1246529-32-7

Basic information

• Product Name: MPI-0479605
• Synonyms: MPI-0479605;N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine;MPI0479605 HCl;N6-Cyclohexyl-N2-[2-methyl-4-(4-morpholinyl)phenyl]-9H-purine-2,6-diamine
• CAS NO: 1246529-32-7
• Molecular Formula: C₂₂H₂₉N₇O
• Molecular Weight: 407.52
• Product Categories: Inhibitors
• Mol File: 1246529-32-7.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 745.8±70.0 °C(Predicted)
• Appearance: /
• Density: 1.318±0.06 g/cm3(Predicted)
• Storage Temp.: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
• Solubility: Soluble in DMSO
• PKA: 10.52±0.10(Predicted)
• CAS DataBase Reference: MPI-0479605(CAS DataBase Reference)
• NIST Chemistry Reference: MPI-0479605(1246529-32-7)
• EPA Substance Registry System: MPI-0479605(1246529-32-7)

Safety Data

• Hazardous Substances Data: 1246529-32-7(Hazardous Substances Data)

Usage

Description

MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1, characterized by its high selectivity and effectiveness in targeting cancer cells.

Uses

Used in Oncology:
MPI-0479605 is used as an anticancer agent for its ability to inhibit the mitotic kinase MPS1, leading to failed cytokinesis, misalignment of chromosomes, aneuploidy, and slowed cell cycle progression in various cancer cell lines. This contributes to the reduction of tumor volume in preclinical models, such as the HCT116 mouse colon cancer xenograft model, in a dose-dependent manner.

references

[1] tardif k d, rogers a, cassiano j, et al. characterization of the cellular and antitumor effects of mpi-0479605, a small-molecule inhibitor of the mitotic kinase mps1. molecular cancer therapeutics, 2011, 10(12): 2267-2275.

Upstream product

• 5451-40-1 2,6 dichloropurine 
• 108-91-8 cyclohexylamine 
• 220679-09-4 4-(3-methyl-4-nitrophenyl)morpholine 
• 581-00-0 2-Methyl-4-morpholin-4-ylphenylamine 
• 1246532-45-5 2-chloro-N-cyclohexyl-9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-amine 
• 39639-45-7 (2-chloro-9H-purin-6-yl)-cyclohexyl-amine 
• 1246532-46-6 N₆-cyclohexyl-N₂-(2-methyl-4-morpholin-4-yl-phenyl)-9-(tetrahydropyran-2-yl)-9H-purine-2,6-diamine 
• 1246532-35-3 2-methyl-4-morpholin-4-yl-phenylamine hydrochloride 

Relevant articles and documents

Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors

Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described in this Letter. Mps1 biochemical activity and cytotoxicity in HCT-116 cell line were improved. On-target activity confirmation via mechanism based G2/M escape assay was demonstrated. Physico-chemical and ADME properties were optimized to improve oral bioavailability in mouse.