Chemical Structure
SAR439859, inhibitor
SAR439859
Purity
0.9813
Synonyms
SAR439859; inhibitor
Purity/Purification
0.9813
Form/Format
Solid
Solubility
DMSO: 125mg/mL (225.44mM)
Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
SMILES
C1CC2=C(C=CC(=C2)C(=O)O)C(=C(C1)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)O[C@H]5CCN(C5)CCCF
Formula
C31H30Cl2FNO3
Target & IC50
ERalpha
In vitro
SAR439859(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]. 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].
CAS Number
2114339-57-8
Preparation and Storage
Store at 0-4 degree C for short term (days to weeks), or -20 degree C for long term (months).
Chemical Structure
Chemical Structure
Related Product Information for SAR439859, inhibitor
SAR439859 is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 for ERalpha degradation).
Product Categories/Family for SAR439859, inhibitor
References
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.
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
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
Similar Products
Product Notes
The SAR439859 (Catalog #AAA5764630) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "SAR439859, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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