| 產(chǎn)品描述： | STF-62247 is TGN inhibitor with IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively. |
| 靶點： |
Autophagy;Estrogen/progestogen Receptor;Estrogen/progestogenReceptor;Autophagy |
| 體外研究： |
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. |
| 體內(nèi)研究： |
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. |
| 細(xì)胞實驗： |
For cell viability, 100,000 cells are plated in a 12-well plate. The following day, 1.25 μM STF-62247 is added in the presence or absence of 1 mM 3-MA for 24 hours at 37 °C. Cells are trypsinized and counted by trypan blue exclusion. For XTT assays, 5000 RCC4 with and without VHL cells or 2,500 SN12C with and without VHL shRNA cells are plated in 96-well plates. The following day, vehicle (DMSO), STF-62247 is added to media by serial dilution. Four days later, the media is aspirated and XTT solution containing 0.3 mg/ml of XTT in Phenol Red-free media, 20% FCS and 2.65 mg/ml N-methyl dibenzopyrazine methyl sulfate (PMS) is added to the cells and incubated at 37 °C for 1-2 hours. Metabolism of XTT is quantified by measuring the absorbance at 450 nm on a plate reader. (Only for Reference) |
| 動物實驗： |
動物模型：SN12C, SN12C-VHL shRNA or 786-O cells are injected subcutaneously into the flanks of immune-deficient mice. |
| 參考文獻(xiàn)： |
1. Turcotte S, et al. A molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. Cancer Cell. 2008, 14(1), 90-102. 2. Chan DA, et al. A molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. Cell Cycle. 2008, 7(19), 21987-21990. 3. Anbalagan S, et al. Radiosensitization of renal cell carcinoma in vitro through the induction of autophagy. Radiother Oncol. 2012, 103(3), 388-393. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.74 ml |
18.702 ml |
37.404 ml |
| 5 mM |
0.748 ml |
3.74 ml |
7.481 ml |
| 10 mM |
0.374 ml |
1.87 ml |
3.74 ml |
| 50 mM |
0.075 ml |
0.374 ml |
0.748 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京