BIBU 1361 DIHYDROCHLORIDE Property

Boiling point:

580.0±60.0 °C(Predicted)

Density 

1.285±0.06 g/cm3(Predicted)

storage temp. 

Desiccate at +4°C

solubility 

DMSO (Slightly), Methanol (Very Slightly)

form 

Solid

pka

10.32±0.25(Predicted)

color 

Yellow

Hazard and Precautionary Statements (GHS)

BIBU 1361 DIHYDROCHLORIDE Chemical Properties,Usage,Production

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.

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.