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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKinetin ribosideCat. No.: HY-101055CAS No.: 4338-47-0Synonyms: N6-Furfuryladenosine分式: CHNO分量: 347.33作靶点: Apoptosis作通路: Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 29 mg/mL (83
2、.49 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8791 mL 14.3955 mL 28.7911 mL5 mM 0.5758 mL 2.8791 mL 5.7582 mL10 mM 0.2879 mL 1.4396 mL 2.8791 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可
3、靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.20 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.20 mM); Clear solution1/2 Master of Small Molecules 您边
4、的抑制剂师www.MedChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.20 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Kinetin riboside是细胞分裂素类似物,可诱导癌症细胞死亡。抑制HCT-15细胞增殖的IC50值为2.5 M。IC50 & Target IC50: 2.5 M (HCT-15 cells) 1体外研究 Kinetin riboside displays antiproliferative and apoptogenic activity a
5、gainst various human cancer cell lines.Kinetin riboside is able to inhibit the proliferation in HCT-15 human colon cancer cells in a dose-dependentmanner (IC50=2.5 M) 1. Kinetin riboside induces apoptosis in HeLa and mouse melanoma B16F-10 cells.Kinetin riboside disrupts the mitochondrial membrane p
6、otential and induces the release of cytochrome c andactivation of caspase-3. Bad are up-regulated while Bcl-2 is down-regulated under kinetin riboside exposure2.体内研究 Kinetin riboside significantly suppresses tumor growth. The most effective anti-melanoma response is elicitedat 40 mg/kg 2.PROTOCOLCel
7、l Assay 2 HeLa and mouse melanoma B16F-10 cells are treated with 5, 10, 20 M kinetin riboside for 48 h. 15 L ofMTT solution (5 mg/mL) is added to each well and cells are maintained for 4 h at 37C. Hundred microlitresof solubilizing solution is then added. After an overnight incubation at room temper
8、ature, absorbance at 490nm is measured 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Male C57BL/6 mice are injected B16 F-10 cells. After 5 days for tumor growth, kinetin riboside (10, 20,Administration 2 40 mg/kg) is injected to tumor
9、mass directly. Drug injection is performed once a 3 days for three times. Afterthird injection of drug, mice are kept for 3 days with no injection and tumor mass is removed from eachmouse and weighed 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REF
10、ERENCES1. Rajabi M, et al. Antiproliferative activity of kinetin riboside on HCT-15 colon cancer cell line. Nucleosides Nucleotides Nucleic Acids.2012;31(6):474-81.2. Choi BH, et al. Kinetin riboside preferentially induces apoptosis by modulating Bcl-2 family proteins and caspase-3 in cancer cells.Cancer Lett. 2008 Mar 8;261(1):37-45.McePdfHeightCaution: Product has not been fully va
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