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AG-490

別名: Tyrphostin B42, Zinc02557947

AG-490是一種EGFR抑制劑,在無細(xì)胞試驗(yàn)中IC50為0.1 μM,作用于EGFR比作用于ErbB2選擇性高135倍,對(duì)JAK2也有抑制作用,對(duì)Lck,Lyn,Btk,Syk和Src沒有抑制活性。

AG-490 Chemical Structure

AG-490 Chemical Structure

CAS: 133550-30-8

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 790 現(xiàn)貨
10mg 647.01 現(xiàn)貨
25mg 819.84 現(xiàn)貨
50mg 1449.63 現(xiàn)貨
100mg 2760.17 現(xiàn)貨
300mg 5872.23 現(xiàn)貨
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AG-490相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
SUPT1? Apoptosis Assay 50 μM 24/48 h enhances TRAIL-induces cell apoptosis 19564891
Jurkat? Apoptosis Assay 50 μM 24/48 h enhances TRAIL-induces cell apoptosis 19564891
SUPT1? Growth Inhibition Assay 50 μM 24/48/72 h enhances TRAIL-induces cell growth inhibition 19564891
Jurkat? Growth Inhibition Assay 50 μM 24/48/72 h enhances TRAIL-induces cell growth inhibition 19564891
PA-1 Function Assay 10 uM 1 h inhibits LPA-induced ovarian cancer cell motility 19647363
OVCAR-3 Function Assay 10 uM 1 h inhibits LPA-induced ovarian cancer cell motility 19647363
PA-1 Function Assay 10 uM 1 h inhibits LPA-induced STAT3 phosphorylation 19647363
OVCAR-3 Function Assay 10 uM 1 h inhibits LPA-induced STAT3 phosphorylation 19647363
A549 Function Assay 15 μm 1 h inhibits the phosphorylation of STAT1 on tyrosine 701 was detected 15 min after SPE B treatment 19801665
BMMC Function Assay 0-10 μM 15?min inhibits LTC4?release in a dose-dependent fashion with near complete inhibition at concentrations ?10?μM 19835845
THP1 Function Assay 10 uM 30 min? inhibits STAT3 tyrosine phosphorylation by over 60% 20393690
SW1990 Invasion Assay 20 μM 24 h reduces invasion of SW1990 cells? 20482858
SW1990 Function Assay 20 μM 24 h decreases the intensity of p-Stat3 expression 20482858
SW1990 Function Assay 20 μM 24 h decreases the expression of MMP-2 and VEGF mRNAs 20482858
SW1990 Growth Inhibition Assay 20 μM 24/48/72 h inhibits cell growth time dependently 20482858
MZ-304 Function Assay 50/100?μM 48 h reduces transcription of MMP genes and reduces enzymatic activity of MMPs 20589525
MZ-256 Function Assay 50/100?μM 48 h reduces transcription of MMP genes and reduces enzymatic activity of MMPs 20589525
MZ-54 Function Assay 50/100?μM 48 h reduces transcription of MMP genes and reduces enzymatic activity of MMPs 20589525
MZ-18 Function Assay 50/100?μM 48 h reduces transcription of MMP genes and reduces enzymatic activity of MMPs 20589525
A-172 Function Assay 50/100?μM 48 h reduces transcription of MMP genes and reduces enzymatic activity of MMPs 20589525
MZ-304 Function Assay 100?μM 48 h inhibits invasion 20589525
MZ-256 Function Assay 100?μM 48 h inhibits invasion 20589525
MZ-54 Function Assay 100?μM 48 h inhibits invasion 20589525
MZ-18 Function Assay 100?μM 48 h inhibits invasion 20589525
A-172 Function Assay 100?μM 48 h inhibits invasion 20589525
MZ-304 Function Assay 50/100?μM 48 h inhibits migration 20589525
MZ-256 Function Assay 50/100?μM 48 h inhibits migration 20589525
MZ-54 Function Assay 50/100?μM 48 h inhibits migration 20589525
MZ-18 Function Assay 50/100?μM 48 h inhibits migration 20589525
A-172 Function Assay 50/100?μM 48 h inhibits migration 20589525
MZ-304 Growth Inhibition Assay 50/100?μM 48 h leads to a statistically significant reduction of cell proliferation over a time period of 48?h 20589525
MZ-256 Growth Inhibition Assay 50/100?μM 48 h leads to a statistically significant reduction of cell proliferation over a time period of 48?h 20589525
MZ-54 Growth Inhibition Assay 50/100?μM 48 h leads to a statistically significant reduction of cell proliferation over a time period of 48?h 20589525
