KYA1797K
产品说明书
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同义名 : | - |
| CAS号 : | 1956356-56-1 | |
| 货号 : | A228508 | |
| 分子式 : | C17H11KN2O6S2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 442.51 | |
| MDL号 : | MFCD30718585 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Colorectal cancer (CRC) is one of the most frequent cancers and the second leading cause of cancer-related deaths in Western countries. Both the Wnt/β-catenin and Ras pathways are aberrantly activated in most human colorectal cancers (CRCs) and interact cooperatively in tumor promotion. KYA1797K selectively regulates the Wnt/β-catenin and Ras/ERK pathways. YA1797K inhibited TOPflash activity to a greater extent with an IC50 of 0.75 μM, and effectively reduced the levels of both β-catenin and pan-Ras as well as the activities of ERK (extracellular-signal-regulated kinase) and Akt in SW480 cells. Using multipathway reporter arrays, KYA1797K significantly (P < 0.01) decreased reporter activities for the Wnt/β-catenin and MAPK/ERK pathways. In the CRC lines SW480, LoVo, DLD1 and HCT15, KYA1797K degraded both β-catenin and Ras in a dose-dependent manner. Consistently, cell proliferation was suppressed by KYA1797K treatment. KYA1797K destabilized β-catenin and Ras in DLD1 cells expressing WT β-catenin or WT K-Ras. Those data indicated that KYA1797K inhibited proliferation of CRC cells mainly via destabilization of β-catenin with additional Ras degradation. In vivo, KYA1797K was injected intraperitoneally (i.p.) into mice carrying xenografted tumors from the D-MT cell line that harbors both APC and KRAS mutations. KYA1797K administration (25 mg/kg) reduced both weight and volume of the tumor by 70%. KYA1797K treatment significantly reduced levels of β-catenin and Ras proteins as well as Wnt/β-catenin and Ras signaling target[2]. | ||
| 作用机制 | KYA1797K bound directly to the regulators of G-protein signaling domain of axin[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.30mL 2.26mL 1.13mL |
22.60mL 4.52mL 2.26mL |
| 参考文献 |
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