Epitinib

• Description :

  Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer[1][2]. Epitinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

• Product Name Alternative :

  HMPL-813

• UNSPSC :

  12352005

• 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/epitinib.html

• Purity :

  99.95

• Solubility :

  10 mM in DMSO

• Smiles :

  O=C(N1CCN(CC)CC1)NC2=CC3=C(NC4=CC=CC(C#C)=C4)N=CN=C3C=C2OC

• Molecular Formula :

  C24H26N6O2

• Molecular Weight :

  430.50

• References & Citations :

  [1] Zhou et al. The safety profile of a selective EGFR TKI epitinib (HMPL-813) in patients with advanced solid tumors and preliminary clinical efficacy in EGFRm+ NSCLC patients with brain metastasis. Journal of Clinical Oncology 2016 34:15_suppl, e20502-e20502|[2] Zhou et al. Phase I study of the safety and pharmacokinetics of epitinib, an oral EGFR tyrosine kinase inhibitor, in patients with advanced solid tumors. Journal of Clinical Oncology 2013 31:15_suppl, e19042-e19042

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, stored under nitrogen)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• CAS Number :

  [1203902-67-3]