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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    H3B-5942
  • Note
    Research use only, not for human use.
  • Brief Description
    H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo.
  • Description
    H3B-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.
  • In Vitro
    H3B-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.
  • In Vivo
    H3B-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.
  • Synonyms
    H3B5942
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    Estrogen Receptor/ERR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2052128-15-9
  • Formula Weight
    494.639
  • Molecular Formula
    C31H34N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 83.33 mg/mL (168.47 mM)
  • SMILES
    CCC(=C(C1=CC=C(C=C1)OCCNCC=CC(=O)N(C)C)C2=CC3=C(C=C2)NN=C3)C4=CC=CC=C4
  • 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

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Puyang X, et al. Cancer Discov. 2018 Jul 10. pii: CD-17-1229.
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