VEGFR-3-IN-1 是一种有效的高选择性VEGFR3抑制剂，其IC50为 110.4 nM。VEGFR-3-IN-1 通过使 VEGFR3 信号通路失活，显著抑制 VEGF-C 诱导人真皮淋巴管内皮细胞 (HDLEC)、MDA-MB-231 和 MDA-MB-436 细胞的增殖和迁移，并且能有效抑制乳腺癌的生长。
| 生物活性 | VEGFR-3-IN-1 is a potent and selectiveVEGFR3inhibitor with anIC50of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breastcancergrowth[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | VEGFR-3-IN-1 (compound 38k) exhibits a significantly higher antiproliferative activity on MDA-MB-231 and MDA-MB-436 cells than 10 (IC50>50 μM), with IC50values of 2.22 and 3.50 μM, respectively[1].
VEGFR-3-IN-1 markedly suppresses the phosphorylation of VEGFR3 and its downstream proteins in a dose-dependent manner[1].
Cell Viability Assay[1] | Cell Line: | MDA-MB-231 and MDA-MB-436 cells | | Concentration: | 100 nM | | Incubation Time: | 48 hours | | Result: | Exerted antimigration and antiproliferative activities through targeting VEGFR3 in MDA-MB-231 and MDA-MB-436 cells. |
Western Blot Analysis[1] | Cell Line: | HDLEC cells | | Concentration: | 10-500 nM | | Incubation Time: | | | Result: | Antilymphangiogenic activities of VEGFR-3-IN-1 by suppressing the expression of VEGFR3. |
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体内研究
(In Vivo) | VEGFR-3-IN-1 (50, 25 mg/kg; p.o.) reduces the tumor volume, and displays the strongest inhibitory activity in mice, with a growth inhibition rate of 61.9%[1].
VEGFR-3-IN-1 (10 mg/kg; p.o.) treatment shows the Cmax, AUC0-t, AUC0-∞and t1/2values of 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively[1].
| Animal Model: | Nude mice (carrying xenografted BC)[1] | | Dosage: | 50 mg/kg | | Administration: | P.o.;once | | Result: | Reduced the tumor volume, and displayed the strongest inhibitory activity in mice. |
| Animal Model: | Sprague-Dawley (SD) rats[1] | | Dosage: | 10 mg/kg | | Administration: | P.o. (Pharmacokinetic Analysis) | | Result: | The Cmax, AUC0-t, AUC0-∞and t1/2were 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively. |
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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 : 12.5 mg/mL(20.29 mM;ultrasonic and warming and adjust pH to 6 with HCl and heat to 60℃) 配制储备液 | 1 mM | 1.6231 mL | 8.1156 mL | 16.2311 mL | | 5 mM | 0.3246 mL | 1.6231 mL | 3.2462 mL | | 10 mM | 0.1623 mL | 0.8116 mL | 1.6231 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。 |
