937263-43-9

Basic information

• Product Name: Irbinitinib
• Synonyms: (R)-N6-(4-Methyl-4;5-dihydrooxazol-2-yl)-N4-(3-Methyl-4-(thiazol-2-ylMethoxy)phenyl)quinazoline-4;6-diaMine;4-diMethyl-4;5-a]pyridin-7-yloxy)-3-Methylphenyl)-N6-(4;5-dihydrooxazol-2-yl)quinazoline-4;N4-(4-([1;4,6-QuinazolinediaMine, N6-(4,5-dihydro-4,4-diMethyl-2-oxazolyl)-N4-[3-Methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-
• CAS NO: 937263-43-9
• Molecular Formula: C26H24N8O2
• Molecular Weight: 480.52116
• Product Categories: Inhibitors
• Mol File: 937263-43-9.mol
• Article Data: 9

Chemical Properties

• Appearance: /
• Density: 1.41±0.1 g/cm3(Predicted)
• PKA: 6.61±0.70(Predicted)
• CAS DataBase Reference: Irbinitinib(CAS DataBase Reference)
• NIST Chemistry Reference: Irbinitinib(937263-43-9)
• EPA Substance Registry System: Irbinitinib(937263-43-9)

Safety Data

• Hazardous Substances Data: 937263-43-9(Hazardous Substances Data)

Usage

Description

Irbinitinib is also known as ARRY-380 or Tucatinib. ARRY-380 is an orally inhibitor of human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. It selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation. Therefore, ARRY-380 may be an alternative treatmentmethod for the treatment of HER2+ cancers.

Uses

N6-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine is a novel?diarylamine ErbB inhibitor.

References

Lee, P., et al. "In Vivo Activity of ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2 in Combination with Trastuzumab, Docetaxel or Bevacizumab." Cancer Research 69.24 Supplement(2009):5104-5104. Moulder, S. L., et al. "Abstract A143: ARRY-380, a selective HER2 inhibitor: From drug design to clinical evaluation." Molecular Cancer Therapeutics 10.Supplement 1(2011):A143-A143. Dinkel, Victoria, et al. "Abstract 852: ARRY-380, a potent, small molecule inhibitor of ErbB2, increases survival in intracranial ErbB2+ xenograft models in mice." Cancer Research 72.8 Supplement(2012).

Upstream product

• 937263-71-3 4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylaniline 
• 1427452-48-9 7-chloro-[1,2,4]triazolo[1,5-a]pyridine 
• 2131230-48-1 (E)-N'-(4-amino-2-cyanophenyl)-N,N-dimethylformimidamide 
• 39263-34-8 N′-(2-cyano-4-nitrophenyl)-N,N-dimethylformimidamide 
• 17420-30-3 5-nitroanthranilonitrile 
• 937263-44-0 7-(2-methyl-4-nitrophenoxy)-[1,2,4]triazolo[1,5-a] pyridine 
• 864244-98-4 4-(2-methyl-4-nitrophenoxy)pyridin-2-amine 
• 65370-42-5 4-chloro-2-nitropyridine 
• 99-53-6 2-methyl-4-nitrophenol 
• 1429755-58-7 1-(4-((4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)amino)quinazolin-6-yl)-3-(1-hydroxy-2-methylpropan-2-yl)thiourea 
• 19798-80-2 2-Amino-4-chloropyridine 

Relevant articles and documents

A Practical Alternate Synthesis of Tucatinib

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Preclinical activity of HER2-selective tyrosine kinase inhibitor tucatinib as a single agent or in combination with trastuzumab or docetaxel in solid tumor models

HER2 is a transmembrane tyrosine kinase receptor that mediates cell growth, differentiation, and survival. HER2 is overexpressed in approximately 20% of breast cancers and in subsets of gastric, colorectal, and esophageal cancers. Both antibody and smallm

Irbinitinib intermediates for preparation of (by machine translation)

The invention belongs to the organic synthesis and bulk drug preparation technology field, in particular to the treatment of breast cancer drug Irbinitinib preparation method and intermediate, comprising the steps of: 2 - methyl - 4 - nitro-phenol (formul