| Identification | Back Directory | [Name]
P-gp inhibitor 1 | [CAS]
2050747-49-2 | [Synonyms]
P-gp inhibitor 1
4-Quinazolinamine, N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-2-(4-pyridinyl)- | [Molecular Formula]
C32H31N5O2 | [MDL Number]
MFCD31813605 | [MOL File]
2050747-49-2.mol | [Molecular Weight]
517.62 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 16.67 mg/mL (32.21 mM; ultrasonic and warming and heat to 70°C) | [form ]
Solid | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [Uses]
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. | [Biological Activity]
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
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]. | [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. |
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