Catalog Number: 2416
Chemical Name: N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diamine dihydrochloride
Biological Activity
Potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). Oral administration inhibits growth of established human xenografts in athymic mice.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in water and to 50 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Phase I and pharmacokinetic study of BIBX1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration.
    Dittrich et al.
    Eur.J.Cancer, 2002;38:1072
  2. Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.
    Solca et al.
    J.Pharmacol.Exp.Ther., 2004;311:502

The citations listed below are publications that use Tocris products. Selected citations for BIBX 1382 dihydrochloride include:

Showing Results 1 - 1 of 1

  1. Identification of repurposed small molecule drugs for chordoma therapy.
    Authors: Xia Et al.
    Cancer Biol Ther
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