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PELITINIB

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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
  • 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
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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
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Safety Information

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
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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.

PELITINIBSupplier

Shanghai Boyle Chemical Co., Ltd.
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