CL-387785 (EKI-785)

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Description:IC50: 370 pMThe EGFR is a 170-kDa protein that contains an extracellular ligand binding domain, a single transmembrane domain, and an intracellular tyrosine kinase domain. EGF-R is hyperactivated in numerous tumors including those derived from the lung, brain, bladder, prostate, head, and neck. It has been shown previously that 4-anilino quinazolines compete with the ability of ATP binding the EGFR, inhibit EGF-stimulated autophosphorylation of tyrosine residues in EGFR, and block EGF-mediated growth. CL-387785 is an irreversible inhibiter of EGFR. In vitro: CL-387785 covalently bound to EGFR. It also specifically inhibited kinase activity of the protein, blocked EGF-stimulated autophosphorylation of the receptor in cells, inhibited cell proliferation primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2 [1]. In vivo: The effects of CL-387785 on tumor growth were assessed in human tumor xenografts implanted s.c. in the flanks of nude mice. CL-387785 inhibited the growth of tumors derived from A431 cells when the drug was administered i.p. or p.o.. Inhibitory effects were observed within 7 days after the onset of therapy. No efficacy was observed with CL-387785 in tumors derived from cell lines that did not overexpress EGF-R, including the human breast carcinoma MDA-MB-435 [1]. Clinical trial: Up to now, CL-387785 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    N-(4-((3-bromophenyl)amino)quinazolin-6-yl)but-2-ynamide
    
    CAS Number
    
    194423-06-8
    
    Molecular Formula
    
    C18H13BrN4O
    
    Molecular Weight
    
    381.23
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥16.85 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CL-387785 (EKI-785)

Background

We Also Recommend

LED209

Regadenoson

Tiplaxtinin(PAI-039)