SU5416
中文名称 | SU5416 |
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中文同义词 | (Z)-3-((3,5-二甲基-1H-吡咯-2-基)亚甲基)吲哚啉-2-酮;1,3-二氢-3-[(3,5-二甲基-1H-吡咯-2-基)亚甲基]-2H-吲哚-2-酮;司马沙尼;3-二氢-3-[(3;5-二甲基-1H-吡咯-2-基)亚甲基)吲哚啉-2-酮;5-二甲基-1H-吡咯-2-基)亚甲基]-2H-吲哚-2-酮;SU 5416, 一种VEGFR2/FLK1抑制剂;3-二氢-3-[(3,5-二甲基-1H-吡咯-2-基)亚甲基]-2H-吲哚-2-酮 |
英文名称 | SU 5416 |
英文同义词 | H-Indol-2-one, 3-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-1,3-dihydro-;SeMaxinib;SU 5416 (SeMaxinib);SU5416 /SU-5416;(Z)-3-((3,5-diMethyl-1H-pyrrol-2-yl)Methylene)indolin-2-one;3-((3,5-diMethyl-1H-pyrrol-2-yl)Methylene)indolin-2-one;3-[(3,5-diMethyl-1H-pyrrol-2-yl)Methylidene]-1H-indol-2-one;SEMAXINIB(SU 5416) |
CAS号 | 204005-46-9 |
分子式 | C15H14N2O |
分子量 | 238.28 |
EINECS号 | 200-256-5 |
相关类别 | 小分子抑制剂,天然产物;小分子抑制剂;细胞凋亡;Angiogenesis and Metastasis;Inhibitors |
Mol文件 | 204005-46-9.mol |
结构式 |
SU5416 性质
熔点 | 226-228 °C |
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沸点 | 481.4±45.0 °C(Predicted) |
密度 | 1.256±0.06 g/cm3(Predicted) |
储存条件 | -20°C |
溶解度 | 不溶于水 |
酸度系数(pKa) | 12.59±0.20(Predicted) |
形态 | 黄橙色固体 |
颜色 | 黄色至黄橙色 |
Flk-1 1.23 μM (IC 50 ) |
Semaxinib (SU5416) inhibits VEGF-driven mitogenesis in a dose-dependent manner with an IC 50 of 0.04±0.02 μM (n=3). In contrast, Semaxinib (SU5416) blocks FGF-dependent mitogenesis of HUVECs with an IC 50 of 50 μM (n=10). An IC 50 of 20.26±5.2 μM, which is about 20-fold less in potency on PDGF-dependent autophosphorylation, is observed when SU5416 is tested in NIH 3T3 cells overexpressing the human PDGF receptor β.
Daily administration of Semaxinib (SU5416) (i.p., 3 mg/kg/day) inhibits the local growth of C6 tumors in the colon. A comparable level of growth inhibition (62% by day 16; P=0.001) is observed for tumors growing in the colon in comparison with ones growing in the hindflank region (54% by day 18; P=0.001). These results indicate that Semaxinib (SU5416) could inhibit tumor growth at a site other than the subcutaneous implantation site, where the preexisting vasculature may be different. Daily treatment with Semaxinib (SU5416) (25 mg/kg) results in a significantly lower tumor growth rate with tumor masses of up to 8% of that present in control animals by day 22 after implantation. Inhibition of tumor growth is clearly preceded by a marked reduction of the tissue area covered by the newly formed glioma microvasculature in the Semaxinib-treated group, indicating a reduced initial tumor vascularization.
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-10374 | Semaxinib | 5 mg | 612元 | |
2024/01/25 | HY-10374 | SU5416 Semaxinib | 204005-46-9 | 10mg | 980元 |