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CAS No. : 496794-70-8
MCE 国际站:HhAntag
产品活性:HhAntag 是一种特异性、强效、具有口服活性的 Hh 通路的 SMO 拮抗剂。
研究领域:Stem Cell/Wnt
作用靶点:Smo
In Vitro: HhAntag (2-30 µM; 72 hours) demonstrates to be 10-times more potent than the natural product SMO antagonist, cyclopamine, at inhibiting Hh pathway activity and it inhibits Hh signalling pathway sensitivitive cells with IC50 values ranging from 2 µM to >30 µM.HhAntag inhibits AsPC-1, BXPC-3, CFPAC, HPAC, HPAF-II, KP4, Panc 03.27, PA-TU-8902, PSN-1, SU.86.86 cells with IC50 values of 30 µM, 5.4 µM, 5.8 µM, 2.7 µM, 6.2 µM,10.3 µM, 2.5 µM, 2.9 µM, 5.8 µM and 2.7 µM, respectively.HhAntag (100 nM) is needed to completely inhibit Hh signalling in a Hh-responsive human mesenchymal cell line (HEPM) expressing a GLI luciferase reporter construct (HEPM-rep), the IC50 of 5 nM 400-times lower than that required to inhibit cell growth by 50% in the most sensitive cancer cell line (1.9 μM).
In Vivo: HhAntag (oral administraion; 75 mg/kg or 100 mg/kg; twice daily; 25 days) results in significant growth delay in HT55 and HT-29 colorectal cell line xenografts models, with average tumour growth inhibitions of 29% and 48%, respectively. Whereas HhAntag had no effect on the growth of DLD-1 xenografts.
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