BIBX 1382

Short Summary : EGFR inhibitor,potent and selective

Category : Tyrosine Kinase|EGFR

Purity : 0.98

CAS Number : 196612-93-8

Formula : C18H19ClFN7

Molecular Weight : 387.84

SMILE : CN1CCC(NC2=NC=C3C(C(NC4=CC(Cl)=C(F)C=C4)=NC=N3)=N2)CC1

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : BIBX1382 is a potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with IC50 value of 3 nM.[1]
BIBX1382 is an inhibitor of EGFR kinase for treatment of cancer. In a tyrosine kinase activity assay using cytoplasmic tyrosine kinase domains of EGFR, HER2, VEGFR2, HGFR, IGF1R, B-InsRK and c-src cloning and expressing in Sf9 insect cells, BIBX1382 selectively and potently inhibited EGFR kinase activity with an IC50 value of 3 nM. In the EGFR and pEGFR ELISA assay using EGFR highly expressed A431 cells (vuval squamous cell carcinoma), BIBX1382 inhibited EGFR phosphorylation at EC50 at 141 nM.[1] In A431, FaDu (hypopharyngeal squamous cell carcinoma) and HN5 (head and neck squamous cell carcinoma) xenograft nude mice models, oral administration of BIBX1382 at dose of 10 mg/kg daily showed strong antitumor activity in a dose-dependent manner after 2 weeks of treatment. Moreover, tumor regressions were obtained after 170 days long term oral administration of BIBX1382 at dose of 50 mg/kg daily in A431 xenograft nice model.[1]
References:1. F. F. Solca, A. Baum, E. Langkopf, G. Dahmann, K. H. Heider, F. Himmelsbach and J. C. van Meel, J Pharmacol Exp Ther 2004, 311, 502-509.

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