MZ-18 Growth Inhibition Assay 50/100?μM 48 h leads to a statistically significant reduction of cell proliferation over a time period of 48?h 20589525
A-172 Growth Inhibition Assay 50/100?μM 48 h leads to a statistically significant reduction of cell proliferation over a time period of 48?h 20589525
MZ-304 Function Assay 50/100?μM 48 h reduces the levels of constitutively activated STAT3 in a time-dependent and dose-dependent fashion 20589525
MZ-256 Function Assay 50/100?μM 48 h reduces the levels of constitutively activated STAT3 in a time-dependent and dose-dependent fashion 20589525
MZ-54 Function Assay 50/100?μM 48 h reduces the levels of constitutively activated STAT3 in a time-dependent and dose-dependent fashion 20589525
MZ-18 Function Assay 50/100?μM 48 h reduces the levels of constitutively activated STAT3 in a time-dependent and dose-dependent fashion 20589525
A-172 Function Assay 50/100?μM 48 h reduces the levels of constitutively activated STAT3 in a time-dependent and dose-dependent fashion 20589525
HEL Growth Inhibition Assay 100?μM 0-5 d reduces growth of JAK2V617F-expressing HEL cells 20621061
HEL? Function Assay 100?μM 12-72 h inhibits the level of p-JAK2, JAK2 20621061
KF8 Function Assay 10?μM? 1?h? inhibits IL-33-induced IκBα degradation and NF-κB activation 20940045
KF8 Function Assay 10?μM? 1?h inhibits IL-33-induced NF-κB activation 20940045
Hep-2 Function Assay 50 μM 24/48/72 h downregulates the STAT3, p-STAT3 and survivin protein levels 21309481
Hep-2 Function Assay 50 μM 24/48/72 h inhibits G1 to S cell cycle transition and induces G1 cell cycle arrest 21309481
Hep-2 Apoptosis Assay 50 μM 24/48/72 h induces cell apoptosis time dependently 21309481
Hep-2 Growth Inhibition Assay 25-100 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 21309481
HSC-T6 Function Assay 10?μM 2?h? inhibits the expressions of pY-STAT1 and Bad induced by CDE 21396998
HSC-T6 Apoptosis Assay 10?μM 2?h? inhibits the apoptosis of HSC-T6 cells induced by CDE 21396998
ARPE-19 Function Assay 5?μM 30?min inhibits JAK2 phosphorilation 21620963
HT29 Function Assay 100 μM? 24/48/72 h decreases the pSTAT3 levels in a time-dependent manner? 22050790
SW1116 Function Assay 100 μM? 24/48/72 h decreases the pSTAT3 levels in a time-dependent manner? 22050790
HT29 Function Assay 100 μM? 24/48/72 h decreases the expression of JAK2 and pJAK2 time-dependently 22050790
SW1116 Function Assay 100 μM? 24/48/72 h decreases the expression of JAK2 and pJAK2 time-dependently 22050790
RPE? Function Assay 30 μM? 3 h inhibits the induction of p-STAT3 expression 23094067
SW620? Function Assay 20 μM 1/6 h inhibits p-STAT3 activation 23110625
NRK-52E? Function Assay 5?μM 30?min attenuates Ang-(1–7)-inhibited TGF-β1 mRNA at 16?h? 23174757
BV-2? Function Assay 20 μM 16 h inhibits LPS-induced STAT1 phosphorylation with almost completely diminished iNOS expression 23236370
HUVECs Apoptosis Assay 20 μM 4 h significantly decreases the cell apoptotic index 23483946
HUVECs Cell Viability Assay 20 μM 4 h attenuates H2O2-induced cell shrinkage and improved the attachment rate of the cells 23483946
A549? Function Assay 10/20/40 μM 24 h suppresses the radiation-induced elevation of VEGF? 23620191
A549? Function Assay 20/40 μM 20 h 20 μM AG490 suppresses the radiation-induced invasion of A549 cells 23620191
RAW264.7 Function Assay 50?μM 24/48 h inhibits RANKL-induced NFATc1 expression and phosphorylation of Ser727STAT3 23665018
RAW264.7 Growth Inhibition Assay 0-50?μM? 48?h causes an arrest of RAW264.7 cells at the G0/G1 phase of the cell cycle 23665018
RAW264.7 Growth Inhibition Assay 0-50?μM? 48?h inhibits cell growth dose-dependently 23665018
RAW264.7? Function Assay 50?μM? 24/48 h suppresses RANKL-induced osteoclastogenesis 23665018
