CL-387785

• Description:

  CL-387785 (EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.

• Product Name Alternative:

  EKI-785; WAY-EKI 785

• UNSPSC:

  12352005

• Hazard Statement:

  H315, H317, H318, H334, H335, H341, H361, H370, H413

• Target:

  EGFR

• Type:

  Reference compound

• Related Pathways:

  JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/CL-387785.html

• Purity:

  98.05

• Solubility:

  DMSO : 13.67 mg/mL (ultrasonic; warming)

• Smiles:

  O=C(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)C#CC

• Molecular Formula:

  C18H13BrN4O

• Molecular Weight:

  381.23

• Precautions:

  H315, H317, H318, H334, H335, H341, H361, H370, H413

• References & Citations:

  [1]Discafani CM, et al. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[ (3-bromophenyl) amino]-6-quinazolinyl]-2-butynamide (CL-387,785) . Biochem Pharmacol. 1999 Apr 15;57 (8) :917-25.|[2]Sweeney WE, et al. Treatment of polycystic kidney disease with a novel tyrosine kinase inhibitor. Kidney Int. 2000 Jan;57 (1) :33-40.|[3]Greulich H, et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med. 2005 Nov;2 (11) :e313.|[4]Kobayashi S, et al. An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res. 2005 Aug 15;65 (16) :7096-101.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  EGFR/ErbB1/HER1

• CAS Number:

  194423-06-8