PELITINIB
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
- PELITINIB (EKB-569;WAY-EKB 569)
- EKB-569; WAY-EKB 569; EKB569; 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
- CAS:
- 257933-82-7
- MF:
- C24H23ClFN5O2
- MW:
- 467.92
- EINECS:
- 803-625-4
- Product Categories:
-
- Inhibitors
- Intermediates & Fine Chemicals
- All Inhibitors
- pyridine
- Pharmaceuticals
- Tyrosine Kinase 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
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
Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.
Uses
An EGFR inhibitor
Uses
Labelled Pelitinib (P218702). A tyrosine kinase inhibitor; it is used to prepare formulation for treating primary or secondary cancer.
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.
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