MAZ51 |
カタログ番号GC16483
One-Click Copy Product Info
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MAZ51は選択的な血管内皮成長因子受容体3(VEGFR-3; FLT4)チロシンキナーゼ阻害剤である。
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は選択的な血管内皮成長因子受容体3(VEGFR-3; FLT4)チロシンキナーゼ阻害剤である[1]。MAZ51はインドリノンに基づいた分子であり、ヒト内皮細胞と腫瘍細胞の増殖を阻害し、アポトーシスを誘発する[2]。MAZ51はシスプラチン腎毒性を悪化させる[3]。
試験管内実験では、MAZ51 (3μM)でヒト前立腺癌PC-3細胞を4時間事前処理した結果、血管内皮成長因子C(VEGF-C)誘発の血管内皮成長因子受容体3(VEGFR-3)リン酸化を阻害し、セリン/スレオニンキナーゼ（Akt）リン酸化を遮断した[4]。MAZ51 (2.5-5μM)を二つの神経膠腫細胞株（ラットC6とヒトU251MG細胞）に24時間処理した結果、神経膠腫細胞株で形態変化を誘発し、G2/M細胞周期の停止を誘発した[5]。
生体内実験では、乳癌MT450細胞の異種移植を負うラットにMAZ51 (8mg/kg)を腹腔内注射した結果、著しく腫瘍増殖を阻害し、増殖細胞核抗原（PCNA）陽性細胞の数を減らした[6]。全層皮膚病変のマウスに、MAZ51 (10mg/kg)を皮下注射した結果、リンパ管新生を影響した可能性があるが、血管新生に影響はなかった[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).
| 細胞実験[1]: | |
細胞株 | PC-3細胞 |
準備方法 | 3μMのMAZ51のある/ない条件で、PC-3細胞を50ng/mLのVEGF-Cで4時間刺激した。VEGF-C-誘発性の活性後、VEGFR-3のリン酸化シグナルをウエスタンブロットで検出した。 |
反応条件 | 3μM；4時間 |
アプリケーション | 4時間の3μMのMAZ51事前処理の後、VEGFR-3のVEGF-C誘発性リン酸化は完全に遮断された。 |
| 動物実験 [2]: | |
動物モデル | Wistar Furthラット |
準備方法 | MT450細胞(1匹に5×105)をWistar Furthラット（8匹/グループ）のグループに皮下注射した。その後、実験が終わるまで、一つのグループに200μLのDMSO/ラット/日を腹腔内注射した。 もう一つのグループに、200μLのMAZ51(DMSOに10mg/mL)/ラット（8mg/kgの用量に同等）を毎日腹腔内注射した。あるいは、実験の開始前、腫瘍を250mm3の平均体積まで成長させた。腫瘍細胞の注射後、腫瘍の体積を定期的に測定した。 |
投与形態 | 8mg/kg；腹腔内 |
アプリケーション | MAZ51はMT450腫瘍の成長を著しく抑制する。 |
References: | |
| 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 |
| 溶解度 | 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 | |||
|
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 |
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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.)