Uprosertib (GSK2141795)

別名: GSK795

目錄號(hào)：S7492 Purity: 99.84%

Uprosertib (GSK2141795, GSK795)是一種選擇性的，ATP競(jìng)爭(zhēng)性的，具有口服活性的Akt抑制劑，其對(duì)Akt 1/2/3的 IC50分別為180 nM, 328 nM和38 nM。Phase 2。

Uprosertib (GSK2141795) Chemical Structure

CAS: 1047634-65-0

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1122.03	現(xiàn)貨
5mg	958.71	現(xiàn)貨
25mg	3252.14	現(xiàn)貨
100mg	7347.21	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.84%

99.84

Uprosertib (GSK2141795)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	Akt1 Akt2 Akt3	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	MK-2206 2HCl Perifosine SC79 Capivasertib (AZD5363) GSK690693 Ipatasertib (GDC-0068) Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) A-674563 HCl AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) Miransertib (ARQ 092) HCl AT13148 Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl	點(diǎn)擊展開(kāi)
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(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	孵育時(shí)間	活性描述	文獻(xiàn)信息
Sf9	Function assay	40 mins	Inhibition of full length human AKT2 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50=0.01585μM	ChEMBL
Sf9	Function assay	40 mins	Inhibition of full length human AKT1 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50=0.001995μM	ChEMBL
OVCAR8	Cytotoxicity assay	72 hrs	Cytotoxicity against human OVCAR8 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=0.54μM	31301565
HCT116	Antiproliferative assay	72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.72μM	31298542
PTEN-null LNCAP	Function assay	1 hr	Inhibition of Akt in human PTEN-null LNCAP cells assessed as suppression in PRAS40 phosphorylation after 1 hr by ELISA analysis, IC50=0.07563μM	27089211
HCT116	Growth inhibition assay	72 hrs	Growth inhibition of human HCT116 cells over-expressing DHODH at 2 times antiproliferative IC50 after 72 hrs in absence of uridine by MTT assay	31301565
OVCAR8	Cytotoxicity assay	72 hrs	Cytotoxicity against human OVCAR8 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=0.54μM	31301565
HCT116	Antiproliferative assay	72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.72μM	31298542
HCT116	Growth inhibition assay	72 hrs	Growth inhibition of human HCT116 cells over-expressing DHODH at 2 times antiproliferative IC50 after 72 hrs in absence of uridine by MTT assay	31301565
RPMI8226	Antiproliferative assay		Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability, IC50=0.538μM	31301565
MM1S	Antiproliferative assay		Antiproliferative activity against human MM1S cells assessed as reduction in cell viability, IC50=0.032μM	31301565
CEM/C1	Antiproliferative assay		Antiproliferative activity against human CEM/C1 cells assessed as reduction in cell viability, IC50=0.03μM	31301565
HUT78	Antiproliferative assay		Antiproliferative activity against human HUT78 cells assessed as reduction in cell viability, IC50=0.378μM	31301565
KB-3-1	qHTS assay		P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	ChEMBL
JVM2	Antiproliferative assay		Antiproliferative activity against human JVM2 cells assessed as reduction in cell viability, IC50=0.293μM	31301565
OVCAR8	Antiproliferative assay		Antiproliferative activity against human OVCAR8 cells, IC50=0.24μM	31298542
MOLT4	Antiproliferative assay		Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability, IC50=0.066μM	31301565
MV4-11	Antiproliferative assay		Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability, IC50=0.635μM	31301565
LNCAP	Antiproliferative assay		Antiproliferative activity against human LNCAP cells, IC50=0.07μM	31298542
U937	Antiproliferative assay		Antiproliferative activity against human U937 cells assessed as reduction in cell viability, IC50=0.101μM	31301565
OVCAR8	Antiproliferative assay		Antiproliferative activity against human OVCAR8 cells, IC50=0.24μM	31298542
JVM2	Antiproliferative assay		Antiproliferative activity against human JVM2 cells assessed as reduction in cell viability, IC50=0.293μM	31301565
HUT78	Antiproliferative assay		Antiproliferative activity against human HUT78 cells assessed as reduction in cell viability, IC50=0.378μM	31301565
RPMI8226	Antiproliferative assay		Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability, IC50=0.538μM	31301565
MV4-11	Antiproliferative assay		Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability, IC50=0.635μM	31301565
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生物活性

產(chǎn)品描述

靶點(diǎn)

Akt3 ^[1] (Cell-free assay)	Akt1 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)
38 nM	180 nM	328 nM

