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STF 31

 
Catalog No.
B7670
GLUT1和NAMPT抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 909.00
现货
50mg
¥ 3,636.00
现货

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A

背景

STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1 μΜ [1].

The inactivated von Hippel-Lindau (VHL) tumor suppressor gene drives renal cell carcinomas (RCCs) development, which imparts the reliance on the GLUT1 and aerobic glycolysis. Compounds of the 3-series, exemplified by STF-31, selectively kills RCCs by specifically targeting glucose uptake through GLU1, on which is the unique dependence of these cells for survival.

STF-31 (0.01-10 μΜ; 10 days) is specifically toxic to RCC4 cells without VHL, while wild-type RCC4 cells (RCC4/VHL) are relatively unaffected. Wild-type RCC4 cells treated with STF-31 (5 μΜ; 10 days) largely recovery, while RCC4 cells dose not on the same condition. No evidence proved the drug-induced cells autophagy, apoptosis, or DNA damages, but wild-type RCC4 cells underwent necrotic cell death in response to STF-31 by the ability of the cells to exclude trypan blue [1].

Soluble analog of STF-31 (11.6 mg/kg; i.p.) treatment delayed tumor growth in mice with VHL-deficient RCC tumor xenografts [1]. STF-31 (10 mg/kg; i.p.; twice daily for 2 days, followed by once daily for another 3 days) did not affect normal mice body weight, behavior and Scotopic electroretinography (ERG) responses. STF-31 reduced light-induced CX3CR1gfp/+ mice microglial activation and retinal degeneration [2].

Reference:

[1] Chan D A, Sutphin P D, Nguyen P, et al. Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality. Sci Transl Med. 2011, 3(94): 94ra70.

[2] Wang L X, Pavlou S, Du X, et al. Glucose transporter 1 critically controls microglial activation through facilitating glycolysis. Mol Neurodegener. 2019, 14(1): 2.

化学属性

Physical AppearanceA solid
StorageStore at RT
M.Wt423.53
Cas No.724741-75-7
FormulaC23H25N3O3S
Solubility≥42.4 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name4-((4-(tert-butyl)phenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide
SDFDownload SDF
Canonical SMILESO=S(NCC1=CC=C(C(NC2=CC=CN=C2)=O)C=C1)(C3=CC=C(C=C3)C(C)(C)C)=O
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