IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects In Vitro IMT1B is a noncompetitive inhibitor that causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. ? IMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells. ? IMT1B depletes cellular metabolites. ? IMT1B increases the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts . ? IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours . ? IMT1B exhibits good oral bioavailability (mice 101 %) and C max (mice 5149 ng/mL) following oral administration (mice 10 mg/kg) . ? IMT1B exhibits elimination half-life (mice 1.88 h) due to plasma clearance (mice 0.44 L/h/kg) following intravenous administration (mice 1 mg/kg) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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%), C max (5149 ng/mL), T 1/2 (1.88 h). Form:Solid IC50& Target:POLRMT
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IMT1B
CAS number：2304621-06-3 molecular formula：C24H21ClFNO6
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2304621-06-3 | molecular formula | C24H21ClFNO6 |
| molecular weight | 473.88 g/mol | Exact mass | ≥98% |
| PSA | 93.100 Ų | logp | 3.700 |
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