ML753286
Based on 1 publication(s) in Google Scholar
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species.
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- No. CAS: 1699720-89-2
- Fòrmula: C20H25N3O3
- Peso molecular:355.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ML753286
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Actividad biológica
IC50: 0.6 μM (BCRP)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
>10 μM
Compound: 14A
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Inhibition of BCRP in human Caco2 cells using 3H-Estron-3-sulfate as substrate measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis
Inhibition of BCRP in human Caco2 cells using 3H-Estron-3-sulfate as substrate measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis
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[PMID: 26642765] |
| Caco-2 | IC50 |
0.61 μM
Compound: 14A
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Inhibition of BCRP in human Caco2 cells using 3H-Estron-3-sulfate as substrate assessed as Ko143 IC50 measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis
Inhibition of BCRP in human Caco2 cells using 3H-Estron-3-sulfate as substrate assessed as Ko143 IC50 measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis
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[PMID: 26642765] |
ML753286 has IC50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Bcrp KO (Abcg2−/−) and WT (Wistar) Rats[1]
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Dosage:25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV) (Pharmacokinetic Study)
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Administration:PO or IV; 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 hours
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Result:The tmax values in plasma were 1.4, 4.0, and 4.1 hours in Bcrp KO rats, WT rats pre-administered 25-mg/kg ML753286, and WT rats pre-administered 50-mg/kg ML753286, respectively.
Chemical Information
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No. CAS 1699720-89-2
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Appearance Solid
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Peso molecular 355.43
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Fòrmula C20H25N3O3
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Color White to off-white
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SMILES
COC1=CC=C2C(NC3=C2C[C@]4(N([C@H]3CC(C)C)C([C@@H](NC4=O)C)=O)[H])=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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566
Solvente y solubilidad
DMSO : 100 mg/mL (281.35 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: 2.5 mg/mL (7.03 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (7.03 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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 (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. 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 | 2.8135 mL | 14.0675 mL | 28.1349 mL | 70.3373 mL |
| 5 mM | 0.5627 mL | 2.8135 mL | 5.6270 mL | 14.0675 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8135 mL | 7.0337 mL | |
| 15 mM | 0.1876 mL | 0.9378 mL | 1.8757 mL | 4.6892 mL | |
| 20 mM | 0.1407 mL | 0.7034 mL | 1.4067 mL | 3.5169 mL | |
| 25 mM | 0.1125 mL | 0.5627 mL | 1.1254 mL | 2.8135 mL | |
| 30 mM | 0.0938 mL | 0.4689 mL | 0.9378 mL | 2.3446 mL | |
| 40 mM | 0.0703 mL | 0.3517 mL | 0.7034 mL | 1.7584 mL | |
| 50 mM | 0.0563 mL | 0.2813 mL | 0.5627 mL | 1.4067 mL | |
| 60 mM | 0.0469 mL | 0.2345 mL | 0.4689 mL | 1.1723 mL | |
| 80 mM | 0.0352 mL | 0.1758 mL | 0.3517 mL | 0.8792 mL | |
| 100 mM | 0.0281 mL | 0.1407 mL | 0.2813 mL | 0.7034 mL |
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