SAR439859 (Synonyms: SAR439859) |
| رقم الكتالوجGC61267 |
SAR439859 (المركب 43d) عبارة عن مادة فعالة عن طريق الفم وغير سترويدية وانتقائية لمستقبلات هرمون الاستروجين (SERD). SAR439859 هو مناهض ER قوي وله نشاط مهين ER مع EC50 من 0.2 نانومتر لـ ERα ؛ انحلال. يُظهر SAR439859 فعالية قوية ضد الأورام ومقاومة محدودة في سرطان الثدي ER+.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2114339-57-8
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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]
[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.
| Cas No. | 2114339-57-8 | SDF | |
| المرادفات | SAR439859 | ||
| Canonical 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 | ||
| Formula | C31H30Cl2FNO3 | M.Wt | 554.48 |
| الذوبان | DMSO: 125 mg/mL (225.44 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 | 3.607 mL |
| 10 mM | 0.1803 mL | 0.9017 mL | 1.8035 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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