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CX-5461

Product Name
CX-5461
CAS No.
1138549-36-6
Chemical Name
CX-5461
Synonyms
CS-1938;CX-5461;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
Formula Weight
513.61
MOL File
1138549-36-6.mol
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CX-5461 Property

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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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.09265
Product name
RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem
Packaging
10mg
Price
$280
Updated
2024/03/01
Cayman Chemical
Product number
18392
Product name
CX-5461
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
18392
Product name
CX-5461
Purity
≥98%
Packaging
5mg
Price
$161
Updated
2024/03/01
Cayman Chemical
Product number
18392
Product name
CX-5461
Purity
≥98%
Packaging
10mg
Price
$231
Updated
2024/03/01
Cayman Chemical
Product number
18392
Product name
CX-5461
Purity
≥98%
Packaging
50mg
Price
$957
Updated
2024/03/01
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CX-5461 Chemical Properties,Usage,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

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CX-5461 Suppliers

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8415
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
Shanghai civi chemical technology co.,Ltd
Tel
86-21-34053660
Fax
86-21-34053661
Email
sale@labgogo.com
Country
China
ProdList
9865
Advantage
52
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Fax
021-50323701
Email
market@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
shanghai cooperpharm co.,LTD .
Tel
+86-021-58975553
Fax
+86-021-58975554
Email
sales@cooperpharm.com
Country
China
ProdList
1210
Advantage
56
Shanghai Witofly Chemical Co.,Ltd
Tel
Email
sales@witofly.com
Country
China
ProdList
2864
Advantage
52
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View Lastest Price from CX-5461 manufacturers

Career Henan Chemical Co
Product
CX-5461 1138549-36-6
Price
US $7.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2019-07-01

1138549-36-6, CX-5461Related Search:


  • 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-
  • CX-5461;CX 5461;CX5461
  • CX-5461 500MG
  • 2-(4-Methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3
  • CX-5461, >=98%
  • CX-5461 USP/EP/BP
  • 2-(4-methyl-1,4-diazepan-1-yl)-N-[(5-methylpyrazin-2-yl)methyl]-5-oxo-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
  • Pidanrulex
  • RNA Polymerase I Inhibitor II CX-5461 CX5461
  • CX-5461 Pidnarulex
  • Pidnarulex
  • 1138549-36-6
  • C27H27N7O2S
  • apis
  • Inhibitors