| Identification | Back Directory | [Name]
RSM932A | [CAS]
850807-63-5 | [Synonyms]
TCD717
RSM932A
TCD 717
TCD-717.
RSM-932A; RSM 932A; RSM932A; TCD 717; TCD717; TCD-717.
1,1''-([1,1''-Biphenyl]-4,4''-diylbis(methylene))bis(4-(methyl(p-tolyl)amino)quinolin-1-ium) bromide | [Molecular Formula]
C46H38BrCl2N4+ | [MDL Number]
MFCD29058562 | [MOL File]
850807-63-5.mol | [Molecular Weight]
797.64 |
| Chemical Properties | Back Directory | [Melting point ]
255-257 °C | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 3 mg/ml; DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml | [form ]
A crystalline solid | [color ]
White to yellow |
| Hazard Information | Back Directory | [Description]
RSM-932A is a selective inhibitor of choline kinase α (CHOKα; IC50s = 1 and >50 μM for CHOKα and β, respectively). It induces apoptosis via CHOP signaling and endoplasmic reticulum (ER) stress in MDA-MB-231, MCF-7, SW620, and H460 cancer cells, but it only induces cell cycle arrest and not apoptosis in NCM460 and MCF-10A normal epithelial cells. RSM-932A inhibits the growth of HT-29 colon cancer cells in vitro (IC50 = 1.15 μM) and in vivo in a mouse xenograft model (ED50 = 7.5 mg/kg). | [Uses]
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]. | [in vivo]
RSM-932A exhibits a potent in vivo anticancer activity, and lack of toxicity at the effective doses[1]. | Animal Model: | Athymic nu/nu mice, CD1 nude mice, and BALB/c nude (six-week-old) bearing human tumor xenografts (colon adenocarcinoma HT29, non-small cell lung cancer (NSCLC) H-460, breast adenocarcinoma MDA-MB-231)[3] | | Dosage: | 7.5 mg/kg, 6 mg/kg, 5 mg/kg, 3 mg/kg, 1 mg/kg, 0.3 mg/kg | | Administration: | Administration routes (intraperitoneal or intravenous), treatment schedule (5 consecutive days, 3 days per week, 2 days per week, 1 day per week) | | Result: | The LD50 was 10.9 mg/kg in mice. The effective dose used in the in vivo experiments was 7.5 mg/kg. |
| [References]
[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. DOI:10.1158/1535-7163.MCT-14-0531
[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. DOI:10.1371/journal.pone.0064961
[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. DOI:10.1038/s41598-020-72165-6
[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. DOI:10.1128/AAC.00920-13 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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