
H3B-5942
CAS No. 2052128-15-9
H3B-5942( H3B5942 )
Catalog No. M13184 CAS No. 2052128-15-9
H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
5MG | 170 | In Stock |
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10MG | 264 | In Stock |
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25MG | 511 | In Stock |
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50MG | 731 | In Stock |
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100MG | 972 | In Stock |
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200MG | Get Quote | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameH3B-5942
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NoteResearch use only, not for human use.
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Brief DescriptionH3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo.
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DescriptionH3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo; covalently inactivates both wild-type and mutant ERα by targeting Cys530 and enforcing a unique antagonist conformation; demonstrated significant single-agent antitumor activity in xenograft models representing ERαWT and ERα Y537S breast cancer that was superior to fulvestrant.
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In VitroH3B-5942 is a selective and irreversible 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 elevates ERα protein level distinct from SERMs/SERD, blocks ERα-dependent transcription in breast cancer cells. H3B-5942 (0.01-10 μM) reduces ERα target gene GREB1 in MCF7-ERαWT, various MCF7-ERαMUT lines, and the PDX-ERαY537S/WT line. H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERαWT, and MCF7-LTED-ERαY537C lines with GI50s of 0.5, 2, and 30 nM, respectively. H3B-5942 (10-25 nM) in combination with CDK4/6 inhibitors (≥25 pM) has synergic inhibitory effect on multiple cell lines bearing ERαWT or clinically frequent ERα mutations.
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In VivoH3B-5942 (1, 3, 10, or 30 mg/kg, p.o, q.d. for 17 days) dose-dependently inhibits tumor growth in MCF7 xenograft model in athymic female nude mice.H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERαY537S/WT ST941 model in athymic female nude mice. Animal Model:MCF7 xenograft model in athymic female nude mice Dosage:1, 3, 10, or 30 mg/kg Administration:P.O. once a day (q.d.×1) for 17 days Result:Exhibited tumor growth inhibition (TGI) on day 17 of 19%, 41%, 68%, and 83%, respectively.
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SynonymsH3B5942
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PathwayEndocrinology/Hormones
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TargetEstrogen Receptor/ERR
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RecptorEstrogen Receptor/ERR
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Research Area——
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Indication——
Chemical Information
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CAS Number2052128-15-9
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Formula Weight494.639
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Molecular FormulaC31H34N4O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 83.33 mg/mL (168.47 mM)
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SMILESCCC(=C(C1=CC=C(C=C1)OCCNCC=CC(=O)N(C)C)C2=CC3=C(C=C2)NN=C3)C4=CC=CC=C4
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Chemical Name(E)-4-((2-(4-((E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)phenoxy)ethyl)amino)-N,N-dimethylbut-2-enamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Puyang X, et al. Cancer Discov. 2018 Jul 10. pii: CD-17-1229.
molnova catalog



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