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CX-5461

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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
Product Categories:
  • apis
  • Inhibitors
Mol File:
1138549-36-6.mol
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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)
color 
White to yellow
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CX-5461 Usage And Synthesis

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

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