2114339-57-8
2114339-57-8 structure
- Name: Amcenestrant
- Chemical Name: SAR439859
- CAS Number: 2114339-57-8
- Molecular Formula: C31H30Cl2FNO3
- Molecular Weight: 554.48
- Catalog: Research Areas Cancer
- Create Date: 2020-01-24 00:41:51
- Modify Date: 2024-01-05 05:24:41
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SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation[1]. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer[2].
| Name | SAR439859 |
|---|
| Description | SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation[1]. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer[2]. |
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| Related Catalog | |
| Target |
ERα:0.2 nM (EC50) |
| In Vitro | SAR439859 (compound 43d) induces strong in vivo antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations[1]. |
| In Vivo | SAR439859 (compound 43d; orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID[1]. SAR439859 (3 mg/kg for iv and 10 mg/kg for po) shows a low to moderate clearance in the three animal species tested (0.03-1.92 L/h•kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species. It is noticed that T1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog)[1]. Animal Model: Nu/nu mouse with MCF7 tumor xenograft model[1] Dosage: 2.5, 5, 12.5, 25 mg/kg Administration: Orally; twice daily for 30 days Result: Exhibited substantial tumor-growth inhibition and displayed tumor regression at the dose of 25 mg/kg/BID. Animal Model: Mouse, rat and dog[1] Dosage: 3 mg/kg (iv) and 10 mg/kg (po) (Pharmacokinetic Analysis) Administration: Iv or po Result: Showed a low to moderate clearance in the three animal species tested (0.03-1.92 L/h•kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species. |
| References |
| Density | 1.297±0.06 g/cm3(Predicted) |
|---|---|
| Boiling Point | 676.7±55.0 °C(Predicted) |
| Molecular Formula | C31H30Cl2FNO3 |
| Molecular Weight | 554.48 |
| Storage condition | -20°C |
| Hazard Codes | Xn |
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