GZD-257

• Description:

  GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM) . GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM) [1].

• UNSPSC:

  12352005

• Target:

  Apoptosis; FAK; Pyk2

• Related Pathways:

  Apoptosis; Protein Tyrosine Kinase/RTK

• Field of Research:

  Cancer; Neurological Disease

• Smiles:

  ClC(C=N1)=C(NC2=CC3=CC=C2C(NC)=O)N=C1NC(C=C4)=CC(OCCCCO3)=C4N5CCOCC5

• Molecular Formula:

  C26H29ClN6O4

• Molecular Weight:

  525.00

• References & Citations:

  [1]Wu T, et al. Discovery of a macrocyclic FAK inhibitor GZD-257 for treatment of glioblastoma. Bioorg Med Chem Lett. 2025 Oct 2;130:130424.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported