MedKoo Cat#: 413396 | Name: Pidnarulex HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pidnarulex (CX-5461) is a small-molecule inhibitor that selectively targets RNA polymerase I–mediated rRNA synthesis, exhibiting potent anticancer activity, particularly in tumors with defective homologous recombination (HR) repair mechanisms such as BRCA1/2 mutations. It stabilizes G-quadruplex DNA structures and induces replication stress and DNA damage, leading to synthetic lethality in HR-deficient cancer cells. Preclinical studies have shown nanomolar potency against a range of HR-deficient tumor cell lines, with GI₅₀ values typically in the range of 50–150 nM. In vivo, CX-5461 has demonstrated significant tumor regression in BRCA-deficient xenograft models

Chemical Structure

Pidnarulex HCl
Pidnarulex HCl
CAS# 2101314-20-7 (HCl)

Theoretical Analysis

MedKoo Cat#: 413396

Name: Pidnarulex HCl

CAS#: 2101314-20-7 (HCl)

Chemical Formula: C27H28ClN7O2S

Exact Mass: 0.0000

Molecular Weight: 550.08

Elemental Analysis: C, 58.95; H, 5.13; Cl, 6.44; N, 17.82; O, 5.82; S, 5.83

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
Pidnarulex HCl; Pidnarulex hydrochloride; CX5461; CX-5461; CX 5461;
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
Solvent mg/mL mM
Solubility
Soluble in DMSO 0.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
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.