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| | PELITINIB 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;(2E)-N-{4-[(3-chloro-4-fluorophenyl)aMino]-3-cyano-7-ethoxyquinolin-6-yl}-4-(diMethylaMino)but-2-enaMide;(E)-N-(4-(3-chloro-4-fluorophenylamino)-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;N-[4-(3-Chloro-4-fluorophenylamino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)-2(E)-but·Namide | | CAS: | 257933-82-7 | | MF: | C24H23ClFN5O2 | | MW: | 467.92 | | EINECS: | 803-625-4 | | Product Categories: | Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Tyrosine Kinase Inhibitors;pyridine;All Inhibitors;API;Aromatics;Heterocycles;Isotope Labelled Compounds | | Mol File: | 257933-82-7.mol |  |
| | PELITINIB Chemical Properties |
| Melting point | 173-178°C | | Boiling point | 655.5±55.0 °C(Predicted) | | density | 1.34 | | storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | | solubility | DMSO: soluble5mg/mL, clear (warmed) | | form | powder | | pka | 12.23±0.43(Predicted) | | color | white to beige |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 | | HS Code | 2933.59.8000 | | HazardClass | 6.1 | | PackingGroup | III |
| | PELITINIB Usage And Synthesis |
| Description | Pelitinib is a cyanoquinoline that irreversibly inhibits the EGFR receptor tyrosine kinase (IC50 = 39 nM). It inhibits HER2 with a much weaker potency (IC50 = 1.2 μM). By disrupting Akt and MAPK pathways, pelitinib can induce apoptosis and suppress the growth of tumor cell lines, displaying particularly strong efficacy against hepatocellular carcinoma cells (IC50s = ~2 μM). | | Chemical Properties | Off-White Solid | | Uses | Labelled Pelitinib (P218702). A tyrosine kinase inhibitor; it is used to prepare formulation for treating primary or secondary cancer. | | Uses | An EGFR inhibitor | | Uses | Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. | | Definition | ChEBI: Pelitinib is an aminoquinoline, a nitrile, a monocarboxylic acid amide and a member of monochlorobenzenes. It has a role as a protein kinase inhibitor. | | target | EGFR | | storage | Store at -20°C | | 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. |
| | PELITINIB Preparation Products And Raw materials |
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