CX-5461 dihydrochloride
A selective RNA polymerase inhibitor
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包装价格促销价数量
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5mg￥1300.001040.00- +
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50mg￥5950.004760.00- +
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100mg￥0.000.00- +
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200mg￥0.000.00- +
- 货号: ajcx13818
- CAS: N/A
- 别名:
- 分子式: C27H29Cl2N7O2S
- 分子量: 586.54
- 纯度: ＞98%
- 溶解度: Water: ≥ 25 mg/mL (42.62 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
CX-5461 is an inhibitor of ribosomal RNA (rRNA) synthesis. It selectively inhibits RNA polymerase I-driven transcription of rRNA in HCT116, A375, and MIA PaCa-2 tumor cells (IC50s = 142, 113, and 54 nM, respectively) without affecting RNA polymerase II (IC50 > 25?M), DNA replication, or protein translation.1,2 At 50 mg/kg, CX-5461 demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.1
1.Drygin, D., Lin, A., Bliesath, J., et al.Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growthCancer Res.71(4)1418-1430(2011) 2.Haddach, M., Schwaebe, M.K., Michaux, J., et al.Discovery of CX-5461, the first direct and selective inhibitor of RNA polymerase I, for cancer therapeuticsACS Med. Chem. Lett.3(7)602-606(2012)
