868733-71-5

Basic information

• Product Name: 4-(4-aMino-2-fluorophenoxy)-picolinaMide
• Synonyms: 4-(4-aMino-2-fluorophenoxy)-picolinaMide
• CAS NO: 868733-71-5
• Molecular Formula: C₁₂H₁₀FN₃O₂
• Molecular Weight: 247.2251032
• Mol File: 868733-71-5.mol
• Article Data: 8

Chemical Properties

• Boiling Point: 440.6°C at 760 mmHg
• Flash Point: 220.3°C
• Appearance: /
• Density: 1.385g/cm³
• Vapor Pressure: 5.82E-08mmHg at 25°C
• Refractive Index: 1.635
• CAS DataBase Reference: 4-(4-aMino-2-fluorophenoxy)-picolinaMide(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(4-aMino-2-fluorophenoxy)-picolinaMide(868733-71-5)
• EPA Substance Registry System: 4-(4-aMino-2-fluorophenoxy)-picolinaMide(868733-71-5)

Safety Data

• Hazardous Substances Data: 868733-71-5(Hazardous Substances Data)

Usage

InChI:InChI=1/C12H10FN3O2/c13-9-5-7(14)1-2-11(9)18-8-3-4-16-10(6-8)12(15)17/h1-6H,14H2,(H2,15,17)

Upstream product

• 99586-65-9 4-chloropicolinamide 
• 399-96-2 4-amino-2-fluorophenol 
• 1025721-01-0 4-(4-amino-2-fluorophenoxy)-3-chloropyridine-2-carboxamide 
• 403-19-0 2-fluoro-4-nitrophenol 

Downstream Products

• 928038-28-2 4-(2-Fluoro-4-{[1-(4-fluorophenylcarbamoyl)cyclopropanecarbonyl]amino}phenoxy)pyridine-2-carboxamide 
• 928038-29-3 N-{4-[(2-Aminopyridin-4-yl)oxy]-3-fluorophenyl}-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide 

Relevant articles and documents

Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor

The receptor tyrosine kinase Axl plays important roles in promoting cancer progression, metastasis, and drug resistance and has been identified as a promising target for anticancer therapeutics. We used molecular modeling-assisted structural optimization starting with the low micromolar potency compound 9 to discover compound 13c, a highly potent and orally bioavailable Axl inhibitor. Selectivity profiling showed that 13c could inhibit the well-known oncogenic kinase Met with equal potency to its inhibition of Axl superfamily kinases. Compound 13c significantly inhibited cellular Axl and Met signaling, suppressed Axl- and Met-driven cell proliferation, and restrained Gas6/Axl-mediated cancer cell migration or invasion. Furthermore, 13c exhibited significant antitumor efficacy in Axl-driven and Met-driven tumor xenograft models, causing tumor stasis or regression at well-tolerated doses. All these favorable data make 13c a promising therapeutic candidate for cancer treatment.

PHARMACEUTICAL COMPOSITION AND APPLICATION REPLACING QUINOLONE DERIVATIVE, PHARMACEUTICAL ACCEPTABLE SALT, OR STEREOISOMER

Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.

NOVEL PYRIDINE DERIVATIVE AND PYRIMIDINE DERIVATIVE (3)

A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen or the like.]