Amcenestrant
Based on 4 publication(s) in Google Scholar
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER+ breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.79%
- CAS No.: 2114339-57-8
- Formula: C31H30Cl2FNO3
- Molecular Weight:554.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Anti-Cancer Compound Library
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Publications Citing Use of MedChemExpress (MCE) Amcenestrant
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Biological Activity
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ERα 0.2 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | EC50 |
0.2 nM
Compound: 43d; SAR439859
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Induction of ERalpha degradation in human MCF7 cells incubated for 4 hrs by Alexafluor-488 conjugate anti-rabbit antibody/Syto-64 staining based immunofluorescence analysis
Induction of ERalpha degradation in human MCF7 cells incubated for 4 hrs by Alexafluor-488 conjugate anti-rabbit antibody/Syto-64 staining based immunofluorescence analysis
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[PMID: 31721572] |
| MCF7 | EC50 |
20 nM
Compound: 13; SAR439859
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Anti-proliferative activity against wild type human MCF7 cells assessed as reduction in cell growth by CellTiter-Glo assay
Anti-proliferative activity against wild type human MCF7 cells assessed as reduction in cell growth by CellTiter-Glo assay
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[PMID: 37377342] |
| MCF7 | EC50 |
331 nM
Compound: 13; SAR439859
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Anti-proliferative activity against human MCF7 cells harboring ERalpha Y537S mutant assessed as reduction in cell growth by CellTiter-Glo assay
Anti-proliferative activity against human MCF7 cells harboring ERalpha Y537S mutant assessed as reduction in cell growth by CellTiter-Glo assay
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[PMID: 37377342] |
| MCF7 | EC50 |
595 nM
Compound: 13; SAR439859
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Anti-proliferative activity against human MCF7 cells harboring ERalpha D538G mutant assessed as reduction in cell growth by CellTiter-Glo assay
Anti-proliferative activity against human MCF7 cells harboring ERalpha D538G mutant assessed as reduction in cell growth by CellTiter-Glo assay
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[PMID: 37377342] |
| MCF7 | IC50 |
9.1 nM
Compound: SAR439859; 13
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 6 days by cell titre glo luminescence assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 6 days by cell titre glo luminescence assay
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[PMID: 35357160] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nu/nu mouse with MCF7 tumor xenograft model[1]
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Dosage:2.5, 5, 12.5, 25 mg/kg
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Administration:Orally; twice daily for 30 days
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Result:Exhibited substantial tumor-growth inhibition and displayed tumor regression at the dose of 25 mg/kg/BID.
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Animal Model:Mouse, rat and dog[1]
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Dosage:3 mg/kg (iv) and 10 mg/kg (po) (Pharmacokinetic Analysis)
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Administration:Iv or po
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2114339-57-8
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Appearance Solid
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Molecular Weight 554.48
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Formula C31H30Cl2FNO3
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Color White to off-white
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SMILES
O=C(C1=CC=C(C(C2=CC=C(O[C@@H]3CN(CCCF)CC3)C=C2)=C(C4=CC=C(Cl)C=C4Cl)CCC5)C5=C1)O
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Synonyms
SAR439859
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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bioRxiv
Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer Cells. [Abstract]2024 Jun 2:2024.05.28.596307. PMID: 38854123 -
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Solvent & Solubility
DMSO : 83.33 mg/mL (150.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 8.33 mg/mL (15.02 mM); Clear solution
This protocol yields a clear solution of ≥ 8.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (83.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 8.33 mg/mL (15.02 mM); Clear solution
This protocol yields a clear solution of ≥ 8.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (83.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8035 mL | 9.0175 mL | 18.0349 mL | 45.0873 mL |
| 5 mM | 0.3607 mL | 1.8035 mL | 3.6070 mL | 9.0175 mL | |
| 10 mM | 0.1803 mL | 0.9017 mL | 1.8035 mL | 4.5087 mL | |
| 15 mM | 0.1202 mL | 0.6012 mL | 1.2023 mL | 3.0058 mL | |
| 20 mM | 0.0902 mL | 0.4509 mL | 0.9017 mL | 2.2544 mL | |
| 25 mM | 0.0721 mL | 0.3607 mL | 0.7214 mL | 1.8035 mL | |
| 30 mM | 0.0601 mL | 0.3006 mL | 0.6012 mL | 1.5029 mL | |
| 40 mM | 0.0451 mL | 0.2254 mL | 0.4509 mL | 1.1272 mL | |
| 50 mM | 0.0361 mL | 0.1803 mL | 0.3607 mL | 0.9017 mL | |
| 60 mM | 0.0301 mL | 0.1503 mL | 0.3006 mL | 0.7515 mL | |
| 80 mM | 0.0225 mL | 0.1127 mL | 0.2254 mL | 0.5636 mL | |
| 100 mM | 0.0180 mL | 0.0902 mL | 0.1803 mL | 0.4509 mL |
Amcenestrant Related Classifications
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