|N-(3-氯苯基)-6,7-二甲氧基喹唑啉-4-胺|CsnPharm

CAS No.: 153436-53-4

N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine Catalog No. CSN12358

Synonyms: Tyrphostin AG-1478;NSC 693255

AG-1478 selectively inhibits EGFR with IC50 of 3 nM in cell-free assay.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:3nM
描述Epidermal growth factor (EGF) is a well-known growth factor that promotes cancer progression. EGF stimulates cancer growth through the EGFR receptor (EGFR) pathway. Most of cancer tissues are shown to overexpress EGFR, and EGF-EGFR axis has been considered an attractive target for cancer treatment. Indeed, EGFR-tyrosine kinase inhibitors (EGFR-TKIs) have been developed and clinically used in patients with malignancy. EGFR-TKI effectively blocks the EGFR pathway via suppression of EGFR phosphorylation and can therefore inhibit the growth of cancer cells dramaticallyIshiguro Y, Ishiguro H, Miyamoto H. Epidermal growth factor receptor tyrosine kinase inhibition up-regulates interleukin-6 in cancer cells and induces subsequent development of interstitial pneumonia. Oncotarget. 2013 Apr;4(4):550-9. doi: 10.18632/oncotarget.939. PMID: 23592411; PMCID: PMC3720603.|https://pubmed.ncbi.nlm.nih.gov/23592411/}. The quinazoline AG 1478 have been shown to selectively inhibit EGF receptor tyrosine kinase activity in vitro as compared to a variety of tyrosine kinases, including the closely related HER-2/Neu receptor. The IC₅₀s are 0.0020 μM, 2.6 μM, > 100 μM, and >100 μM for EGFR/HER-1 HER-2/neu Insulin-R and c-src, respectively{{Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997 Jun 30;410(2-3):187-90. doi: 10.1016/s0014-5793(97)00580-2. PMID: 9237626.|https://pubmed.ncbi.nlm.nih.gov/9237626/. In vitro study, AG1478 (1 or 10 mg/kg) was intraperitoneally injected to OVA-induced mice at 1 h before the intranasal challenge with OVA, it was showed that AG-1478 significantly and dose-dependently inhibited OVA-induced goblet cell metaplasia, mucus production and infiltration of eosinophils and neutrophils^[3]. Cells were pre-treated with AG1478 antibody before EGF treatment, EGFR phosphorylation was inhibited especially in HSC-3. AG1478 also inhibited phosphorylation of STAT3, Akt, and MAPK induced by EGF. These results suggested that EGFR-TK antibody decreased cell growth via inhibiting EGF phosphorylation^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A431	~10 μM	Kinase assay	-	inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR	10702262
A431	~10 μM	Function assay	-	induces cell cycle arrest	10702262
CNE2	100 μM	Growth inhibitory assay	-	inhibits cell proliferation by 98.4%	11410322

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参考文献

[1] Lee FT, Mountain AJ, et al. Enhanced efficacy of radioimmunotherapy with 90Y-CHX-A''-DTPA-hu3S193 by inhibition of epidermal growth factor receptor (EGFR) signaling with EGFR tyrosine kinase inhibitor AG1478. Clin Cancer Res. 2005 Oct 1;11(19 Pt 2):7080s-7086s.
[2] Han Y, et al. Cancer Res, 1996, 56(17), 3859-3861.
[3] Shimizu S, Takezawa-Yasuoka K, Ogawa T, Tojima I, Kouzaki H, Shimizu T. The epidermal growth factor receptor inhibitor AG1478 inhibits eosinophilic inflammation in upper airways. Clin Immunol. 2018 Mar;188:1-6. doi: 10.1016/j.clim.2017.11.010. Epub 2017 Nov 26. PMID: 29183867.
[4] Ishiguro Y, Ishiguro H, Miyamoto H. Epidermal growth factor receptor tyrosine kinase inhibition up-regulates interleukin-6 in cancer cells and induces subsequent development of interstitial pneumonia. Oncotarget. 2013 Apr;4(4):550-9. doi: 10.18632/oncotarget.939. PMID: 23592411; PMCID: PMC3720603.

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
- 3.1670 mL
- 15.8351 mL
- 31.6702 mL
- 5 mM
- 0.6334 mL
- 3.1670 mL
- 6.3340 mL
- 10 mM
- 0.3167 mL
- 1.5835 mL
- 3.1670 mL

技术信息

CAS号

153436-53-4

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14ClN3O2

运输

蓝冰

分子量

315.75

别名

Tyrphostin AG-1478;NSC 693255

溶解度

DMSO	25.0 mg/mL (79.2 mM)
Water	Insoluble
Ethanol	12.0 mg/mL (38.0 mM)

动物实验配方

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A431	~10 μM	Kinase assay	-	inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR	10702262
A431	~10 μM	Function assay	-	induces cell cycle arrest	10702262
CNE2	100 μM	Growth inhibitory assay	-	inhibits cell proliferation by 98.4%	11410322
CNE2	~100 μM	Kinase assay	-	inhibits EGFR tyrosine phosphorylation	11410322
CNE2	~100 μM	Function assay	-	Inhibits MAPK and AKT activation	11410322
CNE2	~50 μM	Function assay	-	affects cell cycle distribution	11410322
H508	~1 μM	Growth inhibitory assay	-	mitigates CPF-mediated H508 cell growth	26514924
HEp-2	~10 μM	Growth inhibitory assay	-	enhances oridonin-induced growth-inhibitory	20202741
HEp-2	~10 μM	Function assay	-	enhances Oridonin-induced Bax activation, Bcl-2 degradation and SIRT1 inactivation	20202741
HPV 16-immortalized human keratinocytes	~50 μM	Growth inhibitory assay	-	inhibits cell growth	9288782
HPV 16-immortalized human keratinocytes	~50 μM	Function assay	-	induces arrest in the Cell Cycle	9288782
HPV 16-immortalized human keratinocytes	~50 μM	Apoptosis assay	-	induces apoptosis.	9288782
HSC-2	8 μM	Kinase assay	-	inhibits phosphorylation of EGFR and Akt	17689285
HSC-2	8 μM	Apoptosis assay	-	inhibits Fas-mediated apoptosis	17689285
MDA-468	~10 μM	Kinase assay	-	inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR	10702262
MDA-MB-231	~5 μM	Kinase assay	-	inhibits EGF stimulated phosphorylation of FKHR	11030146
SubG1	~10 μM	Apoptosis assay	-	enhances oridonin-induced apoptosis	20202741
U87MG	~100 μM	Growth inhibitory assay	-	IC50=34.6 μM	8752145
U87MG	~100 μM	Kinase assay	-	inhibits EGFR tyrosine kinase activity	8752145
U87MG.wtEGFR.	~100 μM	Growth inhibitory assay	-	IC50=48.4 μM	8752145
U87MG.wtEGFR.	~100 μM	Kinase assay	-	inhibits EGFR tyrosine kinase activity	8752145
U87MG.ΔEGFR	~100 μM	Growth inhibitory assay	-	IC50=8.7 μM	8752145
U87MG.ΔEGFR	~100 μM	Kinase assay	-	inhibits EGFR tyrosine kinase activity	8752145

N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine Catalog No. CSN12358

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