HepG2? Function Assay 100 μM 12/24 h inhibits STAT3 tyrosine phosphorylation 23836400
7TD1-WD-90? Function Assay 50 μM 6 h significantly inhibits the phosphorylation of JAK2 and phosphorylation of STAT3 23871159
7TD1-WD-90 Apoptosis Assay 50 μM 48 h induces apoptosis 23871159
7TD1-DXM Apoptosis Assay 50 μM 48 h induces apoptosis 23871159
7TD1-WD-90 Growth Inhibition Assay 10 μM 72 h inhibits cell growth 23871159
7TD1-DXM Growth Inhibition Assay 10 μM 72 h inhibits cell growth 23871159
MC3T3-E1? Function Assay 50 μM 4 h inhibits HSE-induced BMP7 and GHR protein expression? 23877734
AGS? Function Assay 50 μM 24/48/72 h the cytoplasmic localization of pJAK2 (JAK2 phosphorylated at residues Tyr1007 and Tyr1008) decreased after AG490 treatment for 24 and 48 hr, but started to rebound at 72 hr 24151255
SGC7901 Function Assay 50 μM 24/48/72 h the cytoplasmic localization of pJAK2 (JAK2 phosphorylated at residues Tyr1007 and Tyr1008) decreased after AG490 treatment for 24 and 48 hr, but started to rebound at 72 hr 24151255
AGS? Function Assay 50 μM 24/48/72 h the levels of pJAK2 began to decline at 24 hr, and rebounded at 72 hr? 24151255
SGC7901 Function Assay 50 μM 24/48/72 h the levels of pJAK2 began to decline at 24 hr, and rebounded at 72 hr? 24151255
AGS? Cell Viability Assay 0-100 μM 24/48/72 h causes a significant reduction in cell viability dose-dependently but not time-dependently 24151255
SGC7901 Cell Viability Assay 0-100 μM 24/48/72 h causes a significant reduction in cell viability dose-dependently but not time-dependently 24151255
HepG2 Function Assay 50-500 μM 60?min inhibits the IL-6-induced phosphorylation of STAT1 (Tyr705) and STAT3 (Tyr705) in a dose-dependent manner 24242046
EJ Function Assay 50/80 μM 48 h downregulates c-Myc, cyclinD1, survivin and VEGF expressions 24587049
EJ Growth Inhibition Assay 50/80 μM 48 h causes S-phase arrest 24587049
EJ Growth Inhibition Assay 50/80 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 24587049
HSC? Function Assay 20 μM 1 h abrogates the differential effects of leptin or AGEs 24614199
NRK-52E Function Assay 1?μM 10 min blocks Ang II induced CD24 expression 24710423
NRK-52E Function Assay 1?μM 10 min blocks the stimulatory effect of Ang II on Pax-2 expression? 24710423
GL37? Cell Viability Assay 0-10?μM 48 h suppresses La expression 24999657
TRPM2/HEK? Function Assay 10?μM 40?min reduces TRPM2 activation even at high concentrations of H2O2 25179574
U937? Function Assay 0.1–25?μM 15?min reduces H2O2-induced Ca2+increase in a concentration-dependent manner, and the IC50?value was 0.4?μM 25179574
TRPM2/HEK? Function Assay 0.1–25?μM 15?min reduces H2O2-induced Ca2+increase in a concentration-dependent manner, and the IC50?value was 1.7?μM 25179574
B16-F0 Function Assay 50/100?μM 48 h reduces anoikis resistance 25216522
SK-MEL-2 Function Assay 50/100?μM 48 h reduces anoikis resistance 25216522
SK-MEL-5 Function Assay 50/100?μM 48 h reduces anoikis resistance 25216522
MeWo Function Assay 50/100?μM 48 h reduces anoikis resistance 25216522
SK-MEL-28 Function Assay 50/100?μM 48 h reduces anoikis resistance 25216522
BCBL1 Function Assay 100?μM 24 h induces a complete autophagic flux? 26184999
BC3 Function Assay 100?μM 24 h induces a complete autophagic flux? 26184999
BCBL1 Function Assay 100?μM 24 h mediates de-phosphorylation of STAT3 correlated with HSP70 and HSF2 reduction 26184999
BC3 Function Assay 100?μM 24 h mediates de-phosphorylation of STAT3 correlated with HSP70 and HSF1 reduction 26184999
BCBL1 Function Assay 100?μM 24 h mediates PEL cell apoptosis 26184999
BC3 Function Assay 100?μM 24 h mediates PEL cell apoptosis 26184999
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生物活性

