- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: Bexirestrant
- Price: ￥Inquiry/100mg ￥Inquiry/250mg ￥Inquiry/1g
- Purity: 98.0%
- Stocking Period: 10 Day
- Contact: Huang
- DC Chemicals Limited
- China
- Product Name: Bexirestrant
- Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
2505067-70-7
2505067-70-7 structure
- Name: Bexirestrant
- Chemical Name: Bexirestrant
- CAS Number: 2505067-70-7
- Molecular Formula: C29H26F3NO2
- Molecular Weight: 477.52
- Catalog: Research Areas Cancer
- Create Date: 2022-03-27 20:42:52
- Modify Date: 2024-07-20 17:04:17
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Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic[1][2].
| Name | Bexirestrant |
|---|
| Description | Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic[1][2]. |
|---|---|
| Related Catalog | |
| 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]. |
| 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 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. |
| 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. |
| Molecular Formula | C29H26F3NO2 |
|---|---|
| Molecular Weight | 477.52 |