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Cat. No.: HY-183284

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GZD-552

Name: GZD-552
Brand: MedChemExpress
SKU: HY-183284
Price: 288.00 USD
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GZD-552 is a potent orally active FAK inhibitor with a human FAK IC₅₀ of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G₂/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme.

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

Formula: C₂₇H₃₀F₃N₅O₆
Molecular Weight:577.55

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

GZD-552 Chemical Structure

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Fluorescent Dye

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

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

All ERK Isoforms :

In Vitro

GZD-552 (compound 16c) potently and selectively inhibits the proliferation of U87-MG and U118-MG glioblastoma cells with IC₅₀ values of 6.6 nM and 4.3 nM, respectively, and shows limited activity against NCI-H1975 (IC₅₀ = 0.16 μM), MDA-MB-231 (IC₅₀ = 0.28 μM), and LO2 cells (IC₅₀ = 0.74 μM)^[1].
GZD-552 strongly and stably binds to FAK protein in U87-MG cells^[1].
GZD-552 (0.002-0.08 μM) suppresses FAK protein expression and activation, and downregulates downstream ERK phosphorylation in U87-MG cells in a concentration-dependent manner^[1].
GZD-552 (0.004-0.12 μM; 24 h) induces dose-dependent apoptosis and G₂/M cell cycle arrest in U87-MG cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

U87-MG cells
Concentration:

0.004; 0.04; 0.08; 0.12 μM
Incubation Time:

24 h
Result:

Induced apoptosis in U87-MG cells in a concentration manner.
Exhibited early apoptosis rate of 8.99% and the late apoptosis rate of 19% at 0.12 μM.

Apoptosis Analysis^[1]

Cell Line:

U87-MG cells
Concentration:

0.004; 0.04; 0.08; 0.12 μM
Incubation Time:

24 h
Result:

Induced G2/M cell cycle arrest in U87-MG cells in a concentration manner.
Increased the proportions of cells in
the G2/M phase to 54.09%, 57.22%, 68.77%, and 71.74%, at 0.004, 0.04, 0.08, and 0.12 μM, respectively.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	F	V_z	CL
Mice^[1]	2 mg/kg	i.v.	1299 ng/mL	0.361 h	461 ng·h/mL	466 ng·h/mL	0.254 h	0.277 h	/	2457 mL/kg	4814 mL/h/kg
Mice^[1]	10 mg/kg	i.g.	467 ng/mL	1.90 h	274 ng·h/mL	279 ng·h/mL	1.07 h	1.25 h	18.7 %	/	/

In Vivo

GZD-552 (compound 16c) (10 and 20 mg/kg/day; i.g.; daily; 18 days) inhibits tumor growth in mouse U87-MG xenograft model without detectable systemic toxicity^[1].

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

Animal Model:

Female BALB/c nude mice (5-week-old, 18-22 g) subcutaneously injected with U87-MG cells^[1]
Dosage:

10; 20 mg/kg/day
Administration:

i.g.; daily; 18 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 92.36%.
Achieved a tumor growth inhibition (TGI) rate of 96.68%.
Caused no significant fluctuations in mouse body weight.
Showed no histological abnormalities in heart, liver, spleen, lung, and kidney compared to the control group.
Significantly inhibited FAK, p-FAK, ERK, and p-ERK protein expression in tumor tissues.

Chemical Information

Molecular Weight 577.55
Formula C₂₇H₃₀F₃N₅O₆
SMILES

O=C(NC)C1=CC=CC=C1NC2=C(C(F)(F)F)C=NC(NC3=CC=C4C(OCCOCCOCCOCCO4)=C3)=N2
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

Handling Instructions (2659 KB)

References

[1]. Xu Y, et al. Design, synthesis, and anti-glioblastoma multiforme evaluation of novel multikinase inhibitors via a cyclization strategy with potent FAK inhibition. Eur J Med Chem. 2026;312:118877. [Content Brief]

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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.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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GZD-552

All ERK Isoforms