WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 201190
CAS#: 143851-98-3 (HCl)
Description: Elacridar, also known as GF120918A, is a P-glycoprotein (P-gp) inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.
MedKoo Cat#: 201190
Name: Elacridar HCl
CAS#: 143851-98-3 (HCl)
Chemical Formula: C34H34ClN3O5
Exact Mass:
Molecular Weight: 600.11
Elemental Analysis: C, 68.05; H, 5.71; Cl, 5.91; N, 7.00; O, 13.33
Related CAS #: 143851-98-3 (Elacridar HCl) 143664-11-3 (Elacridar)
Synonym: GF120918; GF-120918; GF 120918; GF-120918A; GF120918A; GF 120918A; GG 918; D03968. Elacridar hydrochloride.
IUPAC/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.
InChi Key: IQOJZZHRYSSFJM-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: O=C(C(C=CC=C1C2=O)=C1NC3=C2C=CC=C3OC)NC4=CC=C(CCN5CC6=C(C=C(OC)C(OC)=C6)CC5)C=C4.[H]Cl
Related CAS#
143851-98-3 (Elacridar HCl); 143664-11-3 (Elacridar)
1: Sato H, Siddig S, Uzu M, Suzuki S, Nomura Y, Kashiba T, Gushimiyagi K, Sekine Y, Uehara T, Arano Y, Yamaura K, Ueno K. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells. Eur J Pharmacol. 2015 Jan 5;746:258-66. doi: 10.1016/j.ejphar.2014.11.021. Epub 2014 Nov 29. PubMed PMID: 25455500.
2: Hendrikx JJ, Lagas JS, Wagenaar E, Rosing H, Schellens JH, Beijnen JH, Schinkel AH. Oral co-administration of elacridar and ritonavir enhances plasma levels of oral paclitaxel and docetaxel without affecting relative brain accumulation. Br J Cancer. 2014 May 27;110(11):2669-76. doi: 10.1038/bjc.2014.222. Epub 2014 Apr 29. PubMed PMID: 24781280; PubMed Central PMCID: PMC4037831.
3: Chuan Tang S, Nguyen LN, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH. Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Int J Cancer. 2014 Mar 15;134(6):1484-94. doi: 10.1002/ijc.28475. Epub 2013 Oct 3. PubMed PMID: 24037730.
4: Pajeva IK, Sterz K, Christlieb M, Steggemann K, Marighetti F, Wiese M. Interactions of the multidrug resistance modulators tariquidar and elacridar and their analogues with P-glycoprotein. ChemMedChem. 2013 Oct;8(10):1701-13. doi: 10.1002/cmdc.201300233. Epub 2013 Aug 13. PubMed PMID: 23943604.
5: Bauer M, Karch R, Zeitlinger M, Stanek J, Philippe C, Wadsak W, Mitterhauser M, Jäger W, Haslacher H, Müller M, Langer O. Interaction of 11C-tariquidar and 11C-elacridar with P-glycoprotein and breast cancer resistance protein at the human blood-brain barrier. J Nucl Med. 2013 Aug;54(8):1181-7. doi: 10.2967/jnumed.112.118232. Epub 2013 Jul 5. PubMed PMID: 23833270; PubMed Central PMCID: PMC3882137.
6: Sane R, Agarwal S, Mittapalli RK, Elmquist WF. Saturable active efflux by p-glycoprotein and breast cancer resistance protein at the blood-brain barrier leads to nonlinear distribution of elacridar to the central nervous system. J Pharmacol Exp Ther. 2013 Apr;345(1):111-24. doi: 10.1124/jpet.112.199786. Epub 2013 Feb 8. PubMed PMID: 23397054; PubMed Central PMCID: PMC3608446.
7: Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci. 2013 Apr;102(4):1343-54. doi: 10.1002/jps.23450. Epub 2013 Jan 18. PubMed PMID: 23334925; PubMed Central PMCID: PMC3967790.
8: Bankstahl JP, Bankstahl M, Römermann K, Wanek T, Stanek J, Windhorst AD, Fedrowitz M, Erker T, Müller M, Löscher W, Langer O, Kuntner C. Tariquidar and elacridar are dose-dependently transported by P-glycoprotein and Bcrp at the blood-brain barrier: a small-animal positron emission tomography and in vitro study. Drug Metab Dispos. 2013 Apr;41(4):754-62. doi: 10.1124/dmd.112.049148. Epub 2013 Jan 10. PubMed PMID: 23305710.
9: Kallem R, Kulkarni CP, Patel D, Thakur M, Sinz M, Singh SP, Mahammad SS, Mandlekar S. A simplified protocol employing elacridar in rodents: a screening model in drug discovery to assess P-gp mediated efflux at the blood brain barrier. Drug Metab Lett. 2012 Jun 1;6(2):134-44. PubMed PMID: 23061481.
10: Sarisozen C, Vural I, Levchenko T, Hincal AA, Torchilin VP. Long-circulating PEG-PE micelles co-loaded with paclitaxel and elacridar (GG918) overcome multidrug resistance. Drug Deliv. 2012 Nov;19(8):363-70. doi: 10.3109/10717544.2012.724473. Epub 2012 Oct 3. PubMed PMID: 23030458.
