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Elacridar

CAT: 0013-GTR19163223-04Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163223-04Size:25 mg
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Description
A potent inhibitor of multidrug resistance (MDR) that fully reverses multidrug resistance CHRC5, OV1/DXR and MCF7/ADR cells to the cytotoxicity of doxorubicin and vincristine with IC50 of 0.02 uM; effectively competes with [3H]azidopine for binding P-glycoprotein; restores sensitivity of the tumor to a single dose of doxorubicin in mice; orally bioavailable.Breast Cancer Phase 1 Discontinued (In Vitro) :Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells.Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines.Elacridar (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells. (In Vivo) :Elacridar (100 mg/kg; i.p. once) shows different distribution in brain and plasma.
CAS Number
143664-11-3
Product Name Alternative
GF-120918 | GW-0918 | GG-918
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
COC1=CC=CC2=C1NC3=C (C2=O) C=CC=C3C (=O) NC4=CC=C (C=C4) CCN5CCC6=CC (=C (C=C6C5) OC) OC
Molecular Formula
C34H33N3O5
Molecular Weight
563.6429
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
4-Acridinecarboxamide, N-[4-[2- (3,4-dihydro-6,7-dimethoxy-2 (1H) -isoquinolinyl) ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-

Chemical Information

Elacridar

Elacridar (GW120918) is an oral bioenhancer that targets multiple drug resistance in tumors. In many cases, the appearance of multidrug resistance in cancer is due to a change in expression of protein inhibitors. As of August 2007 elacridar was not listed on GSK's product pipeline. Development is assumed to have been discontinued.

CAS Number143664-11-3
PubChem CID119373
IUPAC NameN-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide
Molecular FormulaC34H33N3O5
Molecular Weight563.6
XLogP5.6
Topological Polar Surface Area89.1
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count7
Rotatable Bond Count8
Heavy Atom Count42
Formal Charge0
Complexity925
SMILES
COC1=CC=CC2=C1NC3=C(C2=O)C=CC=C3C(=O)NC4=CC=C(C=C4)CCN5CCC6=CC(=C(C=C6C5)OC)OC
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)
InChIKey
OSFCMRGOZNQUSW-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Elacridar
CAS: 143664-11-3
CID: 119373
Formula: C34H33N3O5
MW: 563.6
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight563.6
XLogP35.6
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count7
Rotatable Bond Count8
Exact Mass563.24202116
Monoisotopic Mass563.24202116
Topological Polar Surface Area89.1 Ų
Heavy Atom Count42
Formal Charge0
Complexity925
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

Alternative Products

CatalogName
FE22653-01Elacridar
A3385-10Elacridar hydrochloride
201190Elacridar HCl

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