AC480 (BMS-599626) (Synonyms: BMS-599626) |
| カタログ番号GC13257 |
AC480 (BMS-599626) (AC480) は、選択的かつ経口的に生物学的に利用可能な HER1 および HER2 阻害剤であり、IC50 はそれぞれ 20 および 30 nM です。 AC480 (BMS-599626) は、HER4 (IC50=190 nM) に対しては最大 8 倍、VEGFR2、c-Kit、Lck、MEK に対しては >100 倍の効力を示します。 AC480 (BMS-599626) は腫瘍細胞の増殖を阻害し、放射線療法に対する腫瘍の反応を高める可能性があります。
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Cas No.: 714971-09-2
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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