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BIBX 1382 dihydrochloride

Cat. No. 2416

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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:

460.77

Formula:

C₁₈H₁₉ClFN₇.2HCl

Solubility:

Soluble to 50 mM in water and to 50 mM in DMSO

Purity:

>97 %

Storage:

Desiccate at +4°C

CAS No:

196612-93-8

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Dittrich et al (2002) Phase I and pharmacokinetic study of BIBX1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur.J.Cancer 38 1072. PMID: 12008195.

Solca et al (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J.Pharmacol.Exp.Ther. 311 502. PMID: 15199094.

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