BIBX 1382 dihydrochloride

Cat. No. 2416

BIBX 1382 dihydrochloride C18H19ClFN7.2HCl [1216920-18-1]

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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:
1216920-18-1

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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

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.

If you know of a relevant reference for BIBX 1382 dihydrochloride please let us know.

Citations are publications that use Tocris products. Selected citations for BIBX 1382 dihydrochloride include:

Xia et al (2013) Identification of repurposed small molecule drugs for chordoma therapy. Cancer Biol Ther 14 638. PMID: 23792643.

Do you know of a great paper that uses BIBX 1382 dihydrochloride from Tocris? If so please let us know.

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Keywords: BIBX 1382 dihydrochloride, supplier, selective, EGFR-kinases, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBX1382, dihydrochloride, Tocris Bioscience, EGFR Inhibitor products

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