GZD-257
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].
Product Specifications
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
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