產(chǎn)品描述 AG-490是一種EGFR抑制劑,在無細(xì)胞試驗(yàn)中IC50為0.1 μM,作用于EGFR比作用于ErbB2選擇性高135倍,對(duì)JAK2也有抑制作用,對(duì)Lck,Lyn,Btk,Syk和Src沒有抑制活性。
靶點(diǎn)
JAK2 (V617F) [8] EGFR [1]
(Cell-free assay)
0.1 μM
體外研究(In Vitro)
體外研究活性

AG-490抑制EGF依賴的HER 14細(xì)胞增殖,IC50為3.5 μM。[1] 與特異性作用于前B細(xì)胞急性白血?。ˋLL)細(xì)胞抑制組成型激活的JAK2 相一致,5 μM AG-490通過誘導(dǎo)程序性細(xì)胞死亡,幾乎完全抑制所有ALL 細(xì)胞生長,而對(duì)正常造血功能不會(huì)造成有害影響。AG-490不會(huì)抑制Lck, Lyn, Btk, Syk, 和 Src激活。[2]AG-490 (60-100 μM) 抑制Stat3sm組成型激活,且抑制自發(fā)的或白細(xì)胞介素2誘導(dǎo)的蕈菌(MF)腫瘤細(xì)胞生長 ,IC50分別為75 μM和 20 μM。[3]通過抑制JAK3和 STAT5a/b.的活性,AG-490有效抑制IL-2調(diào)節(jié)的人 T 細(xì)胞生長, IC50 為 25 μM。[4] AG-490 作用于MOPC, MPC11, 和S194細(xì)胞 ,顯著抑制Stat3 組成型激活,導(dǎo)致顯著的細(xì)胞凋亡,這種作用存在劑量依賴性。[6] AG-490 (100 μM) 抑制Akt磷酸化, 抑制核因子-κB激活, 且激活GSK-3β,導(dǎo)致c-Myc降低。AG-490 (50 μM)可以誘導(dǎo)表達(dá)Bcr-Abl 突變型T315I 和E255K 的BaF3細(xì)胞凋亡。[7] 30 μM AG-490 不僅抑制Epo誘導(dǎo)的野生型JAK2磷酸化,也抑制 組成型的JAK2 V617F突變型磷酸化。AG-490作用于BaF3細(xì)胞,有效抑制JAK 2 V617F 突變誘導(dǎo)的細(xì)胞因子非依賴的細(xì)胞生長。[8]

