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编 号:F751514
分子式:C26H20ClFN2O2
分子量:446.9
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models.

体内研究:
cRIPGBM chloride (50 mg/kg;口服;每天两次,持续 5 周) 在携带患者来源的 GBM CSC 颅内异种移植的小鼠模型再,抑制肿瘤生长。Animal Model:Orthotopic intracranial xenograft model in mouse
Dosage:50 mg/kg
Administration:PO; twice daily, 8 h apart, starting at day 7 postinjection; last for 5 weeks
Result:Monitored by Fluorescence Tomography System. Decreased the tumor signal, as well as tumor size.

体外研究:
cRIPGBM(chloride) (0.25 μM;0-24 小时) 时间依赖性地激活半胱天冬酶 1、半胱天冬酶 9 和半胱天冬酶 7,以及 PARP 裂解。cRIPGBM(chloride) (0.125 μM, 0.25 μM;24 小时) 在 CBM-1 GBM CSCs 中诱导 caspase 1 介导的细胞凋亡。
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