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。
| 生物活性 | MAZ51 is a selective inhibitor ofVEGFR-3(Flt-4)tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation ofVEGFR-3without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation ofEGFR,IGF-1RandPDGFRβ. MAZ51 blocks proliferation and inducesapoptosisin a wide variety of tumor cells. Antitumor activity[1][2]. |
| IC50& Target[1] | |
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].
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. |
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体内研究
(In Vivo) | MAZ51 (8 mg/kg; i.p.; daily for 15 day) significantly suppresses the growth of MT450 tumors[2].
| 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. |
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| 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 |
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| 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℃) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
