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Cat. No.: HY-178969

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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.

Formula: C₂₆H₂₉ClN₆O₄
Molecular Weight:525.00

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

GZD-257 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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.

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.

Chemical Information

Molecular Weight 525.00
Formula C₂₆H₂₉ClN₆O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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