Omipalisib (GSK2126458)

別名: GSK458

目錄號(hào)：S2658 Purity: 99.46%

Omipalisib (GSK2126458, GSK458)是一種高選擇性的，有效的p110α/β/γ/δ和 mTORC1/2抑制劑，無(wú)細(xì)胞試驗(yàn)中K_i分別為0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。Omipalisib 可誘導(dǎo)自噬。Phase 1。

Omipalisib (GSK2126458) Chemical Structure

CAS: 1086062-66-9

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	3095.01	現(xiàn)貨
2mg	1387.54	現(xiàn)貨
5mg	2224.11	現(xiàn)貨
10mg	3034.97	現(xiàn)貨
1g	39900	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.46%

99.46

Omipalisib (GSK2126458)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	p110α p110β p110δ p110γ C2β Vps34	點(diǎn)擊展開
相關(guān)產(chǎn)品	LY294002 3-MA (3-Methyladenine) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615 Pilaralisib (XL147) TG100-115 CZC24832 Voxtalisib (XL765) XL147 analogue AS-604850 BGT226 (NVP-BGT226) maleate Quercetin Dihydrate VPS34 inhibitor 1 (Compound 19) Samotolisib (LY3023414) Voxtalisib (XL765) Analogue AMG319 Nemiralisib Bimiralisib (PQR309) CH5132799 PKI-402 TG100713 Paxalisib (GDC-0084) SF2523 Serabelisib (TAK-117) GDC-0326 GNE-317 Inavolisib (GDC-0077) PIK-294 PI-3065 AZD8835 Seletalisib (UCB-5857) leniolisib (CDZ 173) (E)-Akt inhibitor-IV Gallein CAY10505 Selective PI3Kδ Inhibitor 1 (compound 7n) PF-4989216 GNE-477 GNE-493	點(diǎn)擊展開
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) 凋亡分子化合物庫(kù) 細(xì)胞周期化合物庫(kù) NF-κB信號(hào)通路庫(kù)	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

