For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019562 |
| CAS Number | 2050747-49-2 |
| Synonyms | N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-2-pyridin-4-ylquinazolin-4-amine |
| Molecular Formula | C32H31N5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C32H31N5O2/c1-38-29-19-24-14-18-37(21-25(24)20-30(29)39-2)17-13-22-7-9-26(10-8-22)34-32-27-5-3-4-6-28(27)35-31(36-32)23-11-15-33-16-12-23/h3-12,15-16,19-20H,13-14,17-18,21H2,1-2H3,(H,34,35,36) |
| InChIKey | TXKOCTPGTLRGNL-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC4=NC(=NC5=CC=CC=C54)C6=CC=NC=C6)OC |
| Reference | [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. |
