RSM-932A
Based on 1 Customer Validation
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.77%
- CAS 番号: 850807-63-5
- 分子式: C46H38Br2Cl2N4
- 分子量:877.53
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
ChoKα[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
1.2 μM
Compound: 22
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In vitro antiproliferative effect in ras-transformed HT 29 cells
In vitro antiproliferative effect in ras-transformed HT 29 cells
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[PMID: 15857141] |
| MCF-10A | IC50 |
7.1 μM
Compound: 6; RSM-932A
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Cytotoxicity against human MCF10A cells after 72 hrs by MTT assay
Cytotoxicity against human MCF10A cells after 72 hrs by MTT assay
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[PMID: 26700752] |
| MDA-MB-468 | IC50 |
2.4 μM
Compound: 6; RSM-932A
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Cytotoxicity against human MDA-MB-468 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-468 cells after 72 hrs by MTT assay
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[PMID: 26700752] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLD-1, HT29, SW620 and HCT116 CRC cell lines and the non-tumourigenic CCD-841 cell line
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Concentration:2, 3, 4 µM
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Incubation Time:24 hours
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Result:Triggered to cell death.
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Cell Line:DLD-1, HT29 and SW620 cell lines
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Concentration:2, 4, 6, 8, 10 uM
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Incubation Time:24 hours
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Result:A dosage-dependent decrease in the levels of thymidylate synthase (TS) and thymidine kinase (TK1) proteins.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:7.5 mg/kg, 6 mg/kg, 5 mg/kg, 3 mg/kg, 1 mg/kg, 0.3 mg/kg
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Administration:Administration routes (intraperitoneal or intravenous), treatment schedule (5 consecutive days, 3 days per week, 2 days per week, 1 day per week)
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Result:The LD50 was 10.9 mg/kg in mice. The effective dose used in the in vivo experiments was 7.5 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 850807-63-5
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性状 Solid
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分子量 877.53
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分子式 C46H38Br2Cl2N4
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Color White to yellow
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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-]
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別名
TCD-717
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 16.67 mg/mL (19.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (1.90 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1396 mL | 5.6978 mL | 11.3956 mL | 28.4891 mL |
| 5 mM | 0.2279 mL | 1.1396 mL | 2.2791 mL | 5.6978 mL | |
| 10 mM | 0.1140 mL | 0.5698 mL | 1.1396 mL | 2.8489 mL | |
| 15 mM | 0.0760 mL | 0.3799 mL | 0.7597 mL | 1.8993 mL |
RSM-932A 関連分類
HY-101144 関連分類
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