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HomeProduct name listPELITINIB

PELITINIB

Synonym(s):(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;EKB 569;EKB-569;WAY-EKB-569

  • CAS NO.:257933-82-7
  • Empirical Formula: C24H23ClFN5O2
  • Molecular Weight: 467.92
  • MDL number: MFCD09837868
  • EINECS: 803-625-4
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2023-06-30 15:45:59
PELITINIB Structural

What is PELITINIB?

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

The Uses of PELITINIB

Labelled Pelitinib (P218702). A tyrosine kinase inhibitor; it is used to prepare formulation for treating primary or secondary cancer.

The Uses of PELITINIB

Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.

The Uses of PELITINIB

An EGFR inhibitor

What are the applications of Application

Pelitinib is an EGFR inhibitor

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.

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.

Properties of PELITINIB

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

Safety information for PELITINIB

Signal word Danger
Pictogram(s)
ghs
Skull and Crossbones
Acute Toxicity
GHS06
GHS Hazard Statements H301:Acute toxicity,oral
Precautionary Statement Codes P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Computed Descriptors for PELITINIB

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