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AG-1478EGFR inhibitor,potent and selective

AG-1478

Catalog No. A8357
Size Price Stock Qty
10mM (in 1mL DMSO) $50.00 In stock
5mg $50.00 In stock
25mg $150.00 In stock
50mg $250.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

AG-1478

Related Biological Data

AG-1478
AG1478, an inhibitor of EGFR, decreased the expression level of EGFR as shown in the figure.
Method:Western Blot; Cell Lines:EA.hy926; Concentration:100 μM; Incubation Time:24 h.

Biological Activity

Description AG-1478 (Tyrphostin AG-1478) is a selective inhibitor of EGFR with an IC50 values of 3 nM.
Targets EGFR HER2 PDGFR      
IC50 3 nM >100 μM >100 μM      

Protocol

Cell experiment [1]:

Cell lines

Human hepatocellular carcinoma HA22T/VGH cell line

Preparation method

Soluble in DMSO > 15.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

6.25, 12.5, 25μM; 24hr

Applications

Tyrphostin AG-1478, a potent and specific inhibitor of EGFR (Epidermal Growth Factor Receptor) tyrosine kinase, plays a key role in the control of normal cellular growth and abnormal cell proliferation. Tyrphostin AG-1478 shows an enhanced in vitro anti-tumor activity in HA22T/VGH cells when entrapmented into NLC(nanostructured lipid carriers) systems compared to free drug.

Animal experiment [2]:

Animal models

Male C57BL/6 mice aged 8 weeks, male ApoE-/- mice aged 8 weeks

Dosage form

10 mg/kg/day, 8 weeks, oral gavage

Application

Administration of AG1478 significantly reduced myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Bondì ML1, Azzolina A, et al, Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells. J Nanobiotechnology, 2014. 12(21): p. 1477-3155.

[2]. Li W1,2, Fang Q1, EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580. doi: 10.1038/srep24580.

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Chemical Properties

Cas No. 153436-53-4 SDF Download SDF
Synonyms Tyrphostin AG-1478; AG 1478; NSC 693255; AG1478
Chemical Name N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine
Canonical SMILES COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC
Formula C16H14ClN3O2 M.Wt 315.75
Solubility >15.8mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

AG-1478 is an inhibitor of EGFR which acts on EGF-stimulated Erk1/2 phosphorylation with IC50 value of 10 uM using ovarian cell line Ishikawa [1].
EGFR (epidermal growth factor receptor) belongs to human HER-1 family, which is a cell surface receptor and recognized by EGF-family (epidermal growth factor family). Many studies have shown that EGFR is over-expressed in a variety of solid tumors and its over-expression means bad prognosis for cancer patients [1]. AG1478 works as EGFR kinase inhibitor through blocking EGFR phosphorylation and superoxide anion production [2].
Treating human hepatocellular carcinoma HA22T/VGH cells could reduce its anti-tumor activity compared with control group [3]. When tested with ovarian cancer cell lines CAOV-3 or SKOV-3, EGFR signaling was diminished [4]. When human colorectal SW480 was treated with AG-1478, both EGFR phosphorylation and cell proliferation were reduced [5].
In nu/nu mice model with CAOV-3 cells xenografted, treatment with AG-1478 could diminish EGFR phosphorylation thus limited the growth of tumor [4].
Gong XD, et al. had shown that AG-1478 also could reduce the expression of FOXM1 via FOXO3a using a NSCLC cell lines A549, and the A549 cells showed increased chemosensitivity[6].
References:
1.Takai, N., et al., Synergistic anti-neoplastic effect of AG1478 in combination with cisplatin or paclitaxel on human endometrial and ovarian cancer cells. Mol Med Rep, 2010. 3(3): p. 479-84.
2.D'Anneo, A., et al., Parthenolide induces superoxide anion production by stimulating EGF receptor in MDA-MB-231 breast cancer cells. Int J Oncol, 2013. 43(6): p. 1895-900.
3.Bondi, M.L., et al., Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells. J Nanobiotechnology, 2014. 12(21): p. 1477-3155.
4.Yu, Y., et al., Synergistic effects of combined platelet-activating factor receptor and epidermal growth factor receptor targeting in ovarian cancer cells. J Hematol Oncol, 2014. 7(1): p. 1756-8722.
5.Yagublu, V., et al., Combination of the EGFR tyrosine kinase inhibitor AG1478 and 5-FU: no synergistic effect on EGFR phosphorylation, cell proliferation and apoptosis induction. Anticancer Res, 2013. 33(9): p. 3753-8.
6.Gong, X.D., et al., [Effects of AG1478 on the expression of FOXM1 gene via FOXO3a in non-small cell lung cancer cells]. Zhonghua Zhong Liu Za Zhi, 2013. 35(8): p. 572-8.