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CAS No.: 133550-30-8

酪氨酸激酶抑制剂AG 490 Catalog No. CSN13724

Synonyms: Tyrphostin AG490;Tyrphostin B42;Zinc02557947

AG-490 is a broad-spectrum inhibitor that has several targets including EGFR (IC50 = 2 μM), ErbB2 (IC50 = 13.5 μM), STAT3 and JAK2.

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实验方案

技术信息

生物活性

靶点 EGFR

IC50:0.1μM
描述The epidermal growth factor receptor (EGFR) activates several signaling cascades in response to epidermal growth factor stimulation. One of these signaling events involves tyrosine phosphorylation of signal transducer and activator of transcription (STAT), whereas another involves activation of the phosphatidylinositol 3-OH kinase pathway. Two possibilities for STAT activation exist: a janus kinase (JAK)-dependent and a JAK-independent mechanism^[3]. AG 490 is nephroprotective by inhibiting oxidative stress-related Janus activated kinase-2 (JAK2) activation with IC50s 7 μM and 0.1 μM for JAK2 and EGFR, respectively^[4]. AG490 is used to inhibit phosphorylation of EGFR and signal transducer and activator of STAT-3, and subsequently reduce invasion and adhesion potential of malignant cells^[5]. AG-490 belongs to the tyrphostin family of tyrosine kinase inhibitors, which block protein tyrosine kinases by binding to the substrate-binding site. In a vitro study, EPC2 cells were starved for 48h without EGF and then stimulated with 10 ng/ml EGF for designated time periods at 37°C, washed three times with ice-cold PBS, lysed, and centrifuged for 15 min at 4°C, then 50 μM AG-490 were added during culture. It showed that the AG 490 was the most potent, essentially abolishing migration. Importantly, addition of AG-490 had no effect on the viability of the cells^[3]. In a vivo study, one vial of compound containing 5 mg of AG490 was injected into 5 mice (1 mg/mouse) via intraperitoneal (i.p) route. Mice (4 weeks of age) were treated three times per week for 5 consecutive weeks and were euthanized one week after the last injection at week 10. Concentration of Tyrphostin AG 490 was 10 μM. The result showed that AG490 treatment of young non-diabetic NOD mice significantly reduced blood glucose levels^[6].
作用机制AG-490 blocks protein tyrosine kinases by binding to the substrate-binding site^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
7TD1-DXM	10 μM	Growth Inhibition Assay	72 h	inhibits cell growth	23871159
7TD1-DXM	50 μM	Apoptosis Assay	48 h	induces apoptosis	23871159
7TD1-WD-90	10 μM	Growth Inhibition Assay	72 h	inhibits cell growth	23871159

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3978 mL
- 16.9892 mL
- 33.9784 mL
- 5 mM
- 0.6796 mL
- 3.3978 mL
- 6.7957 mL
- 10 mM
- 0.3398 mL
- 1.6989 mL
- 3.3978 mL

技术信息

CAS号

133550-30-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H14N2O3

运输

蓝冰

分子量

294.30

别名

Tyrphostin AG490;Tyrphostin B42;Zinc02557947

溶解度

DMSO	58.0 mg/mL (197.1 mM)
Water	Insoluble
Ethanol	6.0 mg/mL (20.4 mM)

动物实验配方

5% DMSO+40% PEG300+5% Tween80+50% water

6.25 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

酪氨酸激酶抑制剂AG 490 Catalog No. CSN13724

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