CX-5461,RNAPolymeraseIinhibitor M66052-2s|产品详情|进口橙子视频旧款采购网

您好，欢迎来到橙子视频app安卓下载生物网站！请登录注册

我的订单 | 联系橙子视频app安卓下载 | 在线客服QQ：3012681483 | 客服电话：400-968-7988 | 工作时间：08:30-17:30

主营产品： ELISA91橙子视频、抗体、补体血清、兔补体、干扰素、小鼠测温仪、进口橙子视频旧款、Quidel代理、Swant代理、PBL Assay Science代理

网站首页产品中心代理品牌新闻资讯资源中心关于橙子视频app安卓下载

所在位置：首页 > 产品中心 > Xcessbio > Xcessbio产品

订购信息

上海橙子视频app安卓下载生物科技公司

Tel:400-968-7988 021-33779008

CX-5461,RNAPolymeraseIinhibitor

品牌：Xcessbio

货号：M66052-2s

规格：2 mg solid

货期：

应用：

咨询客服

立即购买加入购物车

CX-5461,RNAPolymeraseIinhibitor

商品详情参考文献相关资料

Product Information

Molecular Weight:	513.61
Formula:	C₂₇H₂₇N₇O₂S
Purity:	≥98%
CAS#:	1138549-36-6
Solubility:	DMSO up to 2 mM
Chemical Name:	2-(4-methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
Storage:	Powder: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 1 year.

Details

Biological Activity:

CX-5461 is the first potent, selective, and orally bioavailable inhibitor of RNA Polymerase I with an IC₅₀ ~0.11 µM. It showed good in vivo activities in tumor models. It selectively blocks RNA PolI transcription, PIC assembly and SL1-rDNA interaction. CX-5461 showed potent anti-proliferation activity in cancer cells and antitumor activity in A375 and MiaPaca xenografts. In a recent Cancer Cell paper, CX5461 was shown to induce p53-dependent apoptotic cell death of Em-Myc lymphoma cells via activation of the Rp-MDM2-p53 nucleolar surveillance pathway; selectively induced p53-mediated cell death of lymphoma cells in vivo while sparing normal B cells.

How to Use:

In vitro: CX-5461 was used at 100-500 nM in vitro and in cell culture.
In vivo: In pancreatic carcinoma (MIA PaCa-2) and melanoma (A375) xenograft model, CX-5461 was administered orally at 50 mg/kg either once daily or every 3 days. In MV4;11 xenograft model, CX-5461 was administered intraperitoneally once a week at 125 mg/kg for the length of 25 days, or IP dosed at 25 mg/kg once a day on a 5-on, 2-off schedule over a period of 21 days.

Reference:

1. Drygin D, et al. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. (2011) Cancer Res. 71(4):1418-30.
2. Haddach M, et al. Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics. (2012) ACS Med. Chem. Lett., 3 (7), pp 602–606.
3. Bywater MJ, et al Inhibition of RNA Polymerase I as a Therapeutic Strategy to Promote Cancer-Specific Activation of p53. (2012) Cancer Cell, 22(1), 51 – 65.