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编 号：F753455
分子式：C29H26F3NO2
分子量：477.52
分子式：C29H26F3NO2
分子量：477.52
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CAS No: 2505067-70-7
产品详情
生物活性：
Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.
体内研究：
Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft.Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose：Tmax (h)Cmax (ng/mL)AUClast (hr× ng/mL)AUCinf_obs (hr×ng/mL)T1/2 (h)
4.003437582980426
Animal Model:Female athymic nude mice harboring subcutaneous MCF7-Y537S xenograft
Dosage:50mg/kg
Administration:p.o. for 28 days
Result:Showed 56% tumor growth inhibition compared to vehicle group after 28 days.
体外研究：
Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 6.0, 2.2 nM, respectively.Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 19.6, 12.7 nM, respectively.Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM.
Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.
体内研究：
Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft.Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose：Tmax (h)Cmax (ng/mL)AUClast (hr× ng/mL)AUCinf_obs (hr×ng/mL)T1/2 (h)
4.003437582980426
Animal Model:Female athymic nude mice harboring subcutaneous MCF7-Y537S xenograft
Dosage:50mg/kg
Administration:p.o. for 28 days
Result:Showed 56% tumor growth inhibition compared to vehicle group after 28 days.
体外研究：
Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 6.0, 2.2 nM, respectively.Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 19.6, 12.7 nM, respectively.Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM.
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