CX-5461 Inhibitor CAS No. 1138549-36-6

Cat. No.	Name	Size	Price
KI0469	CX-5461	5 mg	$432
	CX-5461	10 mg	$592
	CX-5461	50 mg	$1552
	CX-5461	200 mg	$4272

Chemical Characteristic

Product Name	CX-5461
CAS No.	1138549-36-6
Molecular Weight	513.61
Formula	C₂₇H₂₇N₇O₂S
Chemical Name	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
Smiles	n12c(c(c(=O)c3ccc(nc13)N1CCN(CCC1)C)C(=O)NCc1cnc(cn1)C)sc1c2cccc1
Chemical Structure

Biological activities

CX-5461 is a potent small-molecule inhibitor of rRNA synthesis. CX-5461 selectively inhibits Pol I-driven transcription of rRNA with IC50 values of 142, 113, and 54 nM in the HCT-116 cells, melanoma A375, and pancreatic carcinoma MIA PaCa-2, respectively. However, the IC50 of CX-5461 against Pol II-driven transcription of rRNA is > 25 μM in the HCT-116 cells. CX-5461 possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation. CX-5461 (1 μM) causes rapid inhibition of Pol I transcription, with an observed half-life of 21 minutes for 45S pre-rRNA in MIA PaCa-2 cells. The median EC50 across all tested cell lines (including EOL-1, SR, K562, HCT-116, and LNCaP) is 147 nM. However, all normal cell lines have EC50 values of approximately 5 μM. CX-5461 shows significant antiproliferative potency against HCT-116, A375, and MIA PaCa-2 cell lines with EC50 values of 167, 58, and 74 nM, respectively. CX-5461 also inhibits the initiation stage of rRNA synthesis and induces both senescence and autophagy through a p53-independent process in solid tumor cell lines. In vivo, CX-5461 is orally bioavailable. CX-5461 also shows antitumor activity against human solid tumors in murine xenograft models.^[1] CX-5461 can selectively kills B-lymphoma cells in vivo while maintaining a viable wild-type B cell population.^[2]

References

[1] Drygin D, et al. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer Res. 2011, 71(4): 1418-1430. [2] Bywater MJ, et al. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer Cell. 2012, 22(1): 51-65.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com