[CAS NO. 2114339-57-8] Amcenestrant (SAR439859)

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PRODUCTS SPECIFICATIONS [2114339-57-8]

Catalog

SLK-S9609

Brand

Selleck

CAS

2114339-57-8

DESCRIPTION [2114339-57-8]

Overview

MDL	-
Molecular Weight	554.48
Molecular Formula	C31H30Cl2FNO3
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

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	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
50 mM	0.0361 mL	0.1803 mL	0.3607 mL

Description

Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent antagonist with EC50 of 0.2 nM for ERα degradation.

Targets

ERα ^[1]
(Cell-free assay)

0.2 nM(EC50)

In vitro

SAR439859 is a novel, orally bioavailable SERD with potent antagonist and degradation activities against both wild-type and mutant Y537S ER. Driven by its fluoropropyl pyrrolidinyl side chain, SAR439859 has demonstrated broader and superior ER antagonist and degrader activities across a large panel of ER+ cells, including inhibition of ER signaling and tumor cell growth.

References

[1] Youssef El-Ahmad, et al. J Med Chem. 2020 Jan 23;63(2):512-528.
[2] Maysoun Shomali, et al. Mol Cancer Ther. 2021 Feb;20(2):250-262.