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MAZ51
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MAZ51图片
CAS NO:163655-37-6
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
MAZ51 是 VEGFR-3 (Flt-4) 酪氨酸激酶的选择性抑制剂。 MAZ51 抑制 VEGF-C 诱导的 VEGFR-3 活化，而不阻断 VEGF-C 介导的 VEGFR2 刺激。 MAZ51 对配体诱导的 EGFR、IGF-1R 和 PDGFRβ 的自磷酸化没有影响。 MAZ51 在多种肿瘤细胞中阻断增殖并诱导细胞凋亡。抗肿瘤活性。
Cas No.163655-37-6
化学名3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-2H-indol-2-one
Canonical SMILESCN(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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.