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

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.