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CSRM617 hydrochloride

CAS No. 1353749-74-2

CSRM617 hydrochloride( —— )

Catalog No. M32871 CAS No. 1353749-74-2

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 μM in SPR assays, directly binding to the OC2-HOX domain.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CSRM617 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 μM in SPR assays, directly binding to the OC2-HOX domain.
  • Description
    CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
  • In Vitro
    CSRM617 (0.01-100 μM; 48 hours) hydrochloride inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells.CSRM617 (10-20 μM; 48 hours) hydrochloride induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion.CSRM617 (20 μM; 72 hours) hydrochloride induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP.
  • In Vivo
    CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft.Animal Model:SCID mice with 22Rv1 xenograft Dosage:50 mg/kg Administration:Oral administration; daily, for 20 days Result:Elicited a significant reduction in the onset and growth of diffuse metastases.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis | Androgen Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1353749-74-2
  • Formula Weight
    291.69
  • Molecular Formula
    C10H14ClN3O5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (428.54 mM; Ultrasonic )
  • SMILES
    Cl.NC(CO)C(=O)N\N=C\c1ccc(O)c(O)c1O
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Rotinen M, et, al. ONECUT2 is a targetable master regulator of lethal prostate cancer that suppresses the androgen axis. Nat Med. 2018 Dec;24(12):1887-1898. ?
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