850807-63-5
Chemical Structure
RSM-932A
Synonym(s): TCD-717
- CAS. Nr.: 850807-63-5
- Formula:C46H38Br2Cl2N4
- Molecular Weight:877.53
IUPAC Name: 1,1'-([1,1'-biphenyl]-4,4'-diylbis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolin-1-ium) bromide
InChIKey: DGBVSSXGHKAASQ-UHFFFAOYSA-L
SMILES: CN(C1=C2C=CC=CC2=[N+](CC3=CC=C(C4=CC=C(C[N+]5=C6C=CC=CC6=C(N(C7=CC=C(Cl)C=C7)C)C=C5)C=C4)C=C3)C=C1)C8=CC=C(Cl)C=C8.[Br-].[Br-]
Biological Activity: 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].
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RSM-932A | 98.77% | 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. | ||||||||||||||||||||
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RSM-932A (Standard) | ≥98% | RSM-932A (Standard) is the analytical standard of RSM-932A (HY-101144). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
