Elacridar

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的多药耐药 (MDR) 抑制剂，可完全逆转多药耐药 CHRC5、OV1/DXR 和 MCF7/ADR 细胞对多柔比星和长春新碱的细胞毒性，IC50 为 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 Cancer Phase 1 Discontinued(In Vitro):Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells.Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines.Elacridar (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells.(In Vivo):Elacridar (100 mg/kg; i.p. once) shows different distribution in brain and plasma.

Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells.Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines.Elacridar (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells. Cell Viability AssayCell Line:786-O cellsConcentration:2.5 and 5 μMIncubation Time:2 hoursResult:Dose-dependently inhibited cell viability of 786-O cells and showed better inhibitory effect with sunitnib addingWestern Blot AnalysisCell Line:MCF-7, Caki-1, and 786-O cell linesConcentration:5 μMIncubation Time:24 hoursResult: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 linesConcentration:5 μMIncubation Time:24 hoursResult:Dose-dependently increased 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells.

Elacridar (100 mg/kg; i.p. once) shows different distribution in brain and plasma.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 the dose.

GF-120918 | GW-0918 | GG-918

Membrane Transporter/Ion Channel

P-glycoprotein

P-gp?(P-glycoprotein)

Cancer

Breast Cancer

143664-11-3

563.6429

C34H33N3O5

>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

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

(-20℃)

With Ice Pack

≥ 2 years