CX-5461
- CAS No.
- 1138549-36-6
- Chemical Name:
- CX-5461
- Synonyms
- CX-5461;CS-1938;Pidanrulex;Pidnarulex;CX-5461 500MG;CX-5461/CX5461;CX-5461, >=98%;CX-5461 USP/EP/BP;CX-5461 Pidnarulex;CX-5461;CX 5461;CX5461
- CBNumber:
- CB62561466
- Molecular Formula:
- C27H27N7O2S
- Molecular Weight:
- 513.61
- MDL Number:
- MFCD21609261
- MOL File:
- 1138549-36-6.mol
| 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) |
| FDA UNII | 3R4C5YLB9I |
CX-5461 price More Price(21)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 5.09265 | RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem | 1138549-36-6 | 10mg | $280 | 2024-03-01 | Buy |
| Cayman Chemical | 18392 | CX-5461 ≥98% | 1138549-36-6 | 1mg | $44 | 2024-03-01 | Buy |
| Cayman Chemical | 18392 | CX-5461 ≥98% | 1138549-36-6 | 5mg | $161 | 2024-03-01 | Buy |
| Cayman Chemical | 18392 | CX-5461 ≥98% | 1138549-36-6 | 10mg | $231 | 2024-03-01 | Buy |
| Cayman Chemical | 18392 | CX-5461 ≥98% | 1138549-36-6 | 50mg | $957 | 2024-03-01 | Buy |
CX-5461 Chemical Properties,Uses,Production
Definition
ChEBI: CX-5461 is an organic heterotetracyclic compound that is 5-oxo-5H-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxylic acid substituted by a 4-methyl-1,4-diazepan-1-yl group at position 2 and in which the carboxy group at position 6 is substituted by a [(5-methylpyrazin-2-yl)methyl]nitrilo group. An inhibitor of ribosomal RNA (rRNA) synthesis which specifically inhibits RNA polymerase I-driven transcription of rRNA in several cancer cell lines. It is currently in phase I/II clinical trials for advanced hematologic malignancies and triple-negative breast cancer with BRCA1/2 mutation. It has a role as an antineoplastic agent, an apoptosis inducer and an EC 2.7.7.6 (RNA polymerase) inhibitor. It is a diazepine, an organic heterotetracyclic compound, a member of pyrazines, a secondary carboxamide and a naphthyridine derivative.
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].
target
Pol I
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
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 | product@chemlin.com.cn | CHINA | 3012 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29118 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
