1581701-28-1

Basic information

• Product Name: 2-(isopropylamino)-N-(2-methyl-5-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)phenyl)pyrimidine-5-carboxamide
• CAS NO: 1581701-28-1
• Molecular Weight: 569.63
• Mol File: 1581701-28-1.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 2-(isopropylamino)-N-(2-methyl-5-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)phenyl)pyrimidine-5-carboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(isopropylamino)-N-(2-methyl-5-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)phenyl)pyrimidine-5-carboxamide(1581701-28-1)
• EPA Substance Registry System: 2-(isopropylamino)-N-(2-methyl-5-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)phenyl)pyrimidine-5-carboxamide(1581701-28-1)

Safety Data

• Hazardous Substances Data: 1581701-28-1(Hazardous Substances Data)

Upstream product

• 148741-62-2 2-isopropylamino-5-methoxycarbonylpyrimidine 
• 77476-95-0 (5-bromopyrimidin-2-yl)-N-isopropylamine 
• 96-98-0 4-methyl-3-nitrobenzoic acid 
• 694499-26-8 4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylaniline 
• 148741-64-4 2-Isopropylamino-5-carboxypyrimidine 
• 1202649-62-4 3-amino-4-methyl-N-(4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl)phenyl)benzamide 
• 1581700-94-8 4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-nitrobenzamide 

Relevant articles and documents

Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib

Epidermal growth factor receptor (EGFR) amplification has been demonstrated to be critical for the inherent and/or acquired resistance against current B-RafV600E inhibitor therapy for melanoma and colorectal cancer patients. We describe the discovery and structure-activity relationship study of a series of 1H-pyrazolo[3,4-b]pyridine-5-carboxamide analogues as novel dual inhibitors of EGFR and B-RafV600E mutant. One of the most promising compounds, 6a, potently inhibited both of the kinases with IC50 values of 8.0 and 51 nM, respectively. The compound also strongly suppressed the proliferation of a panel of intrinsic and acquired resistant melanoma and/or colorectal cancer cells harboring overexpressed EGFR with submicromolar IC 50 values. Further mechanism investigation revealed that 6a could sustainably inhibit the activation of the MAPK path way in the resistant SK-MEL-28 PR30 melanoma cancer cells and WiDr colorectal cancer cells with EGFR amplification. Our results support the hypothesis that the EGFR/B-Raf V600E dual inhibition might be a tractable strategy to overcome the intrinsic and acquired resistance of melanoma and/or colorectal cancers against the current B-RafV600E inhibitor therapy.