體外研究(In Vitro)
體外研究活性	Uprosertib抑制了BT474和LNCaP細(xì)胞中多個(gè)AKT底物的磷酸化水平。Uprosertib優(yōu)先的抑制了AKT通路活化的腫瘤細(xì)胞增殖。在細(xì)胞系LNCaP, BT474, A3和I9.2中，Uprosertib還導(dǎo)致了細(xì)胞周期停滯。^[2] 在SKOV3和PEO4細(xì)胞中，Uprosertib導(dǎo)致了生長(zhǎng)停滯，并且增強(qiáng)了誘導(dǎo)的凋亡。^[3]
激酶實(shí)驗(yàn)	選擇性試驗(yàn)
激酶實(shí)驗(yàn)	裂解液(5 mg總蛋白)分別用DMSO, 2.5 nM, 25 nM, 250 nM, 2.5 μM以及25 μM的抑制劑(GSK690693或者GSK2141795)處理，放到振蕩器上4 °C孵育45 min。雖有，將裂解液加入beads(偶聯(lián)有Akt探針)4 1 h，用于定性和定量實(shí)驗(yàn)。將beads用1× CP緩沖液沖洗，并用離心收集。結(jié)合蛋白用2× NuPAGE LDS樣本緩沖液抽提，抽吸液用50 mM二硫蘇糖醇和55 mM碘乙酰胺處理。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	290個(gè)細(xì)胞系
	濃度	~30 μM
	孵育時(shí)間	3 d
	方法	細(xì)胞系通常培養(yǎng)在加入10% FBS的RPMI 160培養(yǎng)基中。一部分細(xì)胞系生長(zhǎng)在供應(yīng)商特殊處理的培養(yǎng)基中。用CellTiter-GloA來(lái)檢測(cè) 3-day增殖試驗(yàn)中在化合物0–30 µM濃度下的生長(zhǎng)抑制。細(xì)胞成長(zhǎng)數(shù)據(jù)用DMSO處理的細(xì)胞作為空白對(duì)照。EC50利用4或者6個(gè)參數(shù)的抑制數(shù)據(jù)進(jìn)行計(jì)算。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在生長(zhǎng)有BT474乳腺癌腫瘤的小鼠中，Uprosertib (100 mg/kg, p.o.)導(dǎo)致了61%的腫瘤生長(zhǎng)抑制。在生長(zhǎng)有SKOV3卵巢癌腫瘤小鼠中，Uprosertib (30 mg/kg, p.o.)也誘導(dǎo)了61%的腫瘤生長(zhǎng)抑制。^[2]
動(dòng)物實(shí)驗(yàn)	Animal Models	生長(zhǎng)有BT474或者SKOV3腫瘤的小鼠
	Dosages	100 mg/kg
	Administration	p.o.

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)
NCT01958112	Terminated	Cervical Cancer	Dana-Farber Cancer Institute\|Novartis\|National Comprehensive Cancer Network	October 2013	Phase 2
NCT01941927	Completed	Melanoma	Adil Daud\|National Comprehensive Cancer Network\|University of California San Francisco	September 10 2013	Phase 2
NCT01266954	Completed	Solid Tumours	GlaxoSmithKline	June 1 2010	Phase 1
NCT01138085	Completed	Cancer	GlaxoSmithKline	May 4 2010	Phase 1

參考文獻(xiàn)
[1] Pachl F, et al. J Proteome Res. 2013, 12(8), 3792-3800. [2] Dumble M, et al. PLoS One. 2014, 9(6):e100880. [3] Cheraghchi-Bashi A, et al. Oncotarget. 2015, 6(39), 41736-41749.

參考文獻(xiàn)

[1] Pachl F, et al. J Proteome Res. 2013, 12(8), 3792-3800.
[2] Dumble M, et al. PLoS One. 2014, 9(6):e100880.
[3] Cheraghchi-Bashi A, et al. Oncotarget. 2015, 6(39), 41736-41749.

化學(xué)信息&溶解度

分子量	429.25	分子式	C₁₈H₁₆C_l2F₂N₄O₂
CAS號(hào)	1047634-65-0	SDF	Download Uprosertib (GSK2141795) SDF
Smiles	CN1C(=C(C=N1)Cl)C2=C(OC(=C2)C(=O)NC(CC3=CC(=C(C=C3)F)F)CN)Cl
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 : 85 mg/mL ( (198.01 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 85 mg/mL (198.01 mM)

Water : Insoluble

DMSO : 93 mg/mL ( (216.65 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 93 mg/mL (216.65 mM)

Water : 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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