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BRM/BRG1 ATP Inhibitor-1

CAS No. 2270879-17-7

BRM/BRG1 ATP Inhibitor-1( —— )

Catalog No. M24032 CAS No. 2270879-17-7

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    BRM/BRG1 ATP Inhibitor-1
  • Note
    Research use only, not for human use.
  • Brief Description
    BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).
  • Description
    BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).
  • In Vitro
    Cell Proliferation Assay Cell Line:SKMEL5 melanoma cells and SBC-5 small cell carcinoma Concentration:0-10 μM Incubation Time:5 days Result:Inhibited the proliferation of SKMEL5 cells with an AAC50 (absolute AC50) value of 0.004 μM and of SBC-5 cells with the AAC50 more than 10 μM.
  • In Vivo
    Animal Model:Female athymic nude mice with RERF-LC-AI tumor xenografts Dosage:7.5 mg/kg, 20 mg/kg Administration:Oral administration; everyday; 3 weeks Result:Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively.Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    BRM/BRG1
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2270879-17-7
  • Formula Weight
    318.27
  • Molecular Formula
    C11H9F3N4O2S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:250 mg/mL (785.50 mM; Need ultrasonic)
  • SMILES
    O=C(NC1=CC(F)=NC=C1CO)NC2=CC(C(F)F)=NS2
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61(22):10155-10172
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