Cabamiquine
Based on 1 publication(s) in Google Scholar
Cabamiquine (DDD107498) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.61%
- CAS. Nr.: 1469439-69-7
- Formel: C27H31FN4O2
- Molecular Weight:462.56
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Publications Citing Use of MedChemExpress (MCE) Cabamiquine
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Biologische Aktivität
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CaMK III |
Plasmodium |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L6 | IC50 |
28.47 μM
Compound: DDD107498
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Cytotoxicity against rat L6 cells after 70 hrs by alamar blue staining based fluorometric assay
Cytotoxicity against rat L6 cells after 70 hrs by alamar blue staining based fluorometric assay
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[PMID: 28279559] |
| MRC5 | EC50 |
24 μM
Compound: 2; DDD107498
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Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability after 68 hrs by resazurin dye based fluorescence assay
Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability after 68 hrs by resazurin dye based fluorescence assay
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[PMID: 27631715] |
Cabamiquine (24-48 h) leads to abnormal trophozoites, and inhibits the development of trophozoites and schizonts in parasites, and inhibits protein synthesis[1].
Cabamiquine shows excellent activity against 3D7 parasites: EC50 =1.0 nM, EC90 = 2.4 nM, EC99 = 5.9 nM[1].
Cabamiquine shows good metabolic stability when incubated with hepatic microsomes or hepatocyte[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cabamiquine (p.o., 3 mg/kg) shows Cmax of 80 ng/mL, Tmax of 4 h, AUC of 200542 ng·min/mL, F (%) of 84%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1469439-69-7
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Appearance Solid
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Molecular Weight 462.56
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Formel C27H31FN4O2
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC=C(C=C2)CN3CCOCC3)=NC4=CC=C(C=C41)F)NCCN5CCCC5
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Synonyms
DDD107498; DDD-498; M5717
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (216.19 mM; Need ultrasonic; 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 (protect from 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (protect from 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.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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 (protect from 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 | 2.1619 mL | 10.8094 mL | 21.6188 mL | 54.0470 mL |
| 5 mM | 0.4324 mL | 2.1619 mL | 4.3238 mL | 10.8094 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1619 mL | 5.4047 mL | |
| 15 mM | 0.1441 mL | 0.7206 mL | 1.4413 mL | 3.6031 mL | |
| 20 mM | 0.1081 mL | 0.5405 mL | 1.0809 mL | 2.7024 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1619 mL | |
| 30 mM | 0.0721 mL | 0.3603 mL | 0.7206 mL | 1.8016 mL | |
| 40 mM | 0.0540 mL | 0.2702 mL | 0.5405 mL | 1.3512 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0809 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3603 mL | 0.9008 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6756 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL |
Cabamiquine Related Classifications
HY-117684 Related Classifications
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