RSM932A
- Product Name
- RSM932A
- CAS No.
- 850807-63-5
- Chemical Name
- RSM932A
- Synonyms
- TCD717;TCD 717;RSM932A;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;1,1'-([1,1'-Biphenyl]-4,4'-diylbis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolin-1-ium) bromide
- CBNumber
- CB53168588
- Molecular Formula
- C46H38BrCl2N4+
- Formula Weight
- 797.64
- MOL File
- 850807-63-5.mol
RSM932A Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P330Rinse mouth.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SML2696
- Product name
- RSM932A
- Purity
- ≥97% (HPLC)
- Packaging
- 5MG
- Price
- $100
- Updated
- 2025/07/31
- Product number
- SML2696
- Product name
- RSM932A
- Purity
- ≥97% (HPLC)
- Packaging
- 25MG
- Price
- $406
- Updated
- 2025/07/31
- Product number
- 21518
- Product name
- RSM-932A
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $29
- Updated
- 2024/03/01
- Product number
- 21518
- Product name
- RSM-932A
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $107
- Updated
- 2024/03/01
- Product number
- 21518
- Product name
- RSM-932A
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $197
- Updated
- 2024/03/01
RSM932A Chemical Properties,Usage,Production
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
RSM932A Preparation Products And Raw materials
Raw materials
Preparation Products
RSM932A Suppliers
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- United States
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