ChemicalBook--->CAS DataBase List--->793726-84-8

793726-84-8

793726-84-8 Structure

793726-84-8 Structure
IdentificationBack Directory
[Name]

BIBU 1361 DIHYDROCHLORIDE
[CAS]

793726-84-8
[Synonyms]

BIBU 1361
BIBU1361 (BIBU 1361 )
BIBU 1361 DIHYDROCHLORIDE
N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]pyrimido[5,4-d]pyrimidin-4-amine
N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-aminedihydrochloride
N-(3-CHLORO-4-FLUOROPHENYL)-6-[4-[(DIETHYLAMINO)METHYL]-1-PIPERIDINYL]-PYRIMIDO[5,4-D]PYRIMIDIN-4-AMINE DIHYDROCHLORIDE
[Molecular Formula]

C22H27ClFN7
[MDL Number]

MFCD08703120
[MOL File]

793726-84-8.mol
[Molecular Weight]

443.95
Chemical PropertiesBack Directory
[storage temp. ]

Desiccate at +4°C
[solubility ]

DMSO (Slightly), Methanol (Very Slightly)
[form ]

Solid
[color ]

Yellow
Hazard InformationBack Directory
[Uses]

BIBU 1361 Dihydrochloride, is a potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). It also blocks downstream EGFR signaling events such as MAPKK/MAPK activation.
[Biological Activity]

Potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC 50 = 3 nM). Displays ~ 100-fold lower potency against ErbB2 (IC 50 = 290 nM) and is selective over a range of other related tyrosine kinases (IC 50 > 10 μ M). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.
[storage]

Store at -20°C
[References]

[1]. antczak c, mahida jp, bhinder b, et al. a high-content biosensor-based screen identifies cell-permeable activators and inhibitors of egfr function implications in drug discovery. journal of biomolecular screening, 2012, 17(7): 885-899.
[2]. ghildiyal r, dixit d, sen e. egfr inhibitor bibu induces apoptosis and defective autophagy in glioma cells. molecular carcinogenesis, 2013, 52(12): 970-982.
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