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BIBU 1361 dihydrochloride

Cat. No. 2417

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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.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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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