Bexirestrant

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Bexirestrant 

Bexirestrant 是一种具有口服活性的 ER-α 降解剂。Bexirestrant 可用于抗雌激素、抗肿瘤的研究。

Bexirestrant

Bexirestrant Chemical Structure

CAS No. : 2505067-70-7

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生物活性

Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic[1][2].

体外研究
(In Vitro)

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[1].
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[1].
Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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]：

Tmax (h) Cmax (ng/mL) AUClast (hr× ng/mL) AUCinf_obs (hr×ng/mL) T1/2 (h)
4.00 343 7582 9804 26

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

477.52

Formula

C29H26F3NO2
CAS 号

2505067-70-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ranjan Kumar Pal, et al, Selective estrogen receptor degrader. WO2021014386 A1.

    [2]. WHO Drug Information, Vol. 35, No. 4, 2021. Geneva: World Health Organization; 2022.

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