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在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
STF-62247是一个TGN抑制剂,在RCC4 和RCC4/VHL细胞中的IC50分别是0.625 μM和16 μM。STF-62247 may be used as positive control in autophagy inducing cell signaling studies.
Information
STF-62247 is a molecule targeting VHL-deficient renal cell carcinoma that inducesautophagy. STF-62247 shows selective toxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to
In vitro
In vitro, STF-62247 shows cytotoxicity and tumor growth inhibitory activity against wild-type VHL and VHL-deficient renal cell carcinoma (RCC) in a HIF-independent manner with IC50 of 16 μM and 0.625 μM, respectively. Moreover, STF-62247 also leads to cell death by increasing acidification and inducing autophagy in VHL-deficient cells. [1] STF-62247 specifically induces macroautophagy and enhances the fusion of autophagosome and lysosomes to form autolysosomes by interfering with Golgi-endoplasmic reticulum transport in cells that have lost VHL . [2] A recent study shows that induction of autophagy by STF-62247 increases sensitivity of RCC under hypoxic conditions to radiation in a VHL-dependent manner. [3]
In vivo
In vivo mouse model, STF-62247 at a dose of 8 mg/kg by intraperitoneal injection significantly reduces tumor growth of VHL-deficient SN12C tumor cells. [1]
Cell Data
cell lines:
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