2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FAK Pyk2 Apoptosis
  4. 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).

For research use only. We do not sell to patients.

GZD-257

GZD-257 Chemical Structure

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GZD-257 Related Antibodies

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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].

In Vitro

GZD-257 (Compound 7) shows potent activity against glioma cell lines U118-MG (IC50 = 1.64 μM) and U87-MG (IC50 = 1.40 μM), and lower potency against LO2 cells (IC50 = 9.35 μM)[1].
GZD-257 (10 μM, 16 h) shows a permeability coefficient (Pe) of 43.85× 10-6 cm/s, demonstrating excellent blood-brain barrier penetration ability[1].
GZD-257 (1-20 μM, 24 h) induces late apoptosis in a concentration-dependent manner in U118-MG cells[1].
GZD-257 (1-20 μM) causes G2/M phase arrest, with the proportion increasing from 10.38 % to 67.19 % in U118-MG cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GZD-257 Related Antibodies

Apoptosis Analysis[1]

Cell Line: U118-MG cells
Concentration: 1 μM, 5 μM, 10 μM, 20 μM
Incubation Time: 24 h
Result: Induces late apoptosis in a concentration-dependent manner: 8.42 % at 1 μM, 9.65 % at 5 μM, 11.6 % at 10 μM, and 36.8 % at 20 μM.
Molecular Weight

525.00

Formula

C26H29ClN6O4
SMILES

ClC(C=N1)=C(NC2=CC3=CC=C2C(NC)=O)N=C1NC(C=C4)=CC(OCCCCO3)=C4N5CCOCC5
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GZD-257 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GZD-257GZD257GZD 257FAKPyk2ApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2DesignmGlioblastomaMacrocyclizationInhibitorinhibitorinhibit

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