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Elacridar

Catalog No. T2657 CAS 143664-11-3

Synonyms: GW0918, GW120918, GF120918, GG918

Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

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Elacridar, CAS 143664-11-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 35.00
10 mg	In stock	$ 57.00
25 mg	In stock	$ 109.00
50 mg	In stock	$ 198.00
100 mg	In stock	$ 297.00
200 mg	In stock	$ 497.00
500 mg	In stock	$ 793.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 100%

Purity: 99.62%

Purity: 99.32%

Purity: 99.15%

Purity: 99.08%

Purity: 99.04%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.
In vitro	In a study using FVB model mice stained with Friend leukemia virus, Elacridar was administered at doses of 2.5 mg/kg (intravenously), and 100 mg/kg both intraperitoneally and orally. This resulted in brain-to-plasma distribution coefficients (Kp, brain) of 0.82, 0.43, and 4.31, respectively. In wild-type mice, co-administration of Elacridar (100 mg/kg, intraperitoneally) and oral crizotinib significantly increased crizotinib concentrations in both plasma and brain tissue, enhancing the brain-to-plasma ratio of crizotinib to levels comparable with those in Abcb1a/1b; Abcg2-/- mice. Additionally, in Mrp4 (-/-) mice, Elacridar markedly inhibited the P-glycoprotein-mediated transport of topotecan, while it had minimal effect on Bcrp1-mediated transport.
In vivo	In Caki-1 and ACHN cells, Elacridar (2.5 μM) significantly inhibits cell growth and suppresses the activity of P-glycoprotein (P-gp). It inhibits the labeling of P-glycoprotein by [3H]azidopine (IC50: 0.16 μM). Additionally, when used in combination with sunitinib, Elacridar significantly reduces the expression of the ABC subfamily B member 2 in 786-O cells.
Kinase Assay	Photoaffinity radiolabeling of P-gp: 10 μL of unlabeled cell membrane suspension (at 0.4 mg of protein/mL) are aliquoted into each well in 96-well plates. 5 μL of GF120918 are then added to each well. The plate is incubated 25 min at 25℃ in the dark. 5 μL of tritiated azidopine (1.8 TBq/mmol) (0.6 μM in HCI 0.2 mM) are added to each well. After 25 min of incubation at 25℃ in the dark, samples are simultaneously irradiated for 2 min at 254 nm at 0℃ with a thin layer chromatography-designed UV lamp directly in contact with the plate. Samples are solubilized in sodium dodecyl sulfate-polyacrylamide gel electrophoresis sample buffer but not heated. After separation on a 7.5% polyacrylamide gel, the gel is treated for fluorography with Amplify and exposed during 3 days onto a photosensitive film. The fluorography is analysed using a Camag thin layer chromatography Scanner II densitometer.
Cell Research	3.0×103 cells per well are seeded in a 96-well plate. After 24 h incubation, an optimum concentration gradient of elacridar is added to each well. After culturing for 48 h, cell viability is assessed using the proliferation reagent, MTT. Control cells are treated with the vehicle only, 0.1% DMSO. After this ?nal incubation, the medium is aspirated and precipitated formazan crystals are dissolved in DMSO (100 μL/well). The absorbance of each well is measured at 540 nm, and a reference wavelength of 650 nm is read with a multiskan JX microplate reader. Cell viability is calculated as percentage of the control value. (Only for Reference)

Synonyms	GW0918, GW120918, GF120918, GG918
Molecular Weight	563.64
Formula	C34H33N3O5
CAS No.	143664-11-3

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 41 mg/mL (72.74 mM)

References and Literature

1. Tang SC, et al. Int J Cancer. 2014, 134(6), 1484-1494. 2. Hyafil F, et al. Cancer Res. 1993, 53(1), 4595-4602. 3. Sato H, et al. Eur J Pharmacol. 2015, 746, 258-266. 4. Sane R, et al. Drug Metab Dispos. 2012, 40(8), 1612-1619. 5. de Vries NA, et al. Clin Cancer Res. 2007, 13(21), 6440-6449.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library CNS-Penetrant Compound Library Bioactive Compounds Library Max

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Elacridar 143664-11-3 Membrane transporter/Ion channel Neuroscience BCRP P-gp Inhibitor Multidrug resistance protein 1 cancer CD243 P-glycoprotein GG 918 Breast cancer resistance protein GW-120918 inhibit 786-O GW0918 GF-120918 ABCG2 Pgp GW 0918 MCF-7 sunitinib ABCB1 GF 120918 GW120918 GF120918 GW 120918 MDR1 GW-0918 GG-918 GG918 Cluster of differentiation 243 inhibitor

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