|AG-1478EGFR inhibitor,potent and selective|
Sample solution is provided at 25 µL, 10mM.
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|Description||AG-1478 (Tyrphostin AG-1478) is a selective inhibitor of EGFR with an IC50 values of 3 nM.|
|IC50||3 nM||>100 μM||>100 μM|
|Cas No.||153436-53-4||SDF||Download SDF|
|Synonyms||Tyrphostin AG-1478; AG 1478; NSC 693255; AG1478|
|Solubility||>15.8mg/mL in DMSO||Storage||Store at -20°C|
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 .
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 . AG1478 works as EGFR kinase inhibitor through blocking EGFR phosphorylation and superoxide anion production .
Treating human hepatocellular carcinoma HA22T/VGH cells could reduce its anti-tumor activity compared with control group . When tested with ovarian cancer cell lines CAOV-3 or SKOV-3, EGFR signaling was diminished . When human colorectal SW480 was treated with AG-1478, both EGFR phosphorylation and cell proliferation were reduced .
In nu/nu mice model with CAOV-3 cells xenografted, treatment with AG-1478 could diminish EGFR phosphorylation thus limited the growth of tumor .
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.
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.