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IMT1B

CAS No. 2304621-06-3

IMT1B( 3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- | LDC203974 )

Catalog No. M24045 CAS No. 2304621-06-3

IMT1B is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. It has anti-tumour effects.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    IMT1B
  • Note
    Research use only, not for human use.
  • Brief Description
    IMT1B is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. It has anti-tumour effects.
  • Description
    IMT1B is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. It has anti-tumour effects.
  • In Vitro
    Cell Viability Assay Cell Line:A2780 cells Concentration:0.01 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM Incubation Time:72 hours, 96 hours, 168 hours Result:Decreased cell viability in a dose-dependent manner.
  • In Vivo
    Animal Model:7-9 weeks female BALB/c nude mice, with A2780 cells xenograft Dosage:100 mg/kg Administration:Oral administration, daily, for four weeks Result:Led to a clear reduction of tumour volume.Animal Model:Mice Dosage:1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) Administration:Intravenous administration and oral administration Result:Oral bioavailability (101%), Cmax (5149 ng/mL), T1/2 (1.88 h).
  • Synonyms
    3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- | LDC203974
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    POLRMT
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2304621-06-3
  • Formula Weight
    473.88
  • Molecular Formula
    C24H21ClFNO6
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:250 mg/mL?(527.56 mM;?Need ultrasonic)
  • SMILES
    C[C@H](C(=O)N1CCC[C@@H](C1)C(=O)O)OC2=CC3=C(C=C2)C(=CC(=O)O3)C4=C(C=C(C=C4)F)Cl
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Nina A Bonekamp, et al. Small-molecule inhibitors of human mitochondrial DNA transcription. Nature. 2020 Dec;588(7839):712-716.
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