Efflux inhibitor-1
Based on 1 Customer Validation
Efflux inhibitor-1 is a pyrazolo[1,5-a]pyrimidine-based efflux inhibitor that inhibits the efflux activity of ABCG2 (IC50 = 0.45 µM) and ABCB1 (IC50 = 2.17 µM). Efflux inhibitor-1 can be used in research related to drug-resistant ovarian cancer and leukemia.
For research use only. We do not sell to patients.
- Purity : 99.74%
- CAS No.: 1776055-29-8
- Formula: C28H25N5O3
- Molecular Weight:479.53
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
IC50: 0.45 μM (ABCG2/BCRP), 2.17 μM (ABCB1)[1]
In Vitro
Efflux inhibitor-1 (compound 34) exhibits efflux inhibition of ABCG2 (IC50 = 0.45 µM) and ABCB1 (IC50 = 2.17 µM) in vitro, shows 4.8-fold selectivity (B1:G2) in CCRF-ADR 5000 (ABCB1) and Ig-MXP3 (ABCG2) cells, and demonstrates submicromolar chemosensitization with some toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1776055-29-8
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Appearance Solid
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Molecular Weight 479.53
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Formula C28H25N5O3
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Color Light yellow to yellow
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SMILES
COC1=CC=CC=C1C2=NN(C(N3CCN(C(C4=COC=C4)=O)CC3)=CC(C5=CC=CC=C5)=N6)C6=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (104.27 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. 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)
In Vivo:
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 (5.21 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.
In Vivo Dissolution Calculator
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (277 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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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 2.0854 mL | 10.4269 mL | 20.8538 mL | 52.1344 mL |
| 5 mM | 0.4171 mL | 2.0854 mL | 4.1708 mL | 10.4269 mL | |
| 10 mM | 0.2085 mL | 1.0427 mL | 2.0854 mL | 5.2134 mL | |
| 15 mM | 0.1390 mL | 0.6951 mL | 1.3903 mL | 3.4756 mL | |
| 20 mM | 0.1043 mL | 0.5213 mL | 1.0427 mL | 2.6067 mL | |
| 25 mM | 0.0834 mL | 0.4171 mL | 0.8342 mL | 2.0854 mL | |
| 30 mM | 0.0695 mL | 0.3476 mL | 0.6951 mL | 1.7378 mL | |
| 40 mM | 0.0521 mL | 0.2607 mL | 0.5213 mL | 1.3034 mL | |
| 50 mM | 0.0417 mL | 0.2085 mL | 0.4171 mL | 1.0427 mL | |
| 60 mM | 0.0348 mL | 0.1738 mL | 0.3476 mL | 0.8689 mL | |
| 80 mM | 0.0261 mL | 0.1303 mL | 0.2607 mL | 0.6517 mL | |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2085 mL | 0.5213 mL |
Efflux inhibitor-1 Related Classifications
HY-112505 Related Classifications
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