IMT1B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IMT1B 是一种口服活性、非竞争性、特异性线粒体 RNA 聚合酶 (POLRMT) 变构抑制剂，可抑制线粒体 DNA (mtDNA) 表达。

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.

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.

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).

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

Others

Other Targets

POLRMT

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2304621-06-3

473.88

C24H21ClFNO6

>98% (HPLC)

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

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

——

(-20℃)

With Ice Pack

≥ 2 years