Description:
CL-387785, also known as EKI-785, is an irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM). CL-387785 covalently bound to EGF-R. It also specifically inhibited kinase activity of the protein (IC50 = 370+/-120 pM), blocked EGF-stimulated autophosphorylation of the receptor in cells (ic50 approximately 5 nM), inhibited cell proliferation (IC50 = 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2, and profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice (when given orally at 80 mg/kg/day for 10 days, daily). CL-387,785 is useful for studying the interaction of small molecules with EGF-R and may have clinical utility.
- Molecular Weight: 381.233
- Molecular Formula: C18H13BrN4O
Purity: 0.98
Canonical SMILES:
CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br
InChI:
InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)
InChIKey: BTYYWOYVBXILOJ-UHFFFAOYSA-N
- Appearance: Solid powder
- Application: Protein Kinase Inhibitors
Synonyms:
CL-387785; CL 387785; CL-387,785; CL387785; EKI-785; EKI 785; EKI785
More details are to be found on supplier website
