PELITINIB

Bezeichnung:PELITINIB

Englisch Name:PELITINIB

CBNumberCB81011748

SummenformelC24H23ClFN5O2

Molgewicht467.92

PELITINIB physikalisch-chemischer Eigenschaften

Schmelzpunkt	173-178°C
Siedepunkt	655.5±55.0 °C(Predicted)
Dichte	1.34
storage temp.	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	DMSO: soluble5mg/mL, clear (warmed)
Aggregatzustand	powder
pka	12.23±0.43(Predicted)
Farbe	white to beige

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3
HS Code	2933.59.8000
HazardClass	6.1
PackingGroup	III

Gefahreninformationscode (GHS)

Beschreibung
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).
Chemische Eigenschaften
Off-White Solid
Verwenden
Labelled Pelitinib (P218702). A tyrosine kinase inhibitor; it is used to prepare formulation for treating primary or secondary cancer.
Verwenden
An EGFR inhibitor
Verwenden
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
Lager
Store at -20°C
Einzelnachweise
[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.