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CX-5461,rRNA合成抑制剂

CX-5461 （订货以英文为准）

编号：C127663
CAS号：1138549-36-6
分子式：C27H27N7O2S
分子量：513.61
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C127663-100mg 阿拉丁 100mg ¥6591.90
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C127663-25mg 阿拉丁 25mg ¥1850.90
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C127663-5mg 阿拉丁 5mg ¥514.90
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产品名称 CX-5461
中文名称 CX-5461,rRNA合成抑制剂
CAS号 1138549-36-6
分子式（M.F.） C27H27N7O2S
分子量（M.W.） 513.61
储存条件 -20°C储存
溶解性DMSO 0.02 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件储存温度-20°C
产品介绍CX-5461是rRNA合成抑制剂，选择性抑制Pol I驱动的rRNA转录，IC50为142nM，对Pol II无效。
备注CX-5461 is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA repli
生化机理CX-5461 is a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. CX-5461 selectively inhibits rRNA synthesis by Pol I in the nucleolus, but does not inhibit mRNA synthesis by RNA Polymerase II (Pol II) and does not inhibit DNA replication or protein synthesis. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. The RP bind to Mdm2 and liberate p53 to orchestrate apoptosis in cancer cells. CX-5461 demonstrates a favorable preclinical profile, potently and selectively kills cancer cells, demonstrates robust in vivo efficacy in multiple models, and has demonstrated oral bioavailability in multiple species. cGMP manufacture has been completed and the molecule is being advanced to the clinic and will be developed for the treatment of leukemias, lymphomas and multiple myeloma. (source: Cylene Pharmaceuticals website)
别名CX 5461;CX5461;2-(4-甲基-1H-1,4-二氮杂环庚烷-1-基)-N-((5-甲基-2-吡嗪基)甲基)-5-氧代-5H-苯并噻唑并(3,2-a)(1,8)萘啶-6-甲酰胺;;CX 5461;CX5461;2-(hexahydro-4-methyl-1h-1,4-diazepin-1-yl)-n-((5-methyl-2-pyrazinyl)methyl)-5-oxo-5h-benzothiazolo(3,2-a)(1,8)naphthyridine-6-carboxamide
WGK德国3
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