Sunday, December 7, 2014

Pelitinib is a tyrosine kinase inhibitor


Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM.
Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. EKB-569 irreversibly binds covalently to epidermal growth factor receptors (EGFR) ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these receptors. Check for active clinical trials or closed clinical trials using this agent.
Appearance: White to off-white solid
CAS :  257933-82-7
Molecular Formula: C₂₄H₂₃ClFN₅O₂
Molecular Weight: 467.92
Purity: ≥98% by HPLC
Solubility:DMSO (>10 mg/ml)
Storage Temp.: -20 ̊C
Handling: Protect from air and light

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