MAZ51 |
Catalog No.GC16483
One-Click Copy Product Info
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MAZ51 is a selective vascular endothelial growth factor receptor 3 (VEGFR-3; FLT4) tyrosine kinase inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 163655-37-6
Sample solution is provided at 25 µL, 10mM.
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MAZ51 is a selective vascular endothelial growth factor receptor 3 (VEGFR-3; FLT4) tyrosine kinase inhibitor[1]. MAZ51 is an indolinone-based molecule that inhibits the proliferation of human endothelial cells and tumor cells and induces apoptosis[2]. MAZ51 can aggravate cisplatin nephrotoxicity[3].
In vitro, pretreatment of human prostate cancer PC-3 cells with MAZ51 (3μM) for 4h inhibited vascular endothelial growth factor C (VEGF-C)-induced vascular endothelial growth factor receptor 3 (VEGFR-3) phosphorylation and blocked serine/threonine kinase (Akt) phosphorylation[4]. MAZ51 (2.5-5μM) for 24h in two glioma cell lines (rat C6 and human U251MG cells) induced morphological changes in glioma cell lines and induced G2/M cell cycle arrest[5].
In vivo, MAZ51 (8mg/kg) was intraperitoneally injected into rats bearing mammary tumor MT450 cell xenografts, which significantly inhibited tumor growth and reduced the number of proliferating cell nuclear antigen (PCNA)-positive cells[6]. MAZ51 (10mg/kg) was subcutaneously injected into mice with full-thickness skin lesions, which may have affected lymphangiogenesis but not angiogenesis[7].
References:
[1] Varney M L, Singh R K. VEGF-C-VEGFR3/Flt4 axis regulates mammary tumor growth and metastasis in an autocrine manner[J]. American journal of cancer research, 2015, 5(2): 616.
[2] Hlophe Y N, Joubert A M. Vascular endothelial growth factor‐C in activating vascular endothelial growth factor receptor‐3 and chemokine receptor‐4 in melanoma adhesion[J]. Journal of Cellular and Molecular Medicine, 2022, 26(23): 5743-5754.
[3] Black L M, Farrell E R, Barwinska D, et al. VEGFR3 tyrosine kinase inhibition aggravates cisplatin nephrotoxicity[J]. American Journal of Physiology-Renal Physiology, 2021, 321(6): F675-F688.
[4] Yamamura A, Nayeem M J, Muramatsu H, et al. MAZ51 blocks the tumor growth of prostate cancer by inhibiting vascular endothelial growth factor receptor 3[J]. Frontiers in Pharmacology, 2021, 12: 667474.
[5] Park J H, Shin Y J, Riew T R, et al. The indolinone MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells without the inhibition of VEGFR-3 phosphorylation: involvement of the RhoA and Akt/GSK3β signaling pathways[J]. PLoS One, 2014, 9(9): e109055.
[6] Kirkin V, Thiele W, Baumann P, et al. MAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo[J]. International journal of cancer, 2004, 112(6): 986-993.
[7] Takada K, Nakajima Y, Urai T, et al. Effects of inhibition of lymphangiogenesis by the vascular endothelial growth factor receptor 3 (VEGFR-3) inhibitor, MAZ51 on full thickness wounds in mice[J]. Veins and Lymphatics, 2021, 10(1).
| Cell experiment [1]: | |
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Cell lines |
PC-3 cells |
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Preparation Method |
PC-3 cells were stimulated with 50ng/mL VEGF-C for 4h in the absence and presence of 3μM MAZ51. Phosphorylation signals of VEGFR-3 after VEGF-C-induced activation were detected by Western blotting. |
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Reaction Conditions |
3μM; 4h |
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Applications |
The VEGF-C-induced phosphorylation of VEGFR-3 was completely blocked by the pretreatment with 3μM MAZ51 for 4h. |
| Animal experiment [2]: | |
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Animal models |
Wistar Furth rats |
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Preparation Method |
MT450 cells (5×105 per animal) were injected subcutaneously into groups of Wistar Furth rats (8 rats per group). Subsequently, One group was intraperitoneally injected with 200μL DMSO per rat per day for the rest of the experiment. Another group was intraperitoneally injected daily with 200μL MAZ51(10mg/mL in DMSO) per rat, equating to a dose of 8mg/kg. Alternatively, tumors were allowed to grow to an average volume of 250mm3 before treatment commenced. Tumor volume was measured periodically following injection of tumor cells. |
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Dosage form |
8mg/kg; i.p. |
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Applications |
MAZ51 significantly suppresses the growth of MT450 tumors. |
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References: |
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| Cas No. | 163655-37-6 | SDF | |
| Chemical Name | 3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-2H-indol-2-one | ||
| Canonical SMILES | CN(C)C1=C(C=CC=C2)C2=C(/C=C3C(NC4=C/3C=CC=C4)=O)C=C1 | ||
| Formula | C21H18N2O | M.Wt | 314.4 |
| Solubility | 13.3mg/mL in DMSO with ultrasonic and warming. This product is unstable in solution and it is recommended to prepare and use it immediately. | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1807 mL | 15.9033 mL | 31.8066 mL |
| 5 mM | 636.1 μL | 3.1807 mL | 6.3613 mL |
| 10 mM | 318.1 μL | 1.5903 mL | 3.1807 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)