MAZ51

Alias: MAZ51; MAZ-51; MAZ 51
Cat No.:V2187 Purity: ≥98%
Decsription: MAZ-51 is a novel, potent and selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase.
MAZ51 Chemical Structure CAS No.: 163655-37-6
Product category: VEGFR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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10mg
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50mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
MAZ-51 is a novel, potent and selective tyrosine kinase inhibitor for VEGFR-3 (Flt-4). Without obstructing VEGF-C-mediated stimulation of VEGFR2, MAZ51 suppresses VEGF-C-induced activation of VEGFR-3. MAZ51 had no effect on EGFR, IGF-1R, or PDGFRβ autophosphorylation induced by ligands. MAZ51 causes apoptosis and inhibits the growth of many tumor cell types. anticancer action.
Biological Activity I Assay Protocols (From Reference)
Targets
VEGFR-3; Akt; GSK3β; RhoA
ln Vitro
MAZ51 (2.5-10 μM; 24 hours) causes apoptosis and inhibits the growth of many different types of tumor cells[2]. MAZ51 (0.5-50 μM; 25 minutes) does not affect the ligand-induced autophosphorylation of PDGFRβ, IGF-1R, or EGFR in A431 cells, HEK-293 cells, or PAE cells, respectively[2].
ln Vivo
MAZ51 (8 mg/kg; i.p.; daily for 15 day) tumor growth is significantly suppressed by MAZ51[2].
Animal Protocol
Wistar Furth rats (bearing MT450 cells)[1]
8 mg/kg
Intraperitoneal injection; daily for 15 day
References

[1]. Characterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2. Eur J Biochem. 2001 Nov;268(21):5530-40.

[2]. MAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo. Int J Cancer. 2004 Dec 20;112(6):986-93.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₂₁H₁₈N₂O
Molecular Weight
314.38
Exact Mass
314.141913202
CAS #
163655-37-6
Related CAS #
163655-37-6
Appearance
Solid
SMILES
CN(C)C1=CC=C(C2=CC=CC=C21)/C=C/3\C4=CC=CC=C4NC3=O
InChi Key
VFCXONOPGCDDBQ-QGOAFFKASA-N
InChi Code
InChI=1S/C21H18N2O/c1-23(2)20-12-11-14(15-7-3-4-9-17(15)20)13-18-16-8-5-6-10-19(16)22-21(18)24/h3-13H,1-2H3,(H,22,24)/b18-13+
Chemical Name
(3E)-3-[[4-(dimethylamino)naphthalen-1-yl]methylidene]-1H-indol-2-one
Synonyms
MAZ51; MAZ-51; MAZ 51
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 11.4~63 mg/mL (36.1~200.4 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: 4 mg/mL (12.72 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.3181 mL 1.5904 mL 3.1809 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • Enter 10 in the Concentration box and choose the correct unit (mM)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • In vitro kinase assays were performed with the indicated recombinant kinases. Differing amounts of MAZ51 were included in the reactions to test the effect of MAZ51 on the activity of the different kinases. Int J Cancer . 2004 Dec 20;112(6):986-93.
  • Typical H&E-stained sections of tumors from control animals treated with DMSO (a) or treated with MAZ51 (b). Scale bar = 100 μm. Int J Cancer . 2004 Dec 20;112(6):986-93
  • Chemical structure of MAE87, MAE106 and MAZ51. Eur J Biochem . 2001 Nov;268(21):5530-40.
  •  Effect of MAE87, MAE106 and MAZ51 on VEGF-C-induced phosphorylation of VEGFR-2 and VEGFR-3. Eur J Biochem . 2001 Nov;268(21):5530-40.
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