AC480 (BMS-599626) (Synonyms: BMS-599626) |
Catalog No.GC13257 |
AC480(BMS-599626)(AC480)은 선택적이고 경구 생체이용 가능한 HER1 및 HER2 억제제이며 IC50은 각각 20 및 30 nM입니다. AC480(BMS-599626)은 HER4(IC50=190nM)에 대해 ~8배 덜 강력하고 VEGFR2, c-Kit, Lck, MEK에 대해 100배 이상 강력합니다. AC480(BMS-599626)은 종양 세포 증식을 억제하고 방사선 요법에 대한 종양 반응을 증가시킬 가능성이 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 714971-09-2
Sample solution is provided at 25 µL, 10mM.
AC480 (BMS-599626) is a potent, selective inhibitor of human epidermal growth factor receptor (HER) that inhibits HER1 and HER2 with IC values of 20 nM and 30 nM, respectively. AC480 has been proved to inhibit HER1 in an ATP-competitive manner. On the contrary, AC480 has shown to be an ATP noncompetitive inhibitor of HER2 [1]
AC480 inhibited the proliferation of Sal2 cells derived from a transgenic mouse tumor, breast tumor and gastric carcinoma cell lines, GEO colon tumor cells, non–small-cell lung tumor cells line via HER1 and/or HER2 signalings [1].
AC480 by oral administration has been demonstrated to suppress the growth of Sal2 tumor, GEO xenograft tumor, KPL-4 and BT474 breast tumors, N87 gastric tumor, A549 and L2987 non–small-cell lung tumors in nude mice [1].
References:
[1] Wong TW1, Lee FY, Yu C, Luo FR, Oppenheimer S, Zhang H, Smykla RA, Mastalerz H, Fink BE, Hunt JT,Gavai AV, Vite GD. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93.
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