845272-21-1

Basic information

• Product Name: ARRY-334543
• Synonyms: ARRY-334543;AR-00334543;Varlitinib;(R)-4-[[3-Chloro-4-[(thiazol-2-yl)methoxy]phenyl]amino]-6-[(4-methyl-4,5-dihydrooxazol-2-yl)amino]quinazoline;(R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine;Varlitinib ARRY 334543;ARRY 334543 (Varlitinib);N4-[3-chloro-4-(2-thiazolylmethoxy)phenyl]-N6-[(4R)-4,5-dihydro-4-methyl-2-oxazolyl]-4,6-Quinazoline diamine
• CAS NO: 845272-21-1
• Molecular Formula: C₂₂H₁₉ClN₆O₂S
• Molecular Weight: 466.94326
• Product Categories: Inhibitors
• Mol File: 845272-21-1.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 637.1±65.0 °C(Predicted)
• Appearance: /
• Density: 1.51±0.1 g/cm3(Predicted)
• PKA: 6.54±0.70(Predicted)
• CAS DataBase Reference: ARRY-334543(CAS DataBase Reference)
• NIST Chemistry Reference: ARRY-334543(845272-21-1)
• EPA Substance Registry System: ARRY-334543(845272-21-1)

Safety Data

• Hazardous Substances Data: 845272-21-1(Hazardous Substances Data)

Usage

Uses

Varlitinib is a tyrosine kinase inhibitor being developed for the treatment of cancer. Varlitinib acts by disrupting the receptor tyrosine kinases ErbB-2, ErbB-4 and EGFR.

Enzyme inhibitor

This ErbB1/2 inhibitor (FW = 466.94 g/mol; CAS 845272-21-1), also named (R)-N4 -(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6 -(4-methyl-4,5- dihydrooxazol-2-yl)quinazoline-4,6-diamine, selectively targets the intrinsic protein kinase activities of ErbB1, or Epidermal Growth Factor Receptor (EGFR), IC50 = 7 nM and ErbB2, or Human Epidermal growth factor Receptor (HER2), IC50 = 2 nM. ARRY-334543 also reverses multidrug resistance by antagonizing the activity of ATP-binding cassette subfamily G member 2.

Upstream product

• 851545-78-3 2-((2-chloro-4-nitrophenoxy)methyl)thiazole 
• 851545-79-4 3-chloro-4-(thiazol-2-ylmethoxy)aniline 
• 1012041-42-7 4-N-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)quinazoline-4,6-diamine 
• 616-79-5 2-amino-5-nitro-benzoic acid 
• 6943-17-5 6-nitroquinazolone 
• 19815-16-8 4-chloro-6-nitro-quinazoline 
• 619-08-9 2-chloro-4-nitrophenol 

Relevant articles and documents

Preparation method of medicine for treating bile duct cancer

The invention belongs to the field of medical industry, and discloses a preparation method of a medicine for treating bile duct cancer. The preparation method of the drug Varlitinib for treating bileduct cancer comprises the following steps: with 2-amino-5-nitrobenzoic acid as a starting material, carrying out cyclization and chlorination on 2-amino-5-nitrobenzoic acid and methylimidazole acetateso as to synthesize an intermediate I; with 2-chloro-5-nitrophenol as a starting material, carrying out 2-chloromethylthiazole substitution and nitro reduction to synthesize an intermediate II; with1-amino-2-propanol as a starting material, carrying out a cyclization reaction of BTC, and carrying out chlorination to synthesize an intermediate III; and carrying out C-N coupling and nitro reduction on the intermediate I and the intermediate II, and finally carrying out a C-N coupling reaction on the intermediate I and the intermediate II and an intermediate III to synthesize Varlitinib. The method is simple and convenient to synthesize, short in route, economical in raw materials, high in yield, friendly to environment and suitable for industrial production.