BIBX 1382 dihydrochloride

Cat No. 2416

BIBX 1382 dihydrochloride C18H19ClFN7.2HCl [196612-93-8]

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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:
>98 %
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 and MSDS.

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch
Material Safety Data Sheet: View current batch

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

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View Related Products by Target

Keywords: BIBX 1382 dihydrochloride, selective, EGFR-kinases, inhibitors, Epidermal, Growth, Factor, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBX1382, dihydrochloride

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