RSM-932A

RSM-932A, also known as TCD-717, is a ChoKα inhibitor, which targets the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. RSM-932A appears to have an altogether novel mechanism of inhibition and is synergistic with respect to both choline and ATP. RSM-932A have in vitro inhibitory activity in the low nanomolar range. RSM-932A significantly reduced parasitemia and induced the accumulation of trophozoites and schizonts, blocking intraerythrocytic development and interfering with parasite egress or invasion, suggesting a delay of the parasite maturation stage.

Product information

CAS Number: 850807-63-5

Molecular Weight: 877.53

Formula: C46H38Br2Cl2N4

Chemical Name: 1, 1'-([1, 1'-biphenyl]-4, 4'-diylbis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolin-1-ium) bromide

Smiles: [Br-].[Br-].CN(C1=CC=[N+](CC2C=CC(=CC=2)C2C=CC(C[N+]3=CC=C(C4=CC=CC=C34)N(C)C3C=CC(Cl)=CC=3)=CC=2)C2=CC=CC=C12)C1C=CC(Cl)=CC=1

InChiKey: DGBVSSXGHKAASQ-UHFFFAOYSA-L

InChi: InChI=1S/C46H38Cl2N4.2BrH/c1-49(39-23-19-37(47)20-24-39)43-27-29-51(45-9-5-3-7-41(43)45)31-33-11-15-35(16-12-33)36-17-13-34(14-18-36)32-52-30-28-44(42-8-4-6-10-46(42)52)50(2)40-25-21-38(48)22-26-40;;/h3-30H,31-32H2,1-2H3;2*1H/q+2;;/p-2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Lacal JC, Campos JM. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol Cancer Ther. 2015 Jan;14(1):31-9. doi: 10.1158/1535-7163.MCT-14-0531. Epub 2014 Dec 8. PubMed PMID: 25487918.
2. Zimmerman T, Moneriz C, Diez A, Bautista JM, Gómez Del Pulgar T, Cebrián A, Lacal JC. Antiplasmodial activity and mechanism of action of RSM-932A, a promising synergistic inhibitor of Plasmodium falciparum choline kinase. Antimicrob Agents Chemother. 2013 Dec;57(12):5878-88. doi: 10.1128/AAC.00920-13. Epub 2013 Sep 16. PubMed PMID: 24041883; PubMed Central PMCID: PMC3837925.

Products are for research use only. Not for human use.