MAZ51
目录号 : GC16483
An antagonist of VEGFR3 (FLT4)
Cas No.:163655-37-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
MAZ51 is originally synthesized as a selective inhibitor for VEGFR-3. VEGFR-3, a receptor tyrosine kinase (RTK), shows restricted expression in the adult organism and is virtually exclusively expressed on the lymphatic endothelium.VEGFR-3 activation is involved in inducing lymphangiogenesis. Inhibition of VEGFR-3 activation can suppress metastasis formation [1].
In vitro: MAZ51 caused dramatic shape changes, including the retraction of cellular protrusions and cell rounding in the rat C6 and human U251MG glioma cell lines. MAZ51 also inhibited cellular proliferation by inducing G2/M phase cell cycle arrest without triggering significant cell death in dose- and time-dependent patterns. Treatment of glioma cells with MAZ51 increased phosphorylated GSK3β levels by activating Akt and increasing levels of active RhoA. Treatment with MAZ51 in VEGFR-3-silenced cells caused the alterations of cell shape and cytoskeletal arrangements [1]. MAZ51 surprisingly blocked proliferation of human dermal microvascular endothelial cells (HDMEC) with an IC50 of < 1 μM [2].
In vivo: In the rats subcutaneously injected with MT450 rat mammary carcinoma cells, treatment daily with MAZ51 (8 mg/kg, i.p.) significantly suppressed the growth of MT450 tumors when compared with the solvent-treated animals [2]. In the mammary fat pad of BALB/c mice injected with the metastatic mammary tumor cell line Cl66, MAZ51 treatment (i.p.) significantly inhibited tumor growth in a dose-dependent manner [3].
References:
[1]. 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.
[2]. 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.
[3]. Michelle L. Varney, Anguraj Sadanandam, Joyce C. Solheim, James E. Talmadge and Rakesh K. Singh Experimental and Molecular Therapeutics 28: Antibodies and Therapeutic Targets VEGFR3 antagonist (MAZ51) directly and indirectly inhibits murine mammary tumor growth and metastasis.
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。