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BIBX 1382
Cat No.
CEI-1244
Product Overview
BIBX1382 is a potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with IC50 value of 3 nM. 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. 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.
CAS No.
196612-93-8
Molecular Weight
387.84
Storage
Store at -20°C
Synonyms
Falnidamol; BIBX-1382; BIBX1382
Targets
EGFR
Molecular Formula
C18H19ClFN7
Chemical Name
4-N-(3-chloro-4-fluorophenyl)-6-N-(1-methylpiperidin-4-yl)pyrimido[5,4-d]pyrimidine-4,6-diamine
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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