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IMT1B (Synonyms: LDC203974)

Cat. No.: HY-137067 Purity: 98.03%
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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.

For research use only. We do not sell to patients.

IMT1B Chemical Structure

IMT1B Chemical Structure

CAS No. : 2304621-06-3

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5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
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Description

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[1].

IC50 & Target

POLRMT[1]

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[1].
IMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells[1].
IMT1B depletes cellular metabolites[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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

IMT1B (100 mg/kg; ) significantly reduces tumour size in mice containing xenografts[1].
IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours[1].
IMT1B exhibits good oral bioavailability (101 %) and Cmax (5149 ng/mL) following oral administration (mice 10 mg/kg)[1].
IMT1B exhibits elimination half-life (mice 1.88 h) due to plasma clearance (0.44 L/h/kg) following intravenous administration (1 mg/kg)[1].

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[1]
Dosage: 100 mg/kg
Administration: Oral administration, daily, four weeks
Result: Led to a clear reduction of tumour volume.
Animal Model: Mice[1]
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).
Molecular Weight

473.88

Formula

C₂₄H₂₁ClFNO₆

CAS No.

2304621-06-3

SMILES

O=C([[email protected]@H]1CN(C([[email protected]](OC2=CC=C(C(O3)=C2)C(C4=CC=C(F)C=C4Cl)=CC3=O)C)=O)CCC1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (527.56 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1102 mL 10.5512 mL 21.1024 mL
5 mM 0.4220 mL 2.1102 mL 4.2205 mL
10 mM 0.2110 mL 1.0551 mL 2.1102 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

IMT1BLDC203974LDC 203974LDC-203974OthersmitochondrialDNAmtDNAhumanRNApolymerasePOLRMToxidativephosphorylationOXPHOSanti-tumourInhibitorinhibitorinhibit

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IMT1B
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