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

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.

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MAZ51 Chemical Structure

MAZ51 Chemical Structure

CAS No. : 163655-37-6

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Based on 2 publication(s) in Google Scholar

MAZ51 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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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[1]

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].

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

MAZ51 Related Antibodies

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].

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

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.
Appearance

Solid

Color

Orange to red

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (26.50 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1809 mL 15.9043 mL 31.8086 mL
5 mM 0.6362 mL 3.1809 mL 6.3617 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.83 mg/mL (2.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 4 mg/mL (12.72 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.96%

COA (257 KB) HNMR (265 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1809 mL 15.9043 mL 31.8086 mL 79.5216 mL
5 mM 0.6362 mL 3.1809 mL 6.3617 mL 15.9043 mL
10 mM 0.3181 mL 1.5904 mL 3.1809 mL 7.9522 mL
15 mM 0.2121 mL 1.0603 mL 2.1206 mL 5.3014 mL
20 mM 0.1590 mL 0.7952 mL 1.5904 mL 3.9761 mL
25 mM 0.1272 mL 0.6362 mL 1.2723 mL 3.1809 mL
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MAZ51 Related Classifications

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:

MAZ51163655-37-6MAZ 51MAZ-51VEGFRApoptosisVascular endothelial growth factor receptorindolinoneVEGF-CVEGF-Dtumorgrowthapoptosisproliferationligand-inducedIGF-1REGFRPDGFRβphosphorylationInhibitorinhibitorinhibit

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