SU16f 是有效的，选择性PDGFRβ抑制剂，对 PDGFRβ，PDGFR1，PDGFR2 的IC50分别为 10 nM，140 nM，2.29 μM。SU16f 抑制 PDGFRβ 受体从而可以阻断胃癌来源的间充质干细胞 (GC-MSC) 条件培养基在胃癌细胞增殖和迁移中的促进作用。
| 生物活性 | SU16f is a potent and selectivePDGFRβinhibitor withIC50s of 10 nM, 140 nM, 2.29 μM forPDGFRβ, PDGFR1, PDGFR2, respectively[1]. Neutralization ofPDGFRβreceptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastriccancercell proliferation and migration[2]. |
| IC50& Target[1] | PDGFRβ 10 nM (IC50) | PDGFR2 140 nM (IC50) | PDGFR1 2.29 μM (IC50) |
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体外研究
(In Vitro) | SU16f (20 μM; for 8 hours) pretreatment inhibits the promoting role of GC-MSC-CM in SGC-7901 cell proliferation[1].
SU16f (20 μM; for 8 hours) significantly abolishes PDGFRβ activation in SGC-7901 by GC-MSC-CM. SU16f pretreatment results in the upregulation of E-cadherin and downregulation of N-cadherin, Vimentin, and α-SMA. SU16f pretreatment leads to downregulation of p-AKT, Bcl-xl, and Bcl-2 levels and upregulation of Bax expression in SGC-7901 cells by GC-MSC-CM[1].
Cell Proliferation Assay[1] | Cell Line: | SGC-7901 cells in GC-MSC/SGC-7901 co-culture system | | Concentration: | 20 μM | | Incubation Time: | 8 hours | | Result: | Inhibited the promoting role of GC-MSC-CM in SGC-7901 cell proliferation. |
Western Blot Analysis[1] | Cell Line: | SGC-7901 cells | | Concentration: | 20 μM | | Incubation Time: | 8 hours | | Result: | Significantly abolished PDGFRβ activation in SGC-7901 by GC-MSC-CM, and resulted in the upregulation of E-cadherin and downregulation of N-cadherin, Vimentin, and α-SMA. |
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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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(129.39 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5877 mL | 12.9386 mL | 25.8772 mL | | 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | | 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 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。 |
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