IMT1B - 10mM in DMSO , CAS No.2304621-06-3

CAS: 2304621-06-3 Cat. No.: I656332 Formula: C₂₄H₂₁ClFNO₆ Peso molecolare: 473.88 PubChem CID: 138490769

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

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. ?\nIMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells. ?\nIMT1B depletes cellular metabolites. ?\nIMT1B 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 . ?\nIMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours . ?\nIMT1B exhibits good oral bioavailability (mice 101 %) and C max (mice 5149 ng/mL) following oral administration (mice 10 mg/kg) . ?\nIMT1B 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).

IC50& Target:POLRMT

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

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.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

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Tipo di azione

INHIBITOR

Nomi e identificatori

• PubChem CID: 138490769
• Peso molecolare: 473.88

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2304621-06-3, the molecular formula is C24H21ClFNO6, and the molecular weight is 473.88 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.