CL-387785

SKU: orb1305914

Description

CL-387785

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 194423-06-8
• MW: 381.23
• Purity: 99.56%
• Formula: C₁₈H₁₃BrN₄O
• SMILES: CC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
• Target: EGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:60 mg/mL (157.39 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR:370+/-120 pM
• In Vivo:
  CL-387785 effectively blocks EGF-mediated receptor autophosphorylation in cells IC50 5 nM). It principally acts as a cellular inhibitor, suppressing cell proliferation in cell lines overexpressing EGF-R or c-erbB-2 IC50 31 nM).
• In Vitro:
  CL-387785 demonstrates significant inhibitory effects o the growth of HCT-116-induced xenograft tumors at a dose of 50 mg/kg. In nude mice expressing EGF-R, CL-387785 administered orally at 80 mg/kg/day effectively suppresses tumor growth. In a mouse model of autosomal recessive polycystic kidney disease, treatment with CL-387785 at 90 mg/kg intraperitoneally in Balb/c-bpk/bpk (BPK) mice significantly reduces cystic lesions in collecting ducts, improves kidney function, decreases abnormalities in bile duct epithelial cells, and extends lifespan. At 25 mg/kg, CL-387785 can reduc the growth of HCA-7-induced xenograft tumors, and a dose of 100 mg/kg completely inhibits tumor growth.
• Cell Research:
  MTS assays are performed wit the CellTiter 96@ AQueous One solution proliferation kit. A total of 10,000 cells per well in 96-well flat-bottomed plates are incubated with various concentration of inhibitors for 48 h the IC50 is determined from dose–response curves using XL Fit 4.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

WAY-EKI-785, WAY-EKI785, WAY-EKI 785, CL387785, CL-387785, CL 387785, EKI 785, EKI785, EKI-785, EGFR

Compound Identifiers

PubChem CID

2776