BIBU 1361 dihydrochloride

Cat. No. 2417

BIBU 1361 dihydrochloride C22H27ClFN7.2HCl [793726-84-8]

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Chemical Name: N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride

Biological Activity

Potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays ~ 100-fold lower potency against ErbB2 (IC50 = 290 nM) and is selective over a range of other related tyrosine kinases (IC50 > 10 μM). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.

Technical Data

M.Wt:
516.87
Formula:
C22H27ClFN7.2HCl
Solubility:
Soluble to 100 mM in water and to 25 mM in DMSO
Purity:
>97 %
Storage:
Desiccate at +4°C
CAS No:
793726-84-8

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.

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Keywords: BIBU 1361 dihydrochloride, supplier, Selective, inhibitors, inhibits, EGFR-kinases, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBU1361, dihydrochloride, Tocris Bioscience, EGFR Inhibitor products

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