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Merck

SML0486

Sigma-Aldrich

Elacridar

≥98% (HPLC), powder, ABC transporters MDR-1 (P-gp) inhibitor

Sinónimos:

GF120918, GG918, GW0918, N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide

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About This Item

Fórmula empírica (notación de Hill):
C34H33N3O5
Número de CAS:
Peso molecular:
563.64
MDL number:
UNSPSC Code:
12161501
PubChem Substance ID:
NACRES:
NA.77

product name

Elacridar, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL (clear solution, warmed)

shipped in

wet ice

storage temp.

−20°C

SMILES string

COc1cccc2C(=O)c3cccc(C(=O)Nc4ccc(CCN5CCc6cc(OC)c(OC)cc6C5)cc4)c3Nc12

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)

InChI key

OSFCMRGOZNQUSW-UHFFFAOYSA-N

Application

Elacridar has been used:
  • as a chemical to decipher the link between autophagy and the mechanism of resistance to sunitinib
  • as an ATP-binding cassette sub-family B member 1 inhibitor to study its effects on the NSC23766 cytotoxicity
  • to treat rhodamine 123 (Rh123) labeled cells to set sorting gates in fluorescence-activated cell sorting (FACS)

Biochem/physiol Actions

GF120918 (Elacridar) is a very potent inhibitor of the ABC transporters MDR-1 (P-gp) and BCRP. GF120918 increases the bioavailability of cytotoxic anti-tumor drugs, and also leads to increased levels of anti-HIV drugs in the brain and CNS.

Features and Benefits

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Thomas Wanek et al.
European journal of nuclear medicine and molecular imaging, 39(1), 149-159 (2011-10-11)
One important mechanism for chemoresistance of tumours is overexpression of the adenosine triphosphate-binding cassette transporter P-glycoprotein (Pgp). Pgp reduces intracellular concentrations of chemotherapeutic drugs. The aim of this study was to compare the suitability of the radiolabelled Pgp inhibitors [(11)C]tariquidar
Tomoteru Yamasaki et al.
Nuclear medicine and biology, 38(5), 707-714 (2011-07-02)
Topotecan (TPT) is a camptothecin derivative and is an anticancer drug working as a topoisomerase-I-specific inhibitor. But TPT cannot penetrate through the blood-brain barrier. In this study, we synthesized a new positron emission tomography (PET) probe, [(11)C]TPT, to evaluate the
Resistance to sunitinib in renal clear cell carcinoma results from sequestration in lysosomes and inhibition of the autophagic flux
Giuliano S, et al.
Autophagy, 11(10), 1891-1904 (2015)
Ramola Sane et al.
Journal of pharmaceutical sciences, 102(4), 1343-1354 (2013-01-22)
The study objective was to develop a formulation of elacridar to overcome its dissolution-rate-limited bioavailability. Elacridar is a P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor that has been used to improve the brain distribution of drugs that are
Nico Holmstock et al.
Molecular pharmaceutics, 10(3), 1056-1062 (2013-01-31)
Rodent models are less suitable for predicting drug-drug interactions at the level of the human intestinal mucosa, especially when nuclear receptors such as pregnane X receptor (PXR) are involved. Recently, a transgenic mouse model, expressing both human PXR and CYP3A4

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