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Referencia número: 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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₂₆H₂₉ClN₆O₄
Peso molecular:525.00

Almacenamiento:

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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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- In Vitro
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

Peso molecular 525.00
Fòrmula C₂₆H₂₉ClN₆O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (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)
Instrucciones de manejo (2659 KB)

Referencias

[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

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

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MOQ

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100 mg

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