MAZ51
目录号 : GC16483
MAZ51是一种选择性血管内皮生长因子受体3（VEGFR-3；FLT4）酪氨酸激酶抑制剂。
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).
MAZ51是一种选择性血管内皮生长因子受体3（VEGFR-3；FLT4）酪氨酸激酶抑制剂[1]。MAZ51是一种基于吲哚酮的分子，能够抑制人类内皮细胞和肿瘤细胞的增殖，并诱导细胞凋亡[2]。MAZ51会加重顺铂肾毒性[3]。
在体外，MAZ51（3μM）预处理人前列腺癌PC-3细胞4h，抑制了血管内皮生长因子C（VEGF-C）诱导的血管内皮生长因子受体3（VEGFR-3）磷酸化，阻断了丝氨酸/苏氨酸激酶（Akt）磷酸化[4]。MAZ51（2.5-5μM）两种胶质瘤细胞系（大鼠C6和人U251MG细胞）24h，诱导了胶质瘤细胞系的形态变化，诱导了G2/M期细胞周期停滞[5]。
在体内，MAZ51（8mg/kg）通过腹腔注射治疗乳腺肿瘤MT450细胞异种移植大鼠，显著抑制了肿瘤的生长，减少了增殖细胞核抗原（PCNA）阳性细胞的数量[6]。MAZ51（10mg/kg）通过皮下注射治疗全层皮肤损伤小鼠，可能影响了淋巴管生成，但不会影响血管生成[7]。
| Cell experiment [1]: | |
Cell lines | PC-3 cells |
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. |
Reaction Conditions | 3μM; 4h |
Applications | The VEGF-C-induced phosphorylation of VEGFR-3 was completely blocked by the pretreatment with 3μM MAZ51 for 4h. |
| Animal experiment [2]: | |
Animal models | Wistar Furth rats |
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. |
Dosage form | 8mg/kg; i.p. |
Applications | MAZ51 significantly suppresses the growth of MT450 tumors. |
References: | |
| Cas No. | 163655-37-6 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C21H18N2O | 分子量 | 314.4 |
| 溶解度 | ≥ 31.4mg/mL in DMSO with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1807 mL | 15.9033 mL | 31.8066 mL |
| 5 mM | 0.6361 mL | 3.1807 mL | 6.3613 mL |
| 10 mM | 0.3181 mL | 1.5903 mL | 3.1807 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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