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BIBU 1361 dihydrochloride

Names

[ CAS No. ]:
1643609-75-9

[ Name ]:
BIBU 1361 dihydrochloride

[Synonym ]:
N-(3-Chloro-4-fluorophenyl)-6-{4-[(diethylamino)methyl]-1-piperidinyl}pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride
Pyrimido[5,4-d]pyrimidin-4-amine, N-(3-chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-, hydrochloride (1:2)
N-(3-Chloro-4-fluorophenyl)-6-{4-[(diethylamino)methyl]piperidin-1-yl}pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride

Biological Activity

[Description]:

BIBU1361 is a potent, selective, orally active EGFR inhibitor with IC50 of 3 nM, shows weak activity against HER2 (IC50=280 nM) and no inhibition on IGF1R, HGFR, Src, and VEGFR2 (IC50>10 uM); inhibits EGF-induced phosphorylation of EGFR in a dose-dependent manner in A431 cells (EC50=122 nM); demonstrates effectivity in tumour xenografts mice.

[References]

References 1. Solca FF, et al. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9. 2. Ghildiyal R, et al. Mol Carcinog. 2013 Dec;52(12):970-82. View Related Products by Target EGFR

Chemical & Physical Properties

[ Molecular Formula ]:
C22H29Cl3FN7

[ Molecular Weight ]:
516.870

[ Exact Mass ]:
515.153381

Related Compounds