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GW 583340 dihydrochloride

Names

[ CAS No. ]:
1173023-85-2

[ Name ]:
GW 583340 dihydrochloride

[Synonym ]:
GW583340
GW583340 DIHYDROCHLORIDE
N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[2-({[2-(methylsulfonyl)ethyl]amino}methyl)-1,3-thiazol-4-yl]-4-quinazolinamine dihydrochloride
4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[[[2-(methylsulfonyl)ethyl]amino]methyl]-4-thiazolyl]-, hydrochloride (1:2)
N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[2-({[2-(methylsulfonyl)ethyl]amino}methyl)-1,3-thiazol-4-yl]quinazolin-4-amine dihydrochloride
MFCD07370137
4-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenylamino]-6-[2-[[2-(methylsulfonyl)ethyl]aminomethyl]-4-thiazolyl]quinazoline dihydrochloride

Biological Activity

[Description]:

GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[In Vitro]

GW 583340 dihydrochloride (5 μM) 降低 Mitoxantrone 抑制 ABCG2-482-R2 和 ABCG2-482-T7 细胞系的 IC50 值[1]。 GW 583340 dihydrochloride (2.5 和 7.5 μM，24 小时) 增加 SUM149 和 SUM190 细胞中 ROS 的积累，并诱导细胞凋亡[2]。 GW 583340 dihydrochloride (0-10 μM) 减少 SCCF1 细胞和 CatMC 细胞中的集落形成[2]。

[References]

[1]. Sodani K, et al. GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. Biochem Pharmacol. 2012 Jun 15;83(12):1613-22.  

[2]. Aird KM, et al. ErbB1/2 tyrosine kinase inhibitor mediates oxidative stress-induced apoptosis in inflammatory breast cancer cells. Breast Cancer Res Treat. 2012 Feb;132(1):109-19.  

[3]. Gray ME,et al. Dual targeting of EGFR and ERBB2 pathways produces a synergistic effect on cancer cell proliferation and migration in vitro. Vet Comp Oncol. 2017 Sep;15(3):890-909.  

Chemical & Physical Properties

[ Molecular Formula ]:
C28H27Cl3FN5O3S2

[ Molecular Weight ]:
671.03

[ Exact Mass ]:
669.060486

Related Compounds