H3B-5942

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations[1].

Product Specifications

CAS Number

[2052128-15-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/H3B-5942.html

Concentration

10mM

Purity

98.0

Solubility

DMSO : 83.33 mg/mL (ultrasonic)

Smiles

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC/C=C/C(N(C)C)=O)C=C2)\C3=CC(C=NN4)=C4C=C3

Molecular Formula

C31H34N4O2

Molecular Weight

494.63

Precautions

H302, H315, H319, H335

References & Citations

[1]Puyang X, et al. Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer. Cancer Discov. 2018 Sep;8 (9) :1176-1193.