CL-387785

SKU: orb1223206

Description

CL-387785, also known as EKI-785 , is a n 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.

Key Properties

• CAS Number: 194423-06-8
• MW: 381.23
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₃BrN₄O
• SMILES: CC#CC(=O)Nc1cc2c(cc1)ncnc2Nc1cc(ccc1)Br
• Target: VEGFR
• Solubility: DMSO : 13.67 mg/mL 35.86 mM

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CL387785 | CL 387785 | CL-387785

Quick Database Links

Gene Symbol

VEGFR