1357945-49-3

Basic information

• Product Name: 3-c]pyridine
• Synonyms: 6-bromo-3-iodo-1H-pyrazolo[4,3-c]pyridine;6-bromo-3-iodo-2H-pyrazolo[4,3-c]pyridine
• CAS NO: 1357945-49-3
• Molecular Formula: C6H3BrIN3
• Molecular Weight: 323.91659
• Mol File: 1357945-49-3.mol

Chemical Properties

• Boiling Point: 458.7±40.0 °C(Predicted)
• Appearance: /
• Density: 2.559±0.06 g/cm3(Predicted)
• Storage Temp.: under inert gas (nitrogen or Argon) at 2–8 °C
• PKA: 8.47±0.40(Predicted)
• CAS DataBase Reference: 3-c]pyridine(CAS DataBase Reference)
• NIST Chemistry Reference: 3-c]pyridine(1357945-49-3)
• EPA Substance Registry System: 3-c]pyridine(1357945-49-3)

Safety Data

• Hazard Codes: Xn
• Statements: 22
• Hazardous Substances Data: 1357945-49-3(Hazardous Substances Data)

Upstream product

• 1256789-73-7 methyl 6-bromo-4-chloropyridine-3-carboxylate 
• 1206973-12-7 6-bromo-1H-pyrazolo[4,3-c]pyridine 
• 1364663-37-5 2-bromo-4-chloro-5-iodopyridine 
• 1300750-78-0 4-amino-2-bromo-5-iodopyridine 
• 7598-35-8 2-bromo-4-aminopyridine 

Relevant articles and documents

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

Inhibitors targeting the activating mutants of the epidermal growth factor receptor (EGFR) have found success in the treatment of EGFR mutant positive non-small-cell lung cancer. A secondary point mutation (T790M) in the inhibitor binding site has been li

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

Activating mutations within the epidermal growth factor receptor (EGFR) kinase domain, commonly L858R or deletions within exon 19, increase EGFR-driven cell proliferation and survival and are correlated with impressive responses to the EGFR inhibitors erlotinib and gefitinib in nonsmall cell lung cancer patients. Approximately 60% of acquired resistance to these agents is driven by a single secondary mutation within the EGFR kinase domain, specifically substitution of the gatekeeper residue threonine-790 with methionine (T790M). Due to dose-limiting toxicities associated with inhibition of wild-type EGFR (wtEGFR), we sought inhibitors of T790M-containing EGFR mutants with selectivity over wtEGFR. We describe the evolution of HTS hits derived from Jak2/Tyk2 inhibitors into selective EGFR inhibitors. X-ray crystal structures revealed two distinct binding modes and enabled the design of a selective series of novel diaminopyrimidine-based inhibitors with good potency against T790M-containing mutants of EGFR, high selectivity over wtEGFR, broad kinase selectivity, and desirable physicochemical properties.

AZAINDAZOLE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS

This invention relates to novel compounds of formula (I), which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.