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]