257933-82-7

Basic information

• Product Name: PELITINIB
• Synonyms: PELITINIB;2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)-;(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;WAY-EKB 569;(E)-N-(4-(3-chloro-4-fluorophenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide;Pelitinib(EKB-569);(2E)-N-{4-[(3-chloro-4-fluorophenyl)aMino]-3-cyano-7-ethoxyquinolin-6-yl}-4-(diMethylaMino)but-2-enaMide;(2e)-n-(4-((3-chloro-4-fluorophenyl)aMino)-3-cyano-7-ethoxy-6-quinolinyl)-4-(diMethylaMino)-2-butenaMide pelitinib
• CAS NO: 257933-82-7
• Molecular Formula: C₂₄H₂₃ClFN₅O₂
• Molecular Weight: 467.93
• EINECS: 1312995-182-4
• Product Categories: API;All Inhibitors;pyridine;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Tyrosine Kinase Inhibitors;Aromatics;Heterocycles;Isotope Labelled Compounds
• Mol File: 257933-82-7.mol
• Article Data: 3

Chemical Properties

• Melting Point: 173-178°C
• Boiling Point: 655.5 °C at 760 mmHg
• Flash Point: 350.2 °C
• Appearance: white to beige/
• Density: 1.34
• Vapor Pressure: 4.64E-17mmHg at 25°C
• Refractive Index: 1.644
• Storage Temp.: -20°C Freezer
• Solubility: DMSO: soluble5mg/mL, clear (warmed)
• PKA: 12.23±0.43(Predicted)
• CAS DataBase Reference: PELITINIB(CAS DataBase Reference)
• NIST Chemistry Reference: PELITINIB(257933-82-7)
• EPA Substance Registry System: PELITINIB(257933-82-7)

Safety Data

• Hazard Codes: T
• Statements: 25
• Safety Statements: 45
• RIDADR: UN 2811 6.1 / PGIII
• WGK Germany: 3
• HazardClass: 6.1
• PackingGroup: III
• Hazardous Substances Data: 257933-82-7(Hazardous Substances Data)

Usage

Description

Pelitinib, also known as a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor, is a pharmaceutical compound with potential antineoplastic activity. It is characterized by its off-white solid appearance and functions by irreversibly inhibiting the EGFR receptor tyrosine kinase, as well as displaying weaker potency against HER2. By disrupting the Akt and MAPK pathways, pelitinib can induce apoptosis and suppress the growth of tumor cell lines, particularly showing strong efficacy against hepatocellular carcinoma cells.

Uses

Used in Anticancer Applications:
PELITINIB is used as an antineoplastic agent for its ability to inhibit the EGFR receptor tyrosine kinase and disrupt the Akt and MAPK pathways, leading to the suppression of tumor cell growth and the induction of apoptosis.
Used in Pharmaceutical Industry:
PELITINIB is used as an EGFR inhibitor for its potential in treating various types of cancer by targeting the epidermal growth factor receptor, which plays a crucial role in cell proliferation and survival.
Used in Cancer Treatment Formulation:
PELITINIB is used as a tyrosine kinase inhibitor in the preparation of formulations for treating primary or secondary cancer, particularly due to its strong efficacy against hepatocellular carcinoma cells.

references

[1] torrance cj, jackson pe, montgomery e, kinzler kw, vogelstein b, wissner a, nunes m, frost p, discafani cm. combinatorial chemoprevention of intestinal neoplasia. nat med. 2000 sep;6(9):1024-8.[2] nunes m, shi c, greenberger lm. phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase b, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, ekb-569, in tumor cells and normal human keratinocytes. mol cancer ther. 2004 jan;3(1):21-7.

InChI:InChI=1/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+

Upstream product

• 361162-92-7 2-acetylamino-4-ethoxy-5-nitrobenzoic acid 
• 214476-08-1 7-Ethoxy-4-hydroxy-6-nitro-quinoline-3-carbonitrile 
• 214476-09-2 4-Chloro-7-ethoxy-6-nitro-quinoline-3-carbonitrile 
• 909513-02-6 (E)-2-Cyano-3-(3-ethoxy-phenylamino)-acrylic acid ethyl ester 
• 361162-91-6 5-ethoxy-2-methyl-4-nitroacetanilide 
• 214476-07-0 7-ethoxy-4-hydroxyquinoline-3-carbonitrile 
• 361162-90-5 5-methoxy-2-methyl-4-nitroacetanilide 
• 116435-75-7 3-(ethyloxy)-4-nitroaniline 
• 106579-00-4 5-methoxy-2-methyl-4-nitroaniline 
• 367-21-5 3-chloro-4-fluorophenylamine 
• 99083-25-7 4-bromocrotonyl chloride 
• 124-40-3 dimethyl amine 
• 361162-95-0 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile 
• 621-33-0 m-phenetidine 

Relevant articles and documents

USE OF CYANOQUINOLINES FOR TREATING OR INHIBITING COLONIC POLYPS

This invention provides a method of treating or inhibiting colonic polyps which comprises providing a compound of formula (1); wherein R1, R2, R3, R4, X, Y, and n are defined hereinbefore, or a pharmaceutically acceptable salt thereof.

Method of treating or inhibiting colonic polyps

This invention provides a method of treating or inhibiting colonic polyps which comprises providing a compound of formula 1 wherein:R1, R2, R3, R4, X, Y, and n are as defined hereinbefore, or a pharmaceutically acceptable salt thereof.