Chemical Property of N-(4-((3-bromophenyl)amino)quinazolin-6-yl)but-2-ynamide
Chemical Property:
- Melting Point:276 °C
- PKA:9.84±0.43(Predicted)
- PSA：70.40000
- Density:1.577±0.06 g/cm3(Predicted)
- LogP:4.82020
- Storage Temp.:Sealed in dry,Store in freezer, under -20°C
- Solubility.:insoluble in EtOH; insoluble in H2O; ≥16.85 mg/mL in DMSO
- XLogP3:4.3
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:3
- Exact Mass:380.02727
- Heavy Atom Count:24
- Complexity:514
- Purity/Quality:
-
99%, *data from raw suppliers
CL-387785(EKI-785) *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Canonical SMILES:CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br
-
Description
Overactivity of epidermal growth factor receptor (EGFR) tyrosine kinase activity has been associated with a number of cancers. CL 387,785 is a potent, irreversible inhibitor of EGFR kinase activity (IC50 = 370 pM). It blocks EGF-stimulated autophosphorylation of receptors in cells (IC50 = 5 nM) and halts cell cycling in cells that overexpress EGFR or c-ErbB2 (IC50s = 31-125 nM). CL 387,785 profoundly blocks the growth of EGFR-overexpressing tumors in nude mice when given orally at 80 mg/kg/day for 10 days.
-
Uses
CL-387785 (EKI-785) is an irreversible and selective EGFR inhibitor showing activity against mutations of the receptor. Potential therapeutic against various type of cancer, including lung cancer.
