| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S409061-1ml |
1ml |
现货  |
|
| 别名 | 司马沙尼 (SU5416) |
|---|---|
| 英文别名 | 2H-Indol-2-one, 3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylene]-1,3-dihydro-, (3Z)- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Semaxanib (SU5416) |
| 生化机理 | Semaxanib（SU5416）是一种强效的选择性 VEGFR（Flk-1/KDR）抑制剂，IC50 为 1.23 μM，对 VEGFR 的选择性是 PDGFRβ 的 20 倍，对 EGFR、InsR 和 FGFR 缺乏活性。第 3 阶段。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 血管内皮生长因子受体抑制剂 |
| 产品介绍 |
Information Semaxanib (SU5416) is a potent and selectiveVEGFR(Flk-1/KDR) inhibitor withIC50of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3. Semaxanib inhibits VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with IC50 of 1.04 μM. Semaxanib inhibits PDGF-dependent autophosphorylation in NIH 3T3 cells with IC50 of 20.3 μM. Semaxanib inhibits VEGF- and FGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 and 50 μM, respectively. Semaxanib treatment has no effect on the in vitro growth of C6 glioma, Calu 6 lung carcinoma, A375 melanoma, A431 epidermoid carcinoma, and SF767T glioma cells (all IC50s > 20 μM). In vivo Semaxanib dose-related inhibits growth of A375 tumor in vivo. A >85% inhibition of subcutaneous tumor growth is observed with daily i.p. administration of SU5416 in DMSO at Semaxanib, without measurable toxicity. Semaxanib shows broad spectrum antitumor activity. SU5416 significantly inhibits the subcutaneous growth of 8 of 10 tumor lines tested (A431, Calu-6, C6, LNCAP, EPH4-VEGF, 3T3HER2, 488G2M2 and SF763T cells) with an average mortality rate of 2.5%. Semaxanib (25 mg/kg/day) displays potent antiangiogenic activity, resulting in a significant reduction of both the total and functional vascular density of the tumor microvasculature. cell lines： Concentrations：~100 μM Incubation Time：2 days Powder Purity:≥99% |
| IC50 | VEGFR2/Flk1, IC50: 1.23 μM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC1=CC(=C([NH]1)/C=C/2C(=O)NC3=CC=CC=C23)C |
| 分子量 | 238.28 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 65 mg/mL (198.57 mM); Ethanol: 65 mg/mL (198.57 mM); Water: Insoluble; |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Orange Liquid) | Pass |
| Record the entire process by video | Conform |
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