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| 5mg |
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| 25mg |
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Amcenestrant (SAR-439859; SAR439859) is a potent, orally available, and nonsteroidal estrogen receptor degrader (SERD) with potential anticancer activity. It degrades ER with an EC50 of 0.2 nM for ERα degradation.
| ln Vitro |
SAR439859 (compound 43d) exhibits the strongest in vivo anticancer activity against a variety of BC cell lines and patient-derived xenografts, including those with ERα mutations [1].
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| ln Vivo |
At a dose of 25 mg/kg/BID, SAR439859 (Compound 43d; Valve; 2.5–25 mg/kg; twice daily for 30 days) showed a significant reduction in tumor growth [1]. In the largest animal species tested, 3 mg/kg, minimum 10 mg/kg) shows low to moderate clearance (0.03-1.92 L/h?kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good cross-species bioavailability (54-76%). Be aware that the T1/2 time varies depending on the species: 1.98 hours for mice, 4.13 hours for fish, and 9.80 hours for dogs, for example [1].
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| Animal Protocol |
Animal/Disease Models: Nu/nu mouse MCF7 tumor xenograft model [1]
Doses: 2.5, 5, 12.5, 25 mg/kg Doses: Oral;. twice (two times) daily for 30 days Experimental Results: Demonstrated significant tumor growth inhibition and demonstrated tumor regression at a dose of 25 mg/kg/BID. Animal/Disease Models: Mice, rats and dogs [1] Doses: 3 mg/kg (iv) and 10 mg/kg (oral) (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)or oral Experimental Results: In three Shows low to moderate clearance among 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 across species degree (54-76%). |
| References |
[1]. El-Ahmad Y, et al. Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer. J Med Chem. 2019 Nov 27.
[2]. Monsif Bouaboula, et al. Abstract 943: SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer. |
| Molecular Formula |
C₃₁H₃₀CL₂FNO₃
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|---|---|
| Molecular Weight |
554.48
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| CAS # |
2114339-57-8
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| SMILES |
ClC1C([H])=C(C([H])=C([H])C=1C1C([H])([H])C([H])([H])C([H])([H])C2C([H])=C(C(=O)O[H])C([H])=C([H])C=2C=1C1C([H])=C([H])C(=C([H])C=1[H])O[C@@]1([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])F)C1([H])[H])Cl
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| Synonyms |
SAR439859 SAR-439859
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~150.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 8.33 mg/mL (15.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 83.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 8.33 mg/mL (15.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 83.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 8.33 mg/mL (15.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8035 mL | 9.0175 mL | 18.0349 mL | |
| 5 mM | 0.3607 mL | 1.8035 mL | 3.6070 mL | |
| 10 mM | 0.1803 mL | 0.9017 mL | 1.8035 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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