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编 号：F270486
分子式：C19H25Cl2N7
分子量：422.35
分子式：C19H25Cl2N7
分子量：422.35
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CAS No: 21062-28-2
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生物活性：
SKOG102 is a potent OLIG2 inhibitor that is directly engaging OLIG2 and interferes with the ability of OLIG2 to bind DNA. SKOG102 can be used for the research of glioblastoma (GBM).
体内研究：
SKOG102 (10-20 mg/kg; i.p.) 抑制小鼠 GBM4 肿瘤的生长。SKOG102 (5 mg/kg; i.p.) 即使在相对较短的时间内也会在肿瘤中积聚，注射小鼠后 4 小时血浆和脑浓度几乎相同。Animal Model:NSG mice were inoculated in each flank with GBM4 cells
Dosage:10, 15, and 20 mg/kg; dissolved in solutol:PEG400:water (20%:40%:40%)
Administration:Intraperitoneal injection; first 2 weeks (from day 33 to 46) 10 mg/kg, third week (from day 47 to 54) 15 mg/kg, fourth week (from 55 to 66) first 3 days 20 mg/kg, 2 days break, then alternate days from day 60 to 66
Result:Significantly attenuated tumor growth.
体外研究：
SKOG102 (0.1-5 μM; 72 h) 抑制人 GBM4 和 GBM8 细胞生长为神经球，IC50 分别为 10.66 和 1.536 μM。SKOG102 (0.5-5 μM; 12 h) 增加 GBM4 细胞中的 p21 RNA 水平并降低 OMG RNA 水平。SKOG102 (5 μM; 20 h) 抑制 OLIG2-DNA 结合，并降低 GBM8 细胞中的丝氨酸磷酸化 OLIG2 和总 OLIG2 蛋白水平。
SKOG102 is a potent OLIG2 inhibitor that is directly engaging OLIG2 and interferes with the ability of OLIG2 to bind DNA. SKOG102 can be used for the research of glioblastoma (GBM).
体内研究：
SKOG102 (10-20 mg/kg; i.p.) 抑制小鼠 GBM4 肿瘤的生长。SKOG102 (5 mg/kg; i.p.) 即使在相对较短的时间内也会在肿瘤中积聚，注射小鼠后 4 小时血浆和脑浓度几乎相同。Animal Model:NSG mice were inoculated in each flank with GBM4 cells
Dosage:10, 15, and 20 mg/kg; dissolved in solutol:PEG400:water (20%:40%:40%)
Administration:Intraperitoneal injection; first 2 weeks (from day 33 to 46) 10 mg/kg, third week (from day 47 to 54) 15 mg/kg, fourth week (from 55 to 66) first 3 days 20 mg/kg, 2 days break, then alternate days from day 60 to 66
Result:Significantly attenuated tumor growth.
体外研究：
SKOG102 (0.1-5 μM; 72 h) 抑制人 GBM4 和 GBM8 细胞生长为神经球，IC50 分别为 10.66 和 1.536 μM。SKOG102 (0.5-5 μM; 12 h) 增加 GBM4 细胞中的 p21 RNA 水平并降低 OMG RNA 水平。SKOG102 (5 μM; 20 h) 抑制 OLIG2-DNA 结合，并降低 GBM8 细胞中的丝氨酸磷酸化 OLIG2 和总 OLIG2 蛋白水平。
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