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BIBU1361 dihydrochloride

Chemical Structure : BIBU1361 dihydrochloride

CAS No.: 1643609-75-9

BIBU1361 dihydrochloride (BIBU 1361 )

Catalog No.: PC-62999Not For Human Use, Lab Use Only.

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).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 516.871
Formula C22H29Cl3FN7
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

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.

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