A cyanoquinoline that irreversibly inhibits the receptor tyrosine kinases EGFR (IC50 = 39 nM) and HER2 (IC50 = 1.2 μM); disrupts Akt and MAPK pathways

Pelitinib – 25 mg

Brand:
Cayman
CAS:
257933-82-7
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Pelitinib is a cyanoquinoline that irreversibly inhibits the EGFR receptor tyrosine kinase (IC50 = 39 nM).{21790} It inhibits HER2 with a much weaker potency (IC50 = 1.2 μM).{21790} 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).{25562}  

 

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Description

A cyanoquinoline that irreversibly inhibits the receptor tyrosine kinases EGFR (IC50 = 39 nM) and HER2 (IC50 = 1.2 μM); disrupts Akt and MAPK pathways, inducing apoptosis and suppressing the growth of tumor cell lines

Formal name: N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2E-butenamide

Synonyms:  EKB-569

Molecular weight: 467.9

CAS: 257933-82-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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