Bexirestrant

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

For research use only. We do not sell to patients.

Bexirestrant Chemical Structure

CAS No. : 2505067-70-7

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
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Description

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

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]：

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

MedChemExpress (MCE) 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.

Molecular Weight

477.52

Formula

C₂₉H₂₆F₃NO₂

CAS No.

2505067-70-7

SMILES

CC1=C(C2=CC(F)=CC(F)=C2)[C@H](C3=CC=C(C=C3)/C=C/CN4CC(C4)CF)OC5=CC(O)=CC=C51

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

Bexirestrant Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bexirestrant2505067-70-7Estrogen Receptor/ERRMCF-7 cellsY537S mutatD538G mutatcancerantiestrogenInhibitorinhibitorinhibit

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