AC480 (BMS-599626)

Short Summary : HER1/2 inhibitor,selective and efficacious

Category : JAK/STAT Signaling|EGFR

Purity : 0.98

CAS Number : 714971-09-2

Formula : C27H27FN8O3.HCl

Molecular Weight : 567.01

SMILE : CC1=C2C(=NC=NN2C=C1NC(=O)OCC3COCCN3)NC4=CC5=C(C=C4)N(N=C5)CC6=CC(=CC=C6)F

Solubility : >28.4mg/mL in DMSO

Storage : Store at -20°C

Description : 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, nonCsmall-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 nonCsmall-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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