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STF-62247

产品编号 T6683 CAS 315702-99-9

别名: STF 62247

STF-62247 是一种自噬诱导剂，在 RCC4 和 RCC4/VHL 细胞中的IC50分别为 0.625 μM 和 16 μM。它对 VHL 缺陷型肾细胞癌有选择性的细胞毒性。

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STF-62247, CAS 315702-99-9

规格	价格/CNY	货期
5 mg	￥ 272	现货
10 mg	￥ 413	现货
25 mg	￥ 913	现货
50 mg	￥ 1,570	现货
100 mg	￥ 2,350	现货
200 mg	￥ 3,490	现货
500 mg	￥ 5,570	现货
1 mL * 10 mM (in DMSO)	￥ 293	现货

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纯度: 99.3%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	STF-62247 is TGN inhibitor with IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively.
靶点活性	TGN (RCC4/VHL):16 μM, TGN (RCC4):0.625 μM
体外活性	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]
体内活性	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]
激酶实验	SIRT1 fluorescence polarization assay and HTS: In the SIRT1 FP assay, SIRT1 activity is monitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH2 ) derived from the sequence of p53. The peptide is N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity is a coupled enzyme assay where the first reaction is the deacetylation reaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at the newly exposed lysine residue. The reaction is stopped and streptavidin is added in order to accentuate the mass differences between substrate and product. The fluorescence polarization reaction conditions are as follows: 0.5 μM peptide substrate, 150 μM βNAD +, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl 2 , 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37°C and stopped by addition of nicotinamide, and trypsin is added to cleave the deacetylated substrate. This reaction is incubated at 37 ℃ in the presence of 1 μM streptavidin. Fluorescent polarization is determined at excitation (650 nm) and emission (680 nm) wavelengths.
细胞实验	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)

别名	STF 62247
分子量	267.35
分子式	C15H13N3S
CAS No.	315702-99-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 49 mg/mL (183.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 3 mg/mL (11.22 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	3.7404 mL	18.7021 mL	37.4042 mL	93.5104 mL
	5 mM	0.7481 mL	3.7404 mL	7.4808 mL	18.7021 mL
	10 mM	0.374 mL	1.8702 mL	3.7404 mL	9.351 mL
DMSO	20 mM	0.187 mL	0.9351 mL	1.8702 mL	4.6755 mL
	50 mM	0.0748 mL	0.374 mL	0.7481 mL	1.8702 mL
	100 mM	0.0374 mL	0.187 mL	0.374 mL	0.9351 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Turcotte S, et al. Cancer Cell. 2008, 14(1), 90-102. 2. Chan DA, et al. Cell Cycle. 2008, 7(19), 21987-21990. 3. Anbalagan S, et al. Radiother Oncol. 2012, 103(3), 388-393.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

STF-62247 315702-99-9 Autophagy Endocrinology/Hormones Estrogen/progestogen Receptor renal VHL carcinoma inhibit cytotoxic cell RCC Inhibitor STF62247 STF 62247 intracytoplasmic vacuoles inhibitor

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STF-62247

存储

溶解度

溶液配制表

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参考文献

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剂量换算

体内实验配液计算器

技术支持

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