Elacridar

SKU: orb1226281

Description

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.

Key Properties

• CAS Number: 143664-11-3
• MW: 563.6429
• Purity: >98% (HPLC)
• Formula: C₃₄H₃₃N₃O₅
• SMILES: COC1=CC=CC2=C1NC3=C(C2=O)C=CC=C3C(=O)NC4=CC=C(C=C4)CCN5CCC6=CC(=C(C=C6C5)OC)OC
• Target: P-glycoprotein
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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.
• 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. 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 lines. Concentration: 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 Assay Cell 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GF-120918 | GW-0918 | GG-918

Quick Database Links

Gene Symbol

P-glycoprotein