MAZ51

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MAZ51  纯度: 98.21%

MAZ51 是 VEGFR-3 酪氨酸激酶的选择性抑制剂。MAZ51 抑制 VEGF-C 诱导的 VEGFR-3 激活，而没有阻断 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 阻止增殖并诱导多种肿瘤细胞凋亡。具有抗肿瘤活性。

MAZ51

MAZ51 Chemical Structure

CAS No. : 163655-37-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
10 mg ￥1550 In-stock
25 mg ￥3100 In-stock
50 mg ￥5200 In-stock
100 mg ￥8800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity[1][2].

IC50 & Target[1]

VEGFR3

 

体外研究
(In Vitro)

MAZ51 (2.5-10 μM; 24 hours) blocks proliferation and induces apoptosis in a wide variety of tumor cells[2].
MAZ51 (0.5-50 μM; 25 minutes) has no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ in A431 cells, HEK-293 cells, and PAE cells, respectively[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells
Concentration: 2.5, 10 μM
Incubation Time: 24 hours
Result: Induced apoptosis in a wide variety of tumor cells.

Apoptosis Analysis[2]

Cell Line: MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells
Concentration: 2.5, 10 μM
Incubation Time: 24 hours
Result: Blocked proliferation in a wide variety of tumor cells.

体内研究
(In Vivo)

MAZ51 (8 mg/kg; i.p.; daily for 15 day) significantly suppresses the growth of MT450 tumors[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar Furth rats (bearing MT450 cells)[1]
Dosage: 8 mg/kg
Administration: Intraperitoneal injection; daily for 15 day
Result: Significantly suppressed the growth of MT450 tumors.

分子量

314.38

Formula

C21H18N2O
CAS 号

163655-37-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (26.50 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1809 mL 15.9043 mL 31.8086 mL
5 mM 0.6362 mL 3.1809 mL 6.3617 mL
10 mM 0.3181 mL 1.5904 mL 3.1809 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.83 mg/mL (2.64 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.64 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kirkin V, et al. Characterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2. Eur J Biochem. 2001 Nov;268(21):5530-40.

    [2]. Kirkin V, et al. MAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo. Int J Cancer. 2004 Dec 20;112(6):986-93.

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