WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H413396
CAS#: 2101314-20-7 (HCl)
Description: Pidnarulex HCl is the salt form of CX-5461, a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. CX-5461 selectively inhibits rRNA synthesis by Pol I in the nucleolus, but does not inhibit mRNA synthesis by RNA Polymerase II (Pol II) and does not inhibit DNA replication or protein synthesis. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. The RP bind to Mdm2 and liberate p53 to orchestrate apoptosis in cancer cells. CX-5461 demonstrates a favorable preclinical profile, potently and selectively kills cancer cells, demonstrates robust in vivo efficacy in multiple models, and has demonstrated oral bioavailability in multiple species.
Hodoodo Cat#: H413396
Name: Pidnarulex HCl
CAS#: 2101314-20-7 (HCl)
Chemical Formula: C27H28ClN7O2S
Exact Mass: 0.00
Molecular Weight: 550.080
Elemental Analysis: C, 58.95; H, 5.13; Cl, 6.44; N, 17.82; O, 5.82; S, 5.83
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Related CAS #: 2101314-20-7 (HCl) 1138549-36-6 (free base),
Synonym: Pidnarulex HCl; CX5461 hydrochloride; CX 5461 hydrochloride; CX-5461 hydrochloride
IUPAC/Chemical Name: 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 hydrochloride
InChi Key: YCGHUQKYOCALNJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C27H27N7O2S.ClH/c1-17-14-29-18(15-28-17)16-30-26(36)23-24(35)19-8-9-22(33-11-5-10-32(2)12-13-33)31-25(19)34-20-6-3-4-7-21(20)37-27(23)34;/h3-4,6-9,14-15H,5,10-13,16H2,1-2H3,(H,30,36);1H
SMILES Code: O=C(C1=C(SC2=CC=CC=C23)N3C4=NC(N5CCN(C)CCC5)=CC=C4C1=O)NCC6=NC=C(C)N=C6.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 550.08 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Quin JE, Devlin JR, Cameron D, Hannan KM, Pearson RB, Hannan RD. Targeting the nucleolus for cancer intervention. Biochim Biophys Acta. 2014 Jun;1842(6):802-816. doi: 10.1016/j.bbadis.2013.12.009. Epub 2014 Jan 2. Review. PubMed PMID: 24389329.
2: Achiron A, Mashiach R, Zilkha-Falb R, Meijler MM, Gurevich M. Polymerase I pathway inhibitor ameliorates experimental autoimmune encephalomyelitis. J Neuroimmunol. 2013 Oct 15;263(1-2):91-7. doi: 10.1016/j.jneuroim.2013.08.002. Epub 2013 Aug 15. PubMed PMID: 23998422.
3: Bywater MJ, Poortinga G, Sanij E, Hein N, Peck A, Cullinane C, Wall M, Cluse L, Drygin D, Anderes K, Huser N, Proffitt C, Bliesath J, Haddach M, Schwaebe MK, Ryckman DM, Rice WG, Schmitt C, Lowe SW, Johnstone RW, Pearson RB, McArthur GA, Hannan RD. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer Cell. 2012 Jul 10;22(1):51-65. doi: 10.1016/j.ccr.2012.05.019. PubMed PMID: 22789538; PubMed Central PMCID: PMC3749732.
4: Drygin D, 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. doi: 10.1158/0008-5472.CAN-10-1728. Epub 2010 Dec 15. PubMed PMID: 21159662.