1210608-43-7

Basic information

• Product Name: N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
• Synonyms: N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide;PIM447 (LGH447);PIM447;PIM447 (LGH447) Free Base;EOS-60671
• CAS NO: 1210608-43-7
• Molecular Formula: C24H23F3N4O
• Molecular Weight: 440.4608296
• Mol File: 1210608-43-7.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 493.7±45.0 °C(Predicted)
• Appearance: /
• Density: 1.290±0.06 g/cm3(Predicted)
• PKA: 1.35±0.70(Predicted)
• CAS DataBase Reference: N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide(1210608-43-7)
• EPA Substance Registry System: N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide(1210608-43-7)

Safety Data

• Hazardous Substances Data: 1210608-43-7(Hazardous Substances Data)

Usage

Uses

PIM kinases promote growth and survival of tumor cells and are expressed in a wide variety of human cancers. These kinases are potential therapeutic targets. PIM447 is a PIM kinase inhibitor.

Upstream product

• 1187056-55-8 4-tert-butyl [(1S,3R,5S)-3-(3-aminopyridin-4-yl)-5-methylcyclohexyl]carbamate 
• 1210418-12-4 cis-(±)-tert-butyl 3-(3-aminopyridin-4-yl)-5-methylcyclohexylcarbamate 

Relevant articles and documents

Identification of N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a potent and selective proviral insertion site of Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitor in clinical trials for hematological malignancies

Pan proviral insertion site of Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitors have recently begun to be tested in humans to assess whether pan PIM kinase inhibition may provide benefit to cancer patients. Herein, the synthesis, in vitro activity, in vivo activity in an acute myeloid leukemia xenograft model, and preclinical profile of the potent and selective pan PIM kinase inhibitor compound 8 (PIM447) are described. Starting from the reported aminopiperidyl pan PIM kinase inhibitor compound 3, a strategy to improve the microsomal stability was pursued resulting in the identification of potent aminocyclohexyl pan PIM inhibitors with high metabolic stability. From this aminocyclohexyl series, compound 8 entered the clinic in 2012 in multiple myeloma patients and is currently in several phase 1 trials of cancer patients with hematological malignancies.