激酶實(shí)驗(yàn) 體外激酶自磷酸化檢測(cè)
AG-490溶于DMSO 10%-H2O-乙醇 45%。原油膜提取物 (0.125 μg/mL)與EGF (20 nM) 在50 mM HEPES buffer, pH 7.6, 和125 mM NaCl中在 4oC下預(yù)溫育15分鐘。在V形 96孔板上進(jìn)行 EGFR 或 ErbB2激酶自磷酸化活性檢測(cè),在4oC 進(jìn)行30分鐘。在含反應(yīng)混合物(12 μL, 50mM, HEPES, pH 7.4,125 mM NaCl, 12 mM M8Ac2, 2 mM MnCl2, 1 mM NaVO3, 1 μM ATP, 及1 μCi[γ-32P]ATP,) 及濃度不斷增高的AG-490 (4 μL)的每孔中加入膜抽提物(8 μL)。加入熱樣本緩沖液終止反應(yīng),樣本在6% SDS-聚丙烯酰胺凝膠電泳微小膠體上跑膠,然后烘干凝膠,在線性處理時(shí)間進(jìn)行自顯影。掃描受體帶,然后通過Ez-Fit 程序分析結(jié)果。 為了分析 JAK2, JAK2的自磷酸化,使用從G2期細(xì)胞得到的裂解物抗JAK2抗體,進(jìn)行免疫沉淀,與濃度不斷增高的AG-490(0-50 μM)預(yù)處理16小時(shí)。免疫復(fù)合物與抗磷酸抗體進(jìn)行免疫印跡。通過測(cè)量JAK2自磷酸化而測(cè)定對(duì)體外激酶活性的抑制情況。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 Pre-B ALL
濃度 溶于DMSO, 終濃度為~ 50 μM
孵育時(shí)間 16小時(shí)
方法

使用不同濃度AG-490 處理細(xì)胞16小時(shí)。為了測(cè)定細(xì)胞增殖,加入[3H]胸甘(1 μCi) 培養(yǎng),6小時(shí)或更長時(shí)間以后終止培養(yǎng)。收集細(xì)胞,樣本在液體閃爍計(jì)數(shù)器上計(jì)數(shù)。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性

AG-490處理,大幅降低 CD45+和HLA-DR+ 細(xì)胞數(shù),作用于骨髓時(shí),這兩種細(xì)胞數(shù)分別從48% 和46%降低到不可檢測(cè)水平,作用于未處理小鼠脾臟時(shí),這兩種細(xì)胞數(shù)分別從 38%和 22% 降低到不可檢測(cè)水平。[2] 在體內(nèi),AG-490 處理,引起小鼠骨髓瘤細(xì)胞凋亡,但是不抑制IL-12誘導(dǎo)的巨噬細(xì)胞活化和IFN-γ產(chǎn)量。[6]與在體外抑制 JAK2 V617F 突變活性一致,AG-490每天按0.5 mg處理裸鼠 10天,高效抑制JAK2 V617F突變誘導(dǎo)的腫瘤形成和腫瘤細(xì)胞入侵。[8]

動(dòng)物實(shí)驗(yàn) Animal Models 靜脈注射ALL 細(xì)胞的SCID小鼠
Dosages 每天0.85 mg + 0.5 mg
Administration 持續(xù)輸液泵輸液加之以每天腹腔注射

化學(xué)信息&溶解度

分子量 294.30 分子式

C17H14N2O3

CAS號(hào) 133550-30-8 SDF Download AG-490 SDF
Smiles C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次:

DMSO : 58 mg/mL ( (197.07 mM) ;DMSO吸濕會(huì)降低化合物溶解度,請(qǐng)使用新開封DMSO)

Ethanol : 9 mg/mL (30.58 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

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)過程中的損耗,建議多配一只動(dòng)物的藥量)

mg/kg g μL

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,:如該濃度超過該批次藥物DMSO溶解度,請(qǐng)先聯(lián)系Selleck);

體內(nèi)配方配制方法: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: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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常見問題及建議解決方法

問題 1:
I would like to know whether AG490 (S1143) goes to CNS through BBB, or not?

回答:
AG-490 can go through the BBB. You can see this reference: http://bloodjournal.hematologylibrary.org/content/111/4/2062.full.html.

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