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BIBX 1382

Catalog No.
EGFR inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
Ship with 10-15 days
Ship with 10-15 days
Ship with 10-15 days

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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]

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.

Chemical Properties

StorageStore at -20°C
Cas No.196612-93-8
SolubilitySoluble in DMSO
Chemical NameN8-(3-chloro-4-fluorophenyl)-N2-(1-methylpiperidin-4-yl)pyrimido[5,4-d]pyrimidine-2,8-diamine
SDFDownload SDF
Canonical SMILESCN1CCC(NC2=NC=C3C(C(NC4=CC(Cl)=C(F)C=C4)=NC=N3)=N2)CC1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

BIBX 1382