Elacridar hydrochloride

Research use only, not for human use.

A potent inhibitor of multidrug resistance (MDR) that fully reverses multidrug resistance CHRC5, OV1/DXR and MCF7/ADR cells to the cytotoxicity of doxorubicin and vincristine with IC50 of 0.02 uM.

A potent inhibitor of multidrug resistance (MDR) that fully reverses multidrug resistance CHRC5, OV1/DXR and MCF7/ADR cells to the cytotoxicity of doxorubicin and vincristine with IC50 of 0.02 uM; effectively competes with [3H]azidopine for binding P-glycoprotein; restores sensitivity of the tumor to a single dose of doxorubicin in mice; orally bioavailable.Breast CancervPhase 1 Discontinued.

Elacridar hydrochloride (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells.Elacridar hydrochloride (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines.Elacridar hydrochloride (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells. Cell Viability Assay Cell Line:786-O cells Concentration:2.5 and 5 μM Incubation Time:2 hours Result:Dose-dependently inhibited cell viability of 786-O cells and showed better inhibitory effect with sunitnib adding.Western Blot Analysis Cell Line:MCF-7, Caki-1, and 786-O cell linesConcentration:5 μM Incubation Time:24 hours Result:Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells.Cell Viability AssayCell Line:MCF-7 and 786-O cell lines Concentration:5 μM Incubation Time:24 hours Result:Dose-dependently increased 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells.

Elacridar hydrochloride (100 mg/kg; i.p. once) shows different distribution in brain and plasma.Plasma Pharmacokinetic Parameters of Elacridar hydrochloride in mice.Animal Model:FVB wild-type mice Dosage:100 mg/kg Administration:Intraperitoneal injection; 100 mg/kg once Result:Showd a higher concertration in brain than plasma except at 4 h after administration.

GF-120918A

Membrane Transporter/Ion Channel

P-glycoprotein

P-glycoprotein

Cancer

Breast Cancer

143851-98-3

600.1039

C34H34ClN3O5

>98% (HPLC)

10 mM in DMSO

COC1=CC=CC2=C1NC3=C(C2=O)C=CC=C3C(=O)NC4=CC=C(C=C4)CCN5CCC6=CC(=C(C=C6C5)OC)OC.Cl

4-Acridinecarboxamide, N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years