产品
编 号：F369270
分子式：C24H23ClN4O3
分子量：450.92
分子式：C24H23ClN4O3
分子量：450.92
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 496794-70-8
产品详情
生物活性：
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
体内研究：
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.Animal Model:Primary human xenografts?in?female CD1 nu/nu mice of 6–8?weeks (DLD-1, HT55 and HT-29 cells)
Dosage:75 mg/kg or 100 mg/kg
Administration:Oral administraion; twice daily; 25 days
Result:Resulted in growth delay of HT55 and HT-29 xenografts, but had no effects on DLD-1 xenografts.
体外研究：
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).
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
体内研究：
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.Animal Model:Primary human xenografts?in?female CD1 nu/nu mice of 6–8?weeks (DLD-1, HT55 and HT-29 cells)
Dosage:75 mg/kg or 100 mg/kg
Administration:Oral administraion; twice daily; 25 days
Result:Resulted in growth delay of HT55 and HT-29 xenografts, but had no effects on DLD-1 xenografts.
体外研究：
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).
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