AN3661
Based on 2 publication(s) in Google Scholar
AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.58%
- No. CAS: 1268335-33-6
- Fòrmula: C10H11BO4
- Peso molecular:206.00
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) AN3661
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Actividad biológica
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Plasmodium |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
>100 μM
Compound: 65
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Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 31264855] |
| HeLa | IC50 |
>100 μM
Compound: 1
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Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
|
[PMID: 21195617] |
| Jurkat | IC50 |
60.5 μM
Compound: 1
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Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay
Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay
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[PMID: 21195617] |
| MDA-MB-231 | IC50 |
>100 μM
Compound: 65
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Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
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[PMID: 31264855] |
| SK-OV-3 | IC50 |
>100 μM
Compound: 65
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Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay
Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay
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[PMID: 31264855] |
| WI-38 | IC50 |
>100 μM
Compound: 65
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Cytotoxicity against human WI38 cells after 72 hrs by MTT assay
Cytotoxicity against human WI38 cells after 72 hrs by MTT assay
|
[PMID: 31264855] |
AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC50=64 nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC50 60.5 μM against Jurkat cells, and all other CC50 values greater than the highest concentrations tested (25 μM or above)[1].
AN3661 inhibits the stability of P. falciparum transcripts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED90 4 days after initiation of treatment is 0.57 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:P. berghei-infected mice (malaria model)[1]
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Dosage:50, 100, 200 mg/kg
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Administration:Orally; daily for 4 days
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Result:Rapidly controlled parasitemias, with an ED90 of 0.34 mg/kg. Daily dosages of 50 mg/kg and 100 mg/kg extended survival, and mice treated with 200 mg/kg per day demonstrated long-term cures.
Chemical Information
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No. CAS 1268335-33-6
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Appearance Solid
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Peso molecular 206.00
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Fòrmula C10H11BO4
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Color White to off-white
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SMILES
O=C(O)CCC1=C(B(O)OC2)C2=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
-
Most Recent
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RNA
2021 Oct;27(10):1148-1154. PMID: 34230059 -
Solvente y solubilidad
DMSO : 250 mg/mL (1213.59 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (10.10 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (10.10 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (279 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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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.8544 mL | 24.2718 mL | 48.5437 mL | 121.3592 mL |
| 5 mM | 0.9709 mL | 4.8544 mL | 9.7087 mL | 24.2718 mL | |
| 10 mM | 0.4854 mL | 2.4272 mL | 4.8544 mL | 12.1359 mL | |
| 15 mM | 0.3236 mL | 1.6181 mL | 3.2362 mL | 8.0906 mL | |
| 20 mM | 0.2427 mL | 1.2136 mL | 2.4272 mL | 6.0680 mL | |
| 25 mM | 0.1942 mL | 0.9709 mL | 1.9417 mL | 4.8544 mL | |
| 30 mM | 0.1618 mL | 0.8091 mL | 1.6181 mL | 4.0453 mL | |
| 40 mM | 0.1214 mL | 0.6068 mL | 1.2136 mL | 3.0340 mL | |
| 50 mM | 0.0971 mL | 0.4854 mL | 0.9709 mL | 2.4272 mL | |
| 60 mM | 0.0809 mL | 0.4045 mL | 0.8091 mL | 2.0227 mL | |
| 80 mM | 0.0607 mL | 0.3034 mL | 0.6068 mL | 1.5170 mL | |
| 100 mM | 0.0485 mL | 0.2427 mL | 0.4854 mL | 1.2136 mL |