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STF-31

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Chemical Structure| 724741-75-7 同义名 : -
CAS号 : 724741-75-7
货号 : A761947
分子式 : C23H25N3O3S
纯度 : 99%+
分子量 : 423.528
MDL号 : MFCD04153828
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(82.64 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
靶点
  • GLUT1

描述 STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM. STF-31completely suppressed the glucose uptake activity and induced apoptosis in GLUT1 expressing myeloma cells. Moreover, STF-31 synergistically enhanced the cell death induced by melphalan, doxorubicin, and bortezomib[3]. STF-31 (0.01-10 μM; 10 days) is specifically toxic to RCC4 cells, whereas RCC4/VHL cells are relatively unaffected. RCC4/VHL cells treated with STF-31 (5 μM; 10 days) largely recovery, whereas RCC4 cells under the same conditions does not. STF-31 (1.25-5 μM; 3 days) does not induce autophagy, apoptosis, or DNA damage. STF-31 causes a necrotic cell death. Soluble analog of STF-31 (11.6 mg/kg; i.p.) treatment delays tumor growth in mice with VHL-deficient RCC tumor xenografts[4]. STF-31 (10 mg/kg; i.p.; twice daily for 2 days, followed by once daily for another 3 days) does not affect normal mice body weight, behavior, and ERG responses. STF-31 reduces light-induced CX3CR1gfp/+ mice microglial activation and retinal degeneration[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780 cells Function assay 48 h Inhibition of NAMPT in human A2780 cells assessed as reduction in NAD level after 48 hrs by LC-MS/MS analysis, IC50=0.024 μM 24433859
HCT116 cells Proliferation assay 96 h Antiproliferative activity against human HCT116 cells after 96 hrs by CyQuant-based assay, IC50=0.271 μM 24433859
HT1080 cells Proliferation assay 96 h Antiproliferative activity against human HT1080 cells after 96 hrs by CyQuant-based assay, IC50=0.213 μM 24433859
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.81mL

2.36mL

1.18mL

23.61mL

4.72mL

2.36mL

参考文献

[1]Liu Y, Cao Y, et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Mol Cancer Ther. 2012 Aug;11(8):1672-82.

[2]Chan DA, Sutphin PD, et al. Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality. Sci Transl Med. 2011 Aug 3;3(94):94ra70.

[3]Matsumoto T, Jimi S, Migita K, Takamatsu Y, Hara S. Inhibition of glucose transporter 1 induces apoptosis and sensitizes multiple myeloma cells to conventional chemotherapeutic agents. Leuk Res. 2016 Feb;41:103-10

[4]Chan DA, Sutphin PD, Nguyen P, Turcotte S, Lai EW, Banh A, Reynolds GE, Chi JT, Wu J, Solow-Cordero DE, Bonnet M, Flanagan JU, Bouley DM, Graves EE, Denny WA, Hay MP, Giaccia AJ. Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality. Sci Transl Med. 2011 Aug 3;3(94):94ra70

[5]Wang L, Pavlou S, Du X, Bhuckory M, Xu H, Chen M. Glucose transporter 1 critically controls microglial activation through facilitating glycolysis. Mol Neurodegener. 2019 Jan 11;14(1):2