For research use only. Not for therapeutic Use.
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles[1][2][3].
RSM-932A has a potent anti-proliferative activity against most tumor-derived cell lines tested, including those derived from breast, lung, colon, bladder, liver, ovary, bone, cervix, kidney, pancreas, melanoma, and brain tumors, with IC50s of 1.3-7.1 μM for 72 hours[1].?
RSM-932A (TCD-717; 2-4 μM; for 24 hours) promotes cell death of colon cancer cells[2].?
RSM-932A (2-10 μM) exhibits a dosage-dependent decrease in the levels of thymidylate synthase (TS) and thymidine kinase (TK1) proteins proteins[2].?
RSM-932A inhibits Streptococcus pneumoniae choline kinase (sChoK) with IC50 of 0.5 μM in LDH/PK and colorimetric enzymatic assays[3].?
The minimum inhibitory concentration (MIC) of RSM-932A for S. pneumoniae is 0.4 μM, and the minimum lethal concentration (MLC) is 1.6 μM[3]. ?
RSM-932A is a comparatively potent inhibitor with the IC50 of 1.75 μM in a steady-state reaction in which the concentration of Choline is equivalent to its Km[4].
RSM-932A exhibits a potent in vivo anticancer activity, and lack of toxicity at the effective doses[1].
| Catalog Number | I009226 |
| CAS Number | 850807-63-5 |
| Synonyms | 1-[[4-[4-[[4-(4-chloro-N-methylanilino)quinolin-1-ium-1-yl]methyl]phenyl]phenyl]methyl]-N-(4-chlorophenyl)-N-methylquinolin-1-ium-4-amine;dibromide |
| Molecular Formula | C46H38Br2Cl2N4 |
| Purity | ≥95% |
| 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 |
| InChIKey | DGBVSSXGHKAASQ-UHFFFAOYSA-L |
| SMILES | CN(C1=CC=C(C=C1)Cl)C2=CC=[N+](C3=CC=CC=C32)CC4=CC=C(C=C4)C5=CC=C(C=C5)C[N+]6=CC=C(C7=CC=CC=C76)N(C)C8=CC=C(C=C8)Cl.[Br-].[Br-] |
| Reference | [1]. Juan Carlos Lacal, et al. 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. [2]. Ana de la Cueva, et al. Combined 5-FU and ChoKα inhibitors as a new alternative therapy of colorectal cancer: evidence in human tumor-derived cell lines and mouse xenografts. PLoS One. 2013 Jun 10;8(6):e64961. [3]. Tahl Zimmerman, et al. Identification and validation of novel and more effective choline kinase inhibitors against Streptococcus pneumonia. Sci Rep. 2020 Sep 22;10(1):15418. [4]. Tahl Zimmerman, et al. 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. |
