Elacridar hydrochloride

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Cat.No. 4646 - Elacridar hydrochloride | C34H33N3O5.HCl | CAS No. 143851-98-3
Description: P-gp inhibitor
Alternative Names: GF 120918
Chemical Name: N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

P-glycoprotein (P-gp/ABCG1) inhibitor. Blocks P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs doxorubicin (Cat. No. 2252) and vincristine (Cat. No. 1257) in CHRC5 cells. Also inhibits breast cancer resistance protein (BCRP/ABCG2). Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data

M. Wt 600.1
Formula C34H33N3O5.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 143851-98-3
PubChem ID 170320
InChI Key IQOJZZHRYSSFJM-UHFFFAOYSA-N
Smiles O=C1C3=C(C(C(NC4=CC=C(CCN5CC(C=C(OC)C(OC)=C6)=C6CC5)C=C4)=O)=CC=C3)NC2=C1C=CC=C2OC.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 12 20

Preparing Stock Solutions

The following data is based on the product molecular weight 600.1. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.67 mL 8.33 mL 16.66 mL
5 mM 0.33 mL 1.67 mL 3.33 mL
10 mM 0.17 mL 0.83 mL 1.67 mL
50 mM 0.03 mL 0.17 mL 0.33 mL

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Hyafil et al (1993) In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 53 4595 PMID: 8402633

Myer et al (1999) The chemosensitizing potential of GF120918 is independent of the magnitude of P-glycoprotein-mediated resistance to conventional chemotherapeutic agents in a small cell lung cancer line. Oncol Rep. 6 217 PMID: 9864431


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Keywords: GF120918 P-glycoprotein P-gp inhibitors inhibits multidrug resistance MDR BCRP ABCG1 ABCG2 ABCB1 GF 120918 Multidrug Transporters

1 Citation for Elacridar hydrochloride

Citations are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:

Jablonski et al (2014) Inhibiting drug efflux transporters improves efficacy of ALS therapeutics. Ann Clin Transl Neurol 1 996 PMID: 25574474


Do you know of a great paper that uses Elacridar hydrochloride from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
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Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for Elacridar hydrochloride

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