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;Pidnarulex (CX-5461)
- CBNumber
- CB62561466
- Molecular Formula
- C27H27N7O2S
- Formula Weight
- 513.61
- MOL File
- 1138549-36-6.mol
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
- InChIKey
- XGPBJCHFROADCK-UHFFFAOYSA-N
- SMILES
- [s]1c2[n](c4nc(ccc4[c](c2C(=O)NCc6ncc(nc6)C)=O)N5CCN(CCC5)C)c3c1cccc3
Safety
- WGK Germany
- WGK 3
- Storage Class
- 11 - Combustible Solids
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 5.09265
- Product name
- RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem
- Packaging
- 10mg
- Price
- $309
- Updated
- 2026/03/19
- Product number
- 18392
- Product name
- CX-5461
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 18392
- Product name
- CX-5461
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 18392
- Product name
- CX-5461
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $231
- Updated
- 2024/03/01
- Product number
- 18392
- Product name
- CX-5461
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $957
- Updated
- 2024/03/01
CX-5461 Chemical Properties,Usage,Production
Uses
A cell-permeable benzothiazole compound that selectively inhibits RNA polymerase I-mediated pre-rRNA transcription (IC50 = 142, 113, 54, and 74 nM in HCT-116, A375, MIA PaCa-2, and BJ-hTert cells, respectively), but not Pol II-mediated c-myc transcription, by preventing TAF (TATA Binding Protein-/TBP-Associated Factor) SL1 and rDNA association, effectively inhibiting Pol I-dependent proliferation among 39 cancer cell lines (IC50<1 µM) in vitro. While Pol I inhibition by CX-5461 is shown to result in p53-dependent apoptosis in cancer cells of hematopoietic origin, cell death by CX-5461 treatment in solid tumors-derived A375 and MIA PaCa-2 cultures are primarily due to autophagy and senescence, but not apoptosis, induction. Shown to suppress A375 (50 mg/kg/d p.o.) and MIA PaCa-2 (50 mg/kg/3d p.o.) tumor expansion, as well as selectively induce p53-mediated cell death of Eμ-Myc lymphoma, but not normal B cells, in mice (50 mg/kg p.o.) in vivo.
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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View Lastest Price from CX-5461 manufacturers
- Product
- CX-5461 1138549-36-6
- Price
- US $7.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100KG
- Release date
- 2019-07-01