CAS |
143664-11-3 |
Chinese Name |
依克立达 |
English Name |
Elacridar |
Synonym |
依克立达;GF120918;GW0918;GG918;GF-120918; |
Unit |
Bottle |
Purity |
≥98% |
Molecular Formula |
C34H33N3O5 |
Molecular Weight |
563.64 |
Appearance |
Light yellow to yellow solid |
Storage |
Powder : 2-8℃, 2 years; In solvent(mother liquid): -20℃, 1 month; -80℃, 6 months |
Solubility |
Soluble in DMSO |
MDL |
MFCD00912604 |
EC |
EINECS 1532714-185-1 |
InChIKey |
OSFCMRGOZNQUSW-UHFFFAOYSA-N |
InChI |
InChI=1S/C34H33N3O5/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) |
PubChem CID |
119373 |
SMILES |
O=C1C2=CC=CC(C(NC(C=C3)=CC=C3CCN4CC(C=C(C(OC)=C5)OC)=C5CC4)=O)=C2NC6=C1C=CC=C6OC |
Description |
It is a potent inhibitor of P-glycoprotein and BCRP. |
Target Point |
P-gp(P-glycoprotein);BCRP |
Passage |
Membrane Transporter&Ion Channel |
Data Literature Source |
[1]. Tang SC, et al. 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
[2]. Hyafil F, et al. In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 1993 Oct 1;53(19):4595-602.
[3]. Sato H, et al. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells. Eur J Pharmacol. 2015 Jan 5;746:258-66.
[4]. Sane R, et al. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.
[5]. de Vries NA, et al. P-glycoprotein and breast cancer resistance protein: two dominant transporters working together in limiting the brain penetration of topotecan. Clin Cancer Res. 2007 Nov 1;13(21):6440-9. |
Specification |
5mg 10mM*1mL (in DMSO) 10mg |