货号	规格	价格	上海	北京	珠海	重庆	武汉
S80118-1mg买3赠1	99.62%	￥200.00 ￥180.00 S80118-1mg ￥180.00 现货（买3赠1）	3 3	-	-	-	-
S80118-2mg买3赠1	99.62%	￥320.00 ￥280.00 S80118-2mg ￥280.00 现货（买3赠1）	9 9	-	-	-	-
S80118-5mg买3赠1	99.62%	￥400.00 ￥360.00 S80118-5mg ￥360.00 现货（买3赠1）	2 2	-	-	-	-
S80118-10mg买3赠1	99.62%	￥720.00 ￥640.00 S80118-10mg ￥640.00 现货（买3赠1）	4 4	-	-	-	-
S80118-25mg买3赠1	99.62%	￥1520.00 ￥1360.00 S80118-25mg ￥1360.00 现货（买3赠1）	5 5	-	-	-	-
S80118-50mg买3赠1	99.62%	￥2800.00 ￥2520.00 S80118-50mg ￥2520.00 现货（买3赠1）	2 2	-	-	-	-
S80118-100mg促销	≥98%	￥5120.00 ￥4600.00 S80118-100mg ￥4600.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively

靶点：

IC50: 54 nM (rRNA synthesis, MIA PaCa-2 cells), 113 nM (rRNA synthesis, A375 cells), 142 nM (rRNA synthesis, HCT-116 cells);DNA/RNASynthesis

体内研究：

CX-5461 displays antitumor activity against human solid tumors in murine xenograft models. CX-5461 (50 mg/kg, p.o.) shows significant MIA PaCa-2 growth inhibition with TGI equal to 69% on day 31 and 79% TGI on A375 on day 32. CX-5461 (50 mg/kg, p.o.) inhibits the Eμ-Myc tumor cells with 84% repression in Pol I transcription at 1 hr posttreatment in C57BL/6 mice. CX-5461 also induces a rapid reduction in tumor burden in the lymph nodes and a concomitant reduction of spleen size to within the normal range

参考文献：

1. Drygin D et al. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer Res. 2011 Feb 15;71(4):1418-30. 2. Bywater MJ, et al. Inhibition of RNA Polymerase I as a Therapeutic Strategy to Promote Cancer-Specific Activation of p53. Cancer Cell. 2012 Jul 10;22(1):51-65.

溶解性：

50 mM sodium phosphate (pH 3.5) : 10 mg/mL (19.47 mM; Need ultrasonic) DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.947 ml	9.735 ml	19.47 ml
5 mM	0.389 ml	1.947 ml	3.894 ml
10 mM	0.195 ml	0.974 ml	1.947 ml
50 mM	0.039 ml	0.195 ml	0.389 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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