Name | ELACRIDAR |
Synonyms | GG 918 GW-918 GW 0918 GF120918 Elacridar elacridar ELACRIDAR GF-120918 GF 120918 n-[4-[2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10h-acridine-4-carboxamide N-{4-[2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl]phenyl}-5-methoxy-9-oxo-9,10-dihydroacridine-4-carboxamide N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide 4-acridinecarboxamide, N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo- |
CAS | 143664-11-3 |
EINECS | 1532714-185-1 |
InChI | InChI=1/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) |
Molecular Formula | C34H33N3O5 |
Molar Mass | 563.64 |
Density | 1.264±0.06 g/cm3(Predicted) |
Melting Point | 216-218°C |
Boling Point | 701.6±60.0 °C(Predicted) |
Flash Point | 378.1°C |
Solubility | Soluble in chloroform, dichloromethane, DMSO, and methanol. |
Vapor Presure | 1.57E-19mmHg at 25°C |
Appearance | powder |
Color | white to beige |
pKa | 12.58±0.70(Predicted) |
Storage Condition | -20°C |
Refractive Index | 1.644 |
MDL | MFCD00912604 |
Use | Elacridar(GF120918; GW0918) is a P-glycoprotein inhibitor and is often used as a tool compound in in vivo and in vitro experiments. |
In vitro study | Elacridar inhibition [elacridar (2.5 μm) significantly inhibited cell growth in Caki-1 and ACHN cells. Elacridar can inhibit the activity of P glycoprotein. The combined use of Elacridar and sunitinib significantly reduced the expression of ABC subfamily B molecule 2(ABCG2) in 786-O cells. |
In vivo study | In wild-type mice, elacridar (100 mg/kg, I. P.) and crizotinib orally administered in combination increased the concentration of crizotinib in plasma and brain tissue, and the brain-plasma ratio of crizotinib, with Abcb1a/1b; Abcg2 elacridar was injected intravenously (2.5 mg/kg) and intraperitoneally (100 mg/kg) in Flanders leukemia Virus stained B model mice. And after oral administration (100 mg/kg), the brain-plasma partition coefficients (Kp, brain) were 0.82, 0.43 and 4.31, respectively. In Mrp4(-/-) model mice, elacridar sufficiently inhibited P-glycoprotein-mediated topotecan transport, but had limited effect on bcrp1-mediated transport inhibition. |
Safety Description | 24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
RTECS | AR7621300 |
HS Code | 29334900 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.774 ml | 8.871 ml | 17.742 ml |
5 mM | 0.355 ml | 1.774 ml | 3.548 ml |
10 mM | 0.177 ml | 0.887 ml | 1.774 ml |
5 mM | 0.035 ml | 0.177 ml | 0.355 ml |
biological activity | Elacridar (GF120918, GW120918, GG918, GW0918) is an effective P-gp (MDR-1) and BCRP inhibitor. |
target | TargetValue P-gp BCRP |
Target | Value | in vitro study | Elacridar inhibition [in Caki-1 and ACHN cells, elacridar (2.5 μM) significantly inhibited cell growth. Elacridar can inhibit the activity of P glycoprotein. The combined use of Elacridar and sunitinib significantly reduced the expression of ABC subfamily B molecule 2(ABCG2) in 786-O cells. |
in vivo studies | in wild-type mice, elacridar (100 mg/kg, intraperitoneal injection) and crizotinib oral combined administration increases the concentration of crizotinib in plasma and brain tissue, and the crizotinib brain-plasma ratio, with Abcb1a/1b; abcg2 In Flanders leukemia virus-stained model B mice, after elacridar intravenous (2.5 mg/kg), intraperitoneal (100 mg/kg), and oral (100 mg/kg), the brain-plasma partition coefficients (Kp, brain) were 0.82, 0.43, and 4.31, respectively. In Mrp4(-/-) model mice, elacridar fully inhibited P glycoprotein-mediated topotecan transport, but had limited inhibitory effect on Bcrp1-mediated transport. |