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 2-(4-甲基-1,4-二氮杂卓-1-基)-N-((5-甲基吡嗪-2-基)甲基)-5-氧代-5H-苯并[4,5]噻唑并[3,2-a][1,8]萘啶-6-甲酰胺
CAS 1138549-36-6 MFCD238549366
化学结构图
SMILES: Cc1cnc(CNC(=O)c2c(=O)c3ccc(N4CCCN(C)CC4)nc3n3c2sc2ccccc23)cn1
化学属性
| Mol. Weight | 513.61 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| 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 |
|---|---|
| Formula | C27H27N7O2S |
| Synonym | CX5461; CX 5461; CX-5461. |
| IUPAC 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 |
| InChIKey | XGPBJCHFROADCK-UHFFFAOYSA-N |
| InChI | InChI=1S/C27H27N7O2S/c1-17-14-29-18(15-28-17)16-30-26(36)23-24(35)19-8-9-22(33-11-5-10-32(2)12-13-33)31-25(19)34-20-6-3-4-7-21(20)37-27(23)34/h3-4,6-9,14-15H,5,10-13,16H2,1-2H3,(H,30,36) |
| Canonical SMILES | O=C(C1=C(SC2=CC=CC=C23)N3C4=C(C=CC(N5CCN(C)CCC5)=N4)C1=O)NCC6=NC=C(C)N=C6 |
| Chemical Name Translation | 2-(4-甲基-1,4-二氮杂卓-1-基)-N-((5-甲基吡嗪-2-基)甲基)-5-氧代-5H-苯并[4,5]噻唑并[3,2-a][1,8]萘啶-6-甲酰胺 |
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产品应用
- 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.
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