货号	规格	价格	上海	北京	珠海	重庆	武汉
S89684-5mg促销	98.80%	￥1500.00 ￥1200.00 S89684-5mg ￥1200.00 现货	5 5	-	-	-	-
S89684-10mg促销	98.80%	￥2500.00 ￥2000.00 S89684-10mg ￥2000.00 现货	6 6	-	-	-	-
S89684-25mg促销	98.80%	￥5000.00 ￥4000.00 S89684-25mg ￥4000.00 现货	5 5	-	-	-	-
S89684-100mg促销	≥98%	￥13700.00 ￥10900.00 S89684-100mg ￥10900.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

PARP-7:3 nM (IC50); PARP-7:1 nM (Kd);PARP

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. Cell Proliferation Assay Cell Line: NCI-H1373 lung cancer cells Concentration: 0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM Incubation Time: 24 hours Result: Blocked cell proliferation. Western Blot Analysis Cell Line: NCI-H1373 lung cancer cells Concentration: 0.4 nM-1 μM Incubation Time: 24 hours Result: Increased p-STAT1 protein expression.

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 with NCI-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.

参考文献：

1. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency 2. Melissa Vasbinder, et al. RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.91 ml	9.552 ml	19.105 ml
5 mM	0.382 ml	1.91 ml	3.821 ml
10 mM	0.191 ml	0.955 ml	1.91 ml
50 mM	0.038 ml	0.191 ml	0.382 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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