Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewElacridar hydrochloride
Description: P-gp and BCRP 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)
Biological Activity for Elacridar hydrochloride
Elacridar hydrochloride is a P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) inhibitor. Elacridar hydrochloride blocks P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs doxorubicin (Cat. No. 2252) and vincristine (Cat. No. 1257) in CHRC5 cells. Orally active.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data for Elacridar hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Elacridar hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 12 | 20 |
Preparing Stock Solutions for Elacridar hydrochloride
The following data is based on the product molecular weight 600.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 8.33 mL | 41.66 mL | 83.32 mL |
| 1 mM | 1.67 mL | 8.33 mL | 16.66 mL |
| 2 mM | 0.83 mL | 4.17 mL | 8.33 mL |
| 10 mM | 0.17 mL | 0.83 mL | 1.67 mL |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets for Elacridar hydrochloride
References for Elacridar hydrochloride
References are publications that support the biological activity of the product.
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
Durmus et al (2012) Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Mol.Pharm. 9 3236 PMID: 23020847
If you know of a relevant reference for Elacridar hydrochloride, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: Elacridar hydrochloride, Elacridar hydrochloride supplier, GF120918, P-glycoprotein, P-gp, inhibitors, inhibits, multidrug, resistance, MDR, BCRP, ABCG2, ABCB1, GF, 120918, Multidrug, Transporters, 4646, Tocris Bioscience
4 Citations for Elacridar hydrochloride
Citations are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:
Lahmann et al (2015) Systemic Administration of Glibenclamide Fails to Achieve Therapeutic Levels in the Brain and Cerebrospinal Fluid of Rodents. PLoS One 10 e0134476 PMID: 26225433
Jablonski et al (2014) Inhibiting drug efflux transporters improves efficacy of ALS therapeutics. Ann Clin Transl Neurol 1 996 PMID: 25574474
Ramesh et al (2014) Pro-inflammatory human Th17 cells selectively express P-glycoprotein and are refractory to glucocorticoids. J Exp Med 211 89 PMID: 24395888
Terrance G et al (2019) Lower Tubulin Expression in Glioblastoma Stem Cells Attenuates Efficacy of Microtubule-Targeting Agents. ACS Pharmacol Transl Sci 2 402-413 PMID: 32259073
Do you know of a great paper that uses Elacridar hydrochloride from Tocris? Please let us know.
Reviews for Elacridar hydrochloride
Average Rating: 5 (Based on 1 Review.)
Have you used Elacridar hydrochloride?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Filter by:
1uM of elacridar is used to block the p glycoprotein.
By
Shashirekha Shamamandri Markandaiah on 10/29/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Endothelial cell, Astrocytes
Elacridar is used as P glycoprotein transporter blocker to enhance drug penetration in iPsc derived endothelial cell co cultured with ALS astrocytes.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.