850807-63-5
850807-63-5 structure
- Name: RSM-932A
- Chemical Name: rsm932a
- CAS Number: 850807-63-5
- Molecular Formula: C46H38Br2Cl2N4
- Molecular Weight: 877.53500
- Catalog: Research Areas Cancer
- Create Date: 2016-08-29 23:50:59
- Modify Date: 2025-09-03 23:05:49
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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].
| Name | rsm932a |
|---|---|
| Synonyms |
1,1'-([1,1'-biphenyl]-4,4'-diylbis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolin-1-ium) bromide
1,1'-(biphenyl-4,4'-diylmethylene)bis[4-(4-chloro-N-methylanilino)quinolinium] dibromide RSM-932A 1,1'-([1,1'-biphenyl]-4,4'-diylbis(methylene))bis(4-(methyl(p-tolyl)amino)quinolin-1-ium) bromide |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
ChoKα[1] |
| In Vitro | 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]. Cell Proliferation Assay[2] Cell Line: DLD-1, HT29, SW620 and HCT116 CRC cell lines and the non-tumourigenic CCD-841 cell line Concentration: 2, 3, 4 µM Incubation Time: 24 hours Result: Triggered to cell death. Western Blot Analysis[2] Cell Line: DLD-1, HT29 and SW620 cell lines Concentration: 2, 4, 6, 8, 10 uM Incubation Time: 24 hours Result: A dosage-dependent decrease in the levels of thymidylate synthase (TS) and thymidine kinase (TK1) proteins. |
| 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 |
| Melting Point | 255 - 257 °C |
|---|---|
| Molecular Formula | C46H38Br2Cl2N4 |
| Molecular Weight | 877.53500 |
| Exact Mass | 874.08400 |
| PSA | 14.24000 |
| LogP | 13.09040 |