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)	點(diǎn)擊更多
0.019 nM(Ki)	0.024 nM(Ki)	0.06 nM(Ki)	0.13 nM(Ki)	0.18 nM(Ki)	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	GSK2126458有效抑制人類癌細(xì)胞中發(fā)現(xiàn)的p110α(E542K, E545K, 和H1047R)常見激活突變型，K_i 分別為 8 pM, 8 pM 和 9 pM。GSK2126458作用于T47D和BT474 細(xì)胞，顯著降低pAKT-S473水平，IC50分別為 0.41 nM 和 0.18 nM。而且, GSK2126458作用于多種細(xì)胞系，包括T47D 和 BT474乳腺癌細(xì)胞系，導(dǎo)致細(xì)胞周期停在G1期，且抑制細(xì)胞增殖，IC50分別為3 nM 和2.4 nM。^[1]
激酶實(shí)驗(yàn)	體外均相時(shí)間分辨熒光技術(shù)（HTRF）測(cè)定 PI3K 抑制
激酶實(shí)驗(yàn)	在384孔聚丙烯母板上，化合物 (3倍溶于100% DMSO) 從1列到12列，和13列到24列連續(xù)稀釋，獲得11種濃度 GSK2126458。6列和18列只含DMSO。滴定后，0.05μL 立即轉(zhuǎn)移到384孔低容量實(shí)驗(yàn)板上。實(shí)驗(yàn)板中含3種藥物對(duì)照(PI3K 抑制劑)和3組實(shí)驗(yàn)對(duì)照: (1) 不含抑制劑的酶實(shí)驗(yàn);(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 反應(yīng) buffer (1μL 200 μM PIP3)中，交替 18列的行數(shù) ( B, D, F, H, J, L, N, P)。不含酶的對(duì)照實(shí)驗(yàn)在 A, C, E, G, I, K, M, O孔中 (0.1μL 100% DMSO)中進(jìn)行。使用 HTRF試劑盒優(yōu)化PI3K 實(shí)驗(yàn) 。實(shí)驗(yàn)試劑盒中含7種試劑: 1) 4X 反應(yīng)Buffer; 2) PIP2 (底物); 3) Stop A (EDTA); 4) Stop B (生物素-PIP3); 5) 檢測(cè)混合物A (鏈霉親和素-APC); 6)檢測(cè)混合物 B (Eu-標(biāo)記的抗-GST抗體和 GST標(biāo)記的 PH域); 7) 檢測(cè)混合物 C (KF)。通過(guò)使用去離子水按1:4稀釋而制備PI3K反應(yīng) Buffer。加入新鮮制備的 DTT，終濃度為5 mM。加入酶，使用Multidrop Combi 在1X反應(yīng) buffer中加入2.5μL PI3K，加到每孔中，開始預(yù)溫育化合物。實(shí)驗(yàn)板在室溫下溫育15分鐘。使用Multidrop Combi，加入 2.5μL 2X底物溶液(PIP2和 ATP，溶于 1X 反應(yīng)buffer)開始反應(yīng)。實(shí)驗(yàn)板在室溫下溫育1小時(shí)。使用Multidrop Combi在所有孔中加入2.5μL 終止液 (Stop A和 Stop B按5:1比例預(yù)混合)，反應(yīng)淬滅。使用Mulitdrop Combi(檢測(cè)混合物 C, 檢測(cè)混合物 A,和檢測(cè)混合物 B 按18:1:1比率混合，即: 6000 μL 總體積, 混合 5400 μL 檢測(cè)混合物 C, 300μL 檢測(cè)混合物 A, 和 300 μL 檢測(cè)混合物 B)在所有孔中加入2.5μL 檢測(cè)液，進(jìn)行淬火反應(yīng)，檢測(cè)形成的產(chǎn)品。備注:這種溶液在使用前2小時(shí)制備。在暗中溫育1小時(shí)后，在Envision 酶標(biāo)儀上測(cè)量HTRF信號(hào)，在330nm 處測(cè)定激發(fā)光，在620nm (Eu) 和665nm (APC)處雙重發(fā)射光。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	BT474, HCC1954 和 T-47D
	濃度	0 到 1 μM
	孵育時(shí)間	72 小時(shí)
	方法	BT474, HCC1954 和 T-47D(人類乳腺)培養(yǎng)在含10%胎牛血清的 RPMI-1640 培養(yǎng)基中，培養(yǎng)在37^oC下含 5% CO₂的孵育器中。在實(shí)驗(yàn)前2到3天，細(xì)胞按密度分到T75 燒瓶中，這樣在實(shí)驗(yàn)收集時(shí)獲得約70-80% 細(xì)胞匯合。使用0.25% 胰蛋白酶-EDTA收集細(xì)胞。在細(xì)胞懸液中使用臺(tái)酚藍(lán)染色排除染色，進(jìn)行細(xì)胞計(jì)數(shù)。細(xì)胞按每孔1000個(gè)細(xì)胞接種在384孔黑色平底聚苯乙烯板中，每孔含48 μL 培養(yǎng)基。所有實(shí)驗(yàn)板置于5% CO₂, 37^oC 下過(guò)夜，第二天加入 GSK2126458。使用CellTiter-Glo處理一個(gè)實(shí)驗(yàn)板，用于第一天測(cè)量。GSK2126458 在清澈見底的聚丙烯384孔板中制備，連續(xù)稀釋兩倍。4 μL 這些稀釋液加到105 μL 培養(yǎng)基中混合溶液后, 細(xì)胞板的每孔中加入2 μL這些稀釋液。所有孔中的 DMSO 終濃度為0.15%。細(xì)胞在37^oC, 5% CO₂ 環(huán)境中溫育 72小時(shí)。隨后與 GSK2126458溫育72小時(shí)。CellTiter-Glo試劑加到實(shí)驗(yàn)板中，使用與孔中細(xì)胞培養(yǎng)體積相當(dāng)量的體積。震蕩實(shí)驗(yàn)板約2分鐘，在室溫下溫育約30分鐘，然后在Analyst GT 讀數(shù)器上讀取化學(xué)分光信號(hào)。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	p-AKT / AKT / p-RPS6 / RPS6 / p-4E-BP1 / 4E-BP1		31069214
	Growth inhibition assay	IC50		26148118

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	GSK2126458作用于BT474人類移植瘤模型，降低pAKT-S473水平，這種作用存在劑量依賴性，按300 μg /kg低劑量處理抑制腫瘤生長(zhǎng)，這種作用存在劑量依賴性。此外, GSK2126458 作用于四種臨床前期物種(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]
動(dòng)物實(shí)驗(yàn)	Animal Models	在小鼠體內(nèi)移植BT474腫瘤
	Dosages	≤300 μg /kg
	Administration	口服處理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
[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.

參考文獻(xiàn)

[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.

化學(xué)信息&溶解度

分子量	505.5	分子式	C₂₅H₁₇F₂N₅O₃S
CAS號(hào)	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
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 30 mg/mL ( (59.34 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 101 mg/mL ( (199.8 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (197.82 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Omipalisib (GSK2126458)

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實(shí)驗(yàn)計(jì)算

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