi,加入 2.5μL 2X底物溶液(PIP2和 ATP,溶于 1X 反应buffer)开始反应。实验板在室温下温育1小时。 使用Multidrop Combi在所有孔中加入2.5μL 终止液 (Stop A和 Stop B按5:1比例预混合),反应淬灭。使用Mulitdrop Combi(检测混合物 C, 检测混合物 A,和检测混合物 B 按18:1:1比率混合,即: 6000 μL 总体积, 混合 5400 μL 检测混合物 C, 300μL 检测混合物 A, 和 300 μL 检测混合物 B)在所有孔中加入2.5μL 检测液,进行淬火反应,检测形成的产品。备注:这种溶液在使用前2小时制备。在暗中温育1小时后,在Envision 酶标仪上测量HTRF信号,在330nm 处测定激发光,在620nm (Eu) 和665nm (APC)处双重发射光。
细胞实验 细胞系 BT474, HCC1954 和 T-47D
浓度 0 到 1 μM
孵育时间 72 小时
方法 BT474, HCC1954 和 T-47D(人类乳腺)培养在含10%胎牛血清的 RPMI-1640 培养基中,培养在37oC下含 5% CO2的 孵育器中。在实验前2到3天,细胞按密度分到T75 烧瓶中,这样在实验收集时获得约70-80% 细胞汇合。使用0.25% 胰蛋白酶-EDTA收集细胞。在细胞悬液中使用台酚蓝染色排除染色,进行细胞计数。细胞按每孔1000个细胞接种在384孔黑色平底聚苯乙烯板中, 每孔含48 μL 培养基。所有实验板置于5% CO2, 37oC 下过夜,第二天加入 GSK2126458。使用CellTiter-Glo处理一个实验板,用于第一天测量。GSK2126458 在清澈见底的聚丙烯384孔板中制备,连续稀释两倍。4 μL 这些稀释液加到105 μL 培养基中混合溶液后, 细胞板的每孔中加入2 μL这些稀释液。所有孔中的 DMSO 终浓度为0.15%。细胞在37oC, 5% CO2 环境中温育 72小时。随后与 GSK2126458温育72小时。CellTiter-Glo试剂加到实验板中,使用与孔中细胞培养体积相当量的体积。震荡实验板约2分钟,在室温下温育约30分钟,然后在Analyst GT 读数器上读取化学分光信号。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-AKT / AKT / p-RPS6 / RPS6 / p-4E-BP1 / 4E-BP1 31069214
Growth inhibition assay IC50 26148118
体内研究(In Vivo)
体内研究活性 GSK2126458作用于BT474人类移植瘤模型,降低pAKT-S473水平,这种作用存在剂量依赖性,按300 μg /kg低剂量处理抑制肿瘤生长,这种作用存在剂量依赖性。此外, GSK2126458 作用于四种临床前期物种(小鼠, 大鼠,犬 ,和猴 ),具有低血液清除力和良好口服生物有效性。[1]
动物实验 Animal Models 在小鼠体内移植BT474肿瘤
Dosages ≤300 μg /kg
Administration 口服处理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01725139 Completed
Idiopathic Pulmonary Fibrosis
GlaxoSmithKline
March 8 2013 Phase 1
NCT01248858 Terminated
Cancer
GlaxoSmithKline
December 3 2010 Phase 1
NCT00972686 Completed
Solid Tumours
GlaxoSmithKline
August 31 2009 Phase 1

化学信息&溶解度

分子量 505.5 分子式

C25H17F2N5O3S

CAS号 1086062-66-9 SDF Download Omipalisib (GSK2126458) SDF
Smiles COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 30 mg/mL ( (59.34 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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