SAR439859
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MedKoo CAT#: 206998

CAS#: 2114339-57-8

Description: SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD SAR439859 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells


Chemical Structure

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SAR439859
CAS# 2114339-57-8

Theoretical Analysis

MedKoo Cat#: 206998
Name: SAR439859
CAS#: 2114339-57-8
Chemical Formula: C31H30Cl2FNO3
Exact Mass: 553.1587
Molecular Weight: 554.4834
Elemental Analysis: C, 67.15; H, 5.45; Cl, 12.79; F, 3.43; N, 2.53; O, 8.66

Price and Availability

Size Price Availability Quantity
50.0mg USD 1250.0 2 Weeks
100.0mg USD 1850.0 2 Weeks
200.0mg USD 2650.0 2 Weeks
500.0mg USD 4650.0 2 Weeks
1.0g USD 5950.0 2 Weeks
2.0g USD 10950.0 2 Weeks
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Synonym: Amcenestrant, SAR439859; SAR-439859; SAR 439859;

IUPAC/Chemical Name: 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid

InChi Key: KISZAGQTIXIVAR-VWLOTQADSA-N

InChi Code: InChI=1S/C31H30Cl2FNO3/c32-23-8-12-27(29(33)18-23)28-4-1-3-21-17-22(31(36)37)7-11-26(21)30(28)20-5-9-24(10-6-20)38-25-13-16-35(19-25)15-2-14-34/h5-12,17-18,25H,1-4,13-16,19H2,(H,36,37)/t25-/m0/s1

SMILES Code: O=C(C1=CC=C2C(CCCC(C3=CC=C(Cl)C=C3Cl)=C2C4=CC=C(O[C@@H]5CN(CCCF)CC5)C=C4)=C1)O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 554.4834 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: El-Ahmad Y, Tabart M, Halley F, Certal V, Thompson F, Filoche-Rommé B, Gruss-Leleu F, Muller C, Brollo M, Fabien L, Loyau V, Bertin L, Richepin P, Pilorge F, Desmazeau P, Girardet C, Beccari S, Louboutin A, Lebourg G, Le-Roux J, Terrier C, Vallée F, Steier V, Mathieu M, Rak A, Abecassis PY, Vicat P, Benard T, Bouaboula M, Sun F, Shomali M, Hebert A, Levit M, Cheng H, Courjaud A, Ginesty C, Perrault C, Garcia-Echeverria C, McCort G, Schio L. 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. doi: 10.1021/acs.jmedchem.9b01293. [Epub ahead of print] PubMed PMID: 31721572.

SAR439859

50.0mg / USD 1250.0