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H3B-5942
$109 – $1,210
Products Details
Product Description
– 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].
Web ID
– HY-112611
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C31H34N4O2
References
– [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.
CAS Number
– 2052128-15-9
Molecular Weight
– 494.63
Compound Purity
– 99.73
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
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 83.33 mg/mL (ultrasonic)
Target
– Estrogen Receptor/ERR
Isoform
– ERα
Pathway
– Vitamin D Related/Nuclear Receptor
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
