| CX-5461 Basic information |
| Product Name: | CX-5461 |
| Synonyms: | CX-5461;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;RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem;CS-1938;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;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]napht;5H-Benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo- |
| CAS: | 1138549-36-6 |
| MF: | C27H27N7O2S |
| MW: | 513.61 |
| EINECS: | |
| Product Categories: | apis;Inhibitors |
| Mol File: | 1138549-36-6.mol |
| CX-5461 Chemical Properties |
| Boiling point | 739.9±60.0 °C(Predicted) |
| density | 1.45 |
| storage temp. | +2C to +8C |
| solubility | insoluble in H2O; insoluble in EtOH; insoluble in DMSO |
| form | Light beige powder |
| pka | 8.53±0.20(Predicted) |
| Safety Information |
| MSDS Information |
| CX-5461 Usage And Synthesis |
| General Description | A cell-permeable benzothiazole compound that selectively inhibits RNA polymerase I-mediated pre-rRNA transcription (IC50 = 142 nM in HCT-116), but not Pol II-mediated c-myc transcription, by preventing TAF SL1 and rDNA association). Effectively inhibits Pol I-dependent proliferation among 39 cancer cell lines (IC50<1 μM) in vitro and suppresses A375 (50 mg/kg/d p.o.) and MIA PaCa-2 (50 mg/kg/3d p.o.) tumor expansion in vivo. |
| Biological Activity | cx-5461 is a potent and orally bioavailable small-molecule inhibitor of rrna synthesis that specifically inhibits rna polymerase (pol) i-driven transcription with ic50 value of 142 nm. cx-5461 exhibits antiproliferative activity against human pancreatic tumor cells mia paca-2, human melanoma cells a375 and colorectal carcinoma cells hct-116 with ec50 values of 74, 58, and 167 nmol/l, respectively. [1].cx-5461 was revealed to inhibit pol i transcription via promoting the stabilization of p53. in addition, cx-5461 has been demonstrated to induce autophagy and senescence but not apoptosis in mia paca-2 and a375 cell lines. |
| Biochem/physiol Actions | Cell permeable: yes |
| in vivo | cx-5461 has shown to suppress tumor volume in both mia paca-2 and a375 derived xenograft mice models [1]. |
| references | [1] drygin d1, lin a, bliesath j, ho cb, o'brien se, proffitt c, omori m, haddach m, schwaebe mk, siddiqui-jain a, streiner n, quin je, sanij e, bywater mj,hannan rd, ryckman d, anderes k, rice wg. 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 |
| CX-5461 Preparation Products And Raw materials |
Please leave a message for us or use the following ways to contact us, we will reply to you as soon as possible, and provide you with the most sincere service, thank you.
日本语
한국어
Français
Deutsch
España
Türkiye