1、STF-62247Cat. No.: HY-100746CAS No.: 315702-99-9Molecular Formula: CHNSMolecular Weight: 267.35Target: AutophagyPathway: AutophagyStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent & SolubilityIn Vitro DMSO : 31 mg/mL (115.95 mM)* “ means soluble, but saturation unknow
2、n.ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 3.7404 mL 18.7021 mL 37.4041 mL5 mM 0.7481 mL 3.7404 mL 7.4808 mLPreparing Stock Solutions10 mM 0.3740 mL 1.8702 mL 3.7404 mLPlease refer to the solubility information to select the appropriate solvent.BIOLOGICAL ACTIVITYDescription STF-62247 is TGN in
3、hibitor with IC50 of 0.625M and 16M in RCC4 and RCC4/VHL cells,respectively.It specifically induces autophagic cell death in cells that have lost VHL, an essential mutation in the development of RCC.IC50: 0.625/16M in RCC4 and RCC4/VHL cells,respectively.1In vitro: STF-62247 induces cytotoxicity in
4、VHL-deficient cells in a HIF-independent manner, STF-62247 increases acidification in VHL-deficient cells ,TGN is a target of STF-62247 and a drug-selective pathway synthetically lethal in VHL-deficient cells.1 Golgi trafficking are required as initial signals in STF-62247-induced autophagy.2STF-622
5、47 increases radiosensitivity in a VHL-dependent manner.3In vivo: SN12C, SN12C-VHL shRNA, or 786-O cells were implanted subcutaneously into the flanks of immunodeficient mice. The selective cytotoxicity of STF-62247 for the VHL-deficient cells was also demonstrated in 786-O cells compared to their w
6、ild-type VHL counterparts by clonogenic assay in vitro. Daily treatment with STF-62247 significantly reduced tumor growth of VHL-deficient cells. This decrease in tumor growth was concentration dependent. Importantly, drug treatment did not have any effect on the growth of SN12C tumor cells that hav
7、e wild-type VHL. Together,STF-62247 reduces tumor growth in VHL-deficient cells in mice.1Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1REFERENCES1. Turcotte, S. et al. A molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. Cancer cell 14, 90-102, doi:1
8、0.1016/j.ccr.2008.06.004 (2008)2. Chan, D. A. & Giaccia, A. J. Targeting cancer cells by synthetic lethality: autophagy and VHL in cancer therapeutics. Cell cycle 7, 2987-2990, doi:10.4161/cc.7.19.6776 (2008)3. Anbalagan, S. et al. Radiosensitization of renal cell carcinoma in vitro through the indu
9、ction of autophagy. Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology 103, 388-393, doi:10.1016/j.radonc.2012.04.001 (2012Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAwww.MedChemE2
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