产品
编 号：F565087
分子式：C20H23F6N7O3
分子量：523.43
分子式：C20H23F6N7O3
分子量：523.43
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2381037-82-5
产品详情
生物活性：
RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.
体内研究：
RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice.RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg.The half-life (t1/2) of RBN-2397 in vivo is 325 mins.Animal Model:CB17 SCID mice withNCI-H1373 xenografts
Dosage:3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration:Oral administration; once daily; 24-32 days
Result:Decreased tumor volume and exerted anti-tumor effects.
体外研究：
RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells? proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells.RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells.RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM.
RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.
体内研究：
RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice.RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg.The half-life (t1/2) of RBN-2397 in vivo is 325 mins.Animal Model:CB17 SCID mice withNCI-H1373 xenografts
Dosage:3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration:Oral administration; once daily; 24-32 days
Result:Decreased tumor volume and exerted anti-tumor effects.
体外研究：
RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells? proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells.RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells.RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM.
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