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Elacridar hydrochloride
- GF 120918A
- Parent CAS: 143664-11-3
- Soluble in DMSO
- MF: C34H33N3O5.HCl
- MW: 600.1
Description
Elacridar hydrochloride (GF120918A) is an inhibitor of P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2), two major ATP-binding cassette drug efflux transporters.
Efflux transporters influence drug absorption, tissue penetration, blood-brain barrier permeability and multidrug resistance. Elacridar is used to increase intracellular drug retention and study transporter-mediated pharmacokinetics.
Key Features
- Dual P-gp/ABCB1 and BCRP/ABCG2 inhibitor
- Modulates ATP-dependent drug efflux
- Useful for blood-brain barrier and permeability studies
- Third-generation multidrug resistance transporter modulator
Applications
- Drug transporter inhibition assays
- Multidrug resistance reversal studies
- Blood-brain barrier penetration research
- Pharmacokinetic and drug-disposition models
More Information
| Parent CAS No. | 143664-11-3 |
|---|---|
| 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 hydrochloride |
| SMILES | C1=C2C(NC3=C(C2=O)C=CC=C3OC)=C(C(NC2=CC=C(CCN3CCC4=C(C3)C=C(OC)C(OC)=C4)C=C2)=O)C=C1.Cl |
| MFCD | MFCD11040791 |
| InChi | InChI=1S/C34H33N3O5.ClH/c1-40-28-9-5-7-26-32(28)36-31-25(33(26)38)6-4-8-27(31)34(39)35-24-12-10-21(11-13-24)14-16-37-17-15-22-18-29(41-2)30(42-3)19-23(22)20-37;/h4-13,18-19H,14-17,20H2,1-3H3,(H,35,39)(H,36,38);1H |
| InChiKey | IQOJZZHRYSSFJM-UHFFFAOYSA-N |
| CID | 170320 |
| Short Description | P-gp inhibitor |
References
- IELM Kuppens et al. A Phase I, Randomized, Open-Label, Parallel-Cohort, Dose-Finding Study of Elacridar (GF120918) and Oral Topotecan in Cancer Patients. Clin. Cancer Res. 2007, 13, 3276.
- M Hubensack et al. Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice. J.Cancer Res. Clin. Oncol. 2008, 134(5), 597-607.
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