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CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。
CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 857 | 35日内发货 | |
5 mg | ¥ 3,860 | 35日内发货 | |
10 mg | ¥ 6,860 | 35日内发货 |
产品描述 | CYY292 is a chemical compound acting as an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, with respective IC50 values of 5.35, 4.6, 28, 28, and 78 nM. It exhibits selectivity over FGFR4 (IC50 > 1,000 nM) while also targeting c-Kit, VEGFR2, VEGFR1, and IGF-1R (IC50 values of 67, 33, 36, and 75 nM, respectively). Additionally, CYY292 inhibits EGFR, BTK, Cdk4/cyclin D3, and MET with IC50 values of 128, 198, 214, and 396 nM, respectively. This compound demonstrates efficacy in arresting the proliferation of various osteosarcoma cell lines—MG-63, U2OS, MNNG/HOS, and Saos-2—with IC50s ranging from 0.72 to 1.36 µM. Moreover, CYY292 at 0.3 and 0.5 µM concentrations inhibits migration and invasion in glioblastoma cells (U87MG and LN-229) and, at a dose of 30 mg/kg, decreases tumor volume and enhances survival in a U87MG orthotopic mouse xenograft model. |
分子量 | 444.53 |
分子式 | C24H28N8O |
CAS No. | 2644673-04-9 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | Methanol: Slightly soluble Ethanol: Slightly soluble |
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