Bexirestrant

Name: Bexirestrant
Brand: TargetMol
SKU: T40166
Price: 773 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T40166Cas号 2505067-70-7

Bexirestrant is an orally active ER-α degrader commonly employed in the research of antiestrogen and antineoplastic therapies.

还可以

产品编号 T40166Cas号 2505067-70-7

Bexirestrant is an orally active ER-α degrader commonly employed in the research of antiestrogen and antineoplastic therapies.

规格	价格	库存	数量
25 mg	¥ 10,600	期货

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产品介绍

生物活性

产品描述	Bexirestrant is an orally active ER-α degrader commonly employed in the research of antiestrogen and antineoplastic therapies.
体外活性	Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC 50 s of 0.3. 6.0, 2.2 nM, respectively[1]. Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC 50 s of 0.3. 19.6, 12.7 nM, respectively[1]. Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM[1].
体内活性	Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft[1]. Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose[1]： T max (h) C max (ng/mL) AUC last (hr× ng/mL) AUC inf_obs (hr×ng/mL) T 1/2 (h) 4.00 343 7582 9804 26 Animal Model: Female athymic nude mice harboring subcutaneous MCF7-Y537S xenograft[1]Dosage: 50mg/kg Administration: p.o. for 28 days Result: Showed 56% tumor growth inhibition compared to vehicle group after 28 days.