Pelitinib

• Description :

  Pelitinib (EKB-569; WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.

• Product Name Alternative :

  EKB-569; WAY-EKB 569

• UNSPSC :

  12352005

• Hazard Statement :

  H301

• Target :

  EGFR; Src

• 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/Pelitinib.html

• Purity :

  99.13

• Solubility :

  DMSO : 25 mg/mL (ultrasonic)

• Smiles :

  N#CC1=C(C2=CC(NC(/C=C/CN(C)C)=O)=C(OCC)C=C2N=C1)NC3=CC(Cl)=C(C=C3)F

• Molecular Formula :

  C24H23ClFN5O2

• Molecular Weight :

  467.92

• Precautions :

  H301

• References & Citations :

  [1]Torrance CJ, et al. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6 (9) :1024-8.|[2]Nunes M, et al. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3 (1) :21-7.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

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

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  EGFR/ErbB1/HER1

• CAS Number :

  [257933-82-7]