2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway Apoptosis
  3. FAK ERK Apoptosis
  4. GZD-552

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.

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GZD-552

GZD-552 Chemical Structure

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Description

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[1].

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.

GZD-552 Related Antibodies

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 Cmax T1/2 AUC0-t AUC0-∞ MRT0-t MRT0-∞ F Vz 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.
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
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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-552 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-552GZD552GZD 552FAKERKApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseExtracellular signal regulated kinasesG2/M cell cycle arrestERK signalingxenograft modelBALB/c nude mouseU87-MGU118-MGnormal hepatocytesglioblastoma multiforme cellsapoptotic cell deathInhibitorinhibitorinhibit

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