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Chemical Structure| 163655-37-6 Chemical Structure| 163655-37-6

Structure of MAZ51
CAS No.: 163655-37-6

Chemical Structure| 163655-37-6

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MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase.

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Product Details of MAZ51

CAS No. :163655-37-6
Formula : C21H18N2O
M.W : 314.38
SMILES Code : O=C1NC2=C(C=CC=C2)/C1=C\C3=C4C=CC=CC4=C(N(C)C)C=C3
MDL No. :MFCD04036983

Safety of MAZ51

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of MAZ51

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PC-3 cells 3 μM 18 hours Attenuated VEGF-C-induced migration of PC-3 cells Front Pharmacol. 2021 Apr 20;12:667474
PC-3 cells 2.7 μM (IC50) 48 hours Inhibited PC-3 cell proliferation Front Pharmacol. 2021 Apr 20;12:667474
PC-3 cells 1-10 μM 48 hours Reduced VEGFR-3 expression and p-Akt levels Front Pharmacol. 2021 Apr 20;12:667474
CD34+CD38- cells 5 μM 3 hours Inhibition of FLT4 activity, reducing homing and engraftment capacity of AML cells Haematologica. 2023 Nov 1;108(11):2933-2945
AML-MNC 5 μM 2 hours Inhibition of FLT4 tyrosine kinase activity, reducing leukemic colony formation Haematologica. 2023 Nov 1;108(11):2933-2945
human umbilical vein endothelial cells (HUVECs) 10 μM 12 hours MAZ51 significantly suppressed LPA-induced HUVEC tube formation and Prox-1 expression Cell Mol Life Sci. 2008 Sep;65(17):2740-51
human umbilical vein endothelial cells (HUVECs) 10 μM 12 hours MAZ51 significantly suppressed the enhancement effects of LPA on Prox-1, LYVE-1, and podoplanin protein expressions in HUVECs Cell Mol Life Sci. 2008 Sep;65(17):2740-51
PC-3 cells 3 μM 4 hours Inhibited VEGF-C-induced phosphorylation of VEGFR-3 Front Pharmacol. 2021 Apr 20;12:667474
TF cells 10 µmol/L 12 hours MAZ51 inhibits FLT-4 activity, reducing VEGF-A and VEGF-C expression Am J Pathol. 2009 Oct;175(4):1709-21
SAS cells 10 µmol/L 12 hours MAZ51 inhibits FLT-4 activity, reducing VEGF-A and VEGF-C expression Am J Pathol. 2009 Oct;175(4):1709-21
lymphatic endothelial cells (LECs) 7.5 μM 24 hours To investigate the effect of MAZ51 on the proliferation, migration, and protein expression of VEGF-C and VEGFR-3 in lymphatic endothelial cells. Results showed that MAZ51 significantly reduced VEGFR-3 protein expression, and SAB could reverse this effect. Front Pharmacol. 2022 Aug 11;13:915161

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Leukemic xenograft model Intravenous injection 5 μM Single injection, observed for 8 to 15 weeks MAZ51 treatment significantly reduced homing efficiency of AML blasts to BM and PB and inhibited engraftment of CD45dim blasts Haematologica. 2023 Nov 1;108(11):2933-2945
NOD-SCID mice QGP-1 xenograft model Intraperitoneal injection 8 mg/kg 2 weeks (5 days of treatment and 2 days of rest) MAZ51 significantly suppressed the invasiveness of QGP-1 xenografts with PTEN knockdown J Biomed Sci. 2022 Nov 6;29(1):92
Zebrafish Transgenic zebrafish embryos Embryo water treatment 30μM 6 hours pretreatment followed by 48 hours PNS treatment MAZ51 severely impaired the length of TD formation, but PNS treatment significantly increased the length of TD formation J Ethnopharmacol. 2016 Dec 4;193:293-302
BALB/c-nu/nu mice Xenograft mouse model Subcutaneous injection 1 or 3 μM Daily administration for 1-4 weeks Blocked tumor growth of PC-3 cells Front Pharmacol. 2021 Apr 20;12:667474
Zebrafish Zebrafish embryo model Aqueous solution treatment 30 μM Pretreatment for 6 hours, followed by treatment for 48 hours To investigate the effect of MAZ51 on lymphatic vessel formation in zebrafish. Results showed that MAZ51 significantly impaired thoracic duct formation, and KXF could ameliorate this damage. Front Pharmacol. 2022 Aug 11;13:915161
BALB/c nude mice C33A subcutaneous xenograft model Intraperitoneal injection 8 mg/kg Once daily for 15 days To investigate the effect of MAZ51 on TNF-α-promoted tumorigenesis, lymphangiogenesis, and lymphatic metastasis in cervical cancer. Results showed that MAZ51 inhibited these promoting effects of TNF-α and reduced the expression of p-AKT and p-ERK in tumor tissues. Mediators Inflamm. 2023 Apr 21;2023:5679966

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.90mL

3.18mL

1.59mL

31.81mL

6.36mL

3.18mL

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