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

COA

Datasheet

HNMR

HPLC

MSDS

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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

——

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

——

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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