GF120918 (Elacridar) is a very potent inhibitor of the ABC transporters (P-glycoprotein, P-gp) and BCRP. It reverses multidrug resistance at 0.02 to 0.1 µM in vitro. By blocking the activity of ABC transporter, GF120918 effectively increases the cellular concentration and subsequently increases the cytotoxicity of anti-tumor drugs. (1)
GF120918A has been used both in vitro and in vivo as a tool inhibitor of ABC transporters (or P-glycoprotein) to investigate the role of transporters in the disposition of various test molecules and to offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects. (2)
Technical information:
Chemical Formula: | C34H33N3O5 | |
CAS #: | 143664-11-3 | |
Molecular Weight: | 563.64 | |
Purity: | > 98% | |
Appearance: | white | |
Chemical Name: | N-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-5-methoxy-9-oxo-9,10-dihydroacridine-4-carboxamide | |
Solubility: | Up to 10 mM in DMSO | |
Synonyms: | GF120918, GF-120918, GG918, Elacridar |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Hyafil F et al., In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 1993;53(19):4595-602. Pubmed ID: 8402633 |
2. | Ward KW and Azzarano LM, Preclinical pharmacokinetic properties of the P-glycoprotein inhibitor GF120918A (HCl salt of GF120918, 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl]-4-acridine-carboxamide) in the mouse, rat, dog, and monkey. J Pharmacol Exp Ther. 2004;310(2):703-9. Pubmed ID: 15056727 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.