NSC 721648

GW 610 (NSC 721648), an antitumor agent, shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines[1][2][3].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

GW 610 inhibits the proliferation of MCF-7, MDA 468, KM 12, and HCC 2998 cells, with GI50s of <0.1 nM, <0.1 nM, 290 nM, and 0.25 nM, respectively[1]. GW 610 (0.1-1 μM) induces CYP1A1 mRNA and protein in MDA-MB-468, MCF-7, KM12, and HCC2998 cells, whereas CYP2S1 and CYP2W1 are induced only in breast cancer cells[3]. Western Blot Analysis[3] Cell Line: MDA-MB-468, MCF-7, KM12, and HCC2998 cells Concentration: 0.1, 1 μM Incubation Time: 48 hours Result: Induced CYP1A1 mRNA and protein in all cell lines including KM12 and HCC2998 CRC cells. Induced CYP2S1 and CYP2W1 mRNA and protein expression in MDA-MB-468 and MCF-7 breast cancer cells.

[1]. Mortimer CG, et, al. Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines. J Med Chem. 2006 Jan 12;49(1):179-85.

[2]. Aiello S, et, al. Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648). J Med Chem. 2008 Aug 28;51(16):5135-9.

[3]. Tan BS, et, al. CYP2S1 and CYP2W1 mediate 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW-610, NSC 721648) sensitivity in breast and colorectal cancer cells. Mol Cancer Ther. 2011 Oct;10(10):1982-92.