1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. VEGFR
    Apoptosis
  3. MAZ51

MAZ51 

Cat. No.: HY-116624
Handling Instructions

MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.

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

MAZ51 Chemical Structure

MAZ51 Chemical Structure

CAS No. : 163655-37-6

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Description

MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity[1][2].

IC50 & Target

VEGFR3

 

In Vitro

MAZ51 (2.5-10 μM; 24 hours) blocks proliferation and induces apoptosis in a wide variety of tumor cells[2].
MAZ51 (0.5-50 μM; 25 minutes) has no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ in A431 cells, HEK-293 cells, and PAE cells, respectively[2].

Cell Proliferation Assay[2]

Cell Line: MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells
Concentration: 2.5, 10 μM
Incubation Time: 24 hours
Result: Induced apoptosis in a wide variety of tumor cells.

Apoptosis Analysis[2]

Cell Line: MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells
Concentration: 2.5, 10 μM
Incubation Time: 24 hours
Result: Blocked proliferation in a wide variety of tumor cells.
In Vivo

MAZ51 (8 mg/kg; i.p.; daily for 15 day) significantly suppresses the growth of MT450 tumors[2].

Animal Model: Wistar Furth rats (bearing MT450 cells)[1]
Dosage: 8 mg/kg
Administration: Intraperitoneal injection; daily for 15 day
Result: Significantly suppressed the growth of MT450 tumors.
Molecular Weight

314.38

Formula

C₂₁H₁₈N₂O

CAS No.

163655-37-6

SMILES

CN(C1=C2C=CC=CC2=C(C=C1)/C=C3C(NC4=C/3C=CC=C4)=O)C

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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.

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Keywords:

MAZ51MAZ 51MAZ-51VEGFRApoptosisVascular endothelial growth factor receptorindolinoneVEGF-CVEGF-Dtumorgrowthapoptosisproliferationligand-inducedIGF-1REGFRPDGFRβphosphorylationInhibitorinhibitorinhibit

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