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Limantrafin

MCE China：Limantrafin

Brand：MedChemExpress (MCE)

Cat. No.HY-135145

CAS：218457-67-1

Synonyms：CB-103

Purity：99.28%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity.

In Vitro：Limantrafin acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex[2]. Limantrafin can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines[2]. Limantrafin exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines[2].

In Vivo：Limantrafin inhibits NOTCH dependent cellular processes in mice[2]. Limantrafin blocks in vivo growth of PDX models of T-ALL[2]. Limantrafin (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer[3]. Limantrafin exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors[3].

IC50 & Target：notch signaling pathway[1] In Vitro Limantrafin acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex[2]. Limantrafin can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines[2]. Limantrafin exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Limantrafin Related Antibodies Cell Viability Assay[1] Cell Line: RPMI 8402, KOPTK1, PANC1, nRas driven melanoma cells

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References：

[1]. Freddy Radtke, et al. Inhibitors of notch signalling pathway and use thereof in treatment of cancers. US9296682B2.

[2]. R.Lehal, et al. Development of a novel first-in-class oral inhibitor of the NOTCH pathway.

[3]. Rajwinder Lehal, et al. Non clinical pharmacology, pharmacokinetics and safety profiling of CB-103: A novel first-in-class small molecule inhibitor of the NOTCH pathway.

[4]. Jose Manuel Perez Garcia, et al. First-in-human phase 1-2A study of CB-103, an oral Protein-Protein Interaction Inhibitor targeting pan-NOTCH signalling in advanced solid tumors and blood malignancies.