P-gp inhibitor 1
Based on 1 Customer Validation
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
For research use only. We do not sell to patients.
- Purity: 98.79%
- CAS No.: 2050747-49-2
- Formula: C32H31N5O2
- Molecular Weight:517.62
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Anti-Cancer Compound Library
HY-L025
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Anti-Drug-Resistant Compound Library
HY-L169
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
P-glycoprotein[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
73.58 μM
Compound: 12k
|
Cytotoxicity against HUVEC assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against HUVEC assessed as reduction in cell viability after 48 hrs by MTT assay
|
[PMID: 28355069] |
| K562 | IC50 |
4 μM
Compound: 12k
|
Cytotoxicity against human K562 cells assessed as suppression of cell viability after 48 hrs by MTT assay
Cytotoxicity against human K562 cells assessed as suppression of cell viability after 48 hrs by MTT assay
|
[PMID: 28355069] |
| K562/A02 | IC50 |
12.78 μM
Compound: 12k
|
Cytotoxicity against human K562/A02 cells assessed as suppression of cell viability after 48 hrs by MTT assay
Cytotoxicity against human K562/A02 cells assessed as suppression of cell viability after 48 hrs by MTT assay
|
[PMID: 28355069] |
P-gp inhibitor 1 (12k) possesses high potency (EC50=57.9±3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells (1 μM, 80 minutes)[1].
P-gp inhibitor 1 also boosts the potency of other MDR-related cytotoxic agents with different structures, increases accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity in K562/A02 MDR cells (0.1, 1, 5 μM, 1 hour)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:K562/A02 cell
-
Concentration:0.1, 0.5, or 2.0 μM
-
Incubation Time:72 hours
-
Result:MDR reversal by 12k was not caused by a decreased protein expression but instead most likely due to direct inhibition of P-gp efflux[1].
Chemical Information
-
CAS No. 2050747-49-2
-
Appearance Solid
-
Molecular Weight 517.62
-
Formula C32H31N5O2
-
Color Light yellow to brown
-
SMILES
COC(C(OC)=C1)=CC2=C1CCN(C2)CCC3=CC=C(NC4=NC(C5=CC=NC=C5)=NC6=CC=CC=C46)C=C3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 16.67 mg/mL (32.21 mM; ultrasonic and warming and heat to 70°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 (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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (273 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[1]. Qiu Q, et al. Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. J Med Chem. 2017 Apr 27;60(8):3289-3302. [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 (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 | 1.9319 mL | 9.6596 mL | 19.3192 mL | 48.2980 mL |
| 5 mM | 0.3864 mL | 1.9319 mL | 3.8638 mL | 9.6596 mL | |
| 10 mM | 0.1932 mL | 0.9660 mL | 1.9319 mL | 4.8298 mL | |
| 15 mM | 0.1288 mL | 0.6440 mL | 1.2879 mL | 3.2199 mL | |
| 20 mM | 0.0966 mL | 0.4830 mL | 0.9660 mL | 2.4149 mL | |
| 25 mM | 0.0773 mL | 0.3864 mL | 0.7728 mL | 1.9319 mL | |
| 30 mM | 0.0644 mL | 0.3220 mL | 0.6440 mL | 1.6099 mL |
P-gp inhibitor 1 Related Classifications
HY-101791 Related Classifications
Powered by Bioz