Elacridar

Product Name: Elacridar
CAS No.: 143664-11-3
Chemical Name: Elacridar
Synonyms: GG 918;GW-918;CS-1717;GW 0918;GW120918;elacridar;GF 120918;EOS-62436;Elacridar, >=98%;Ecrita impurity 1
CBNumber: CB9855393
Molecular Formula: C34H33N3O5
Formula Weight: 563.64
MOL File: 143664-11-3.mol

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Elacridar Property

Melting point:: 216-218°C
Boiling point:: 701.6±60.0 °C(Predicted)
Density: 1.264±0.06 g/cm3(Predicted)
storage temp.: -20°C
solubility: DMSO: soluble2mg/mL (clear solution, warmed)
pka: 12.58±0.70(Predicted)
form: powder
color: white to beige
CAS DataBase Reference: 143664-11-3(CAS DataBase Reference)

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Safety

Safety Statements: 24/25
WGK Germany: 3
RTECS: AR7621300
HS Code: 29334900

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P273Avoid release to the environment.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0486
Product name: Elacridar
Purity: ≥98% (HPLC)
Packaging: 10mg
Price: $158
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML0486
Product name: Elacridar
Purity: ≥98% (HPLC)
Packaging: 50mg
Price: $631
Updated: 2024/03/01

TCI Chemical

Product number: E1371
Product name: Elacridar
Packaging: 25MG
Price: $241
Updated: 2024/03/01

TCI Chemical

Product number: E1371
Product name: Elacridar
Packaging: 100MG
Price: $727
Updated: 2024/03/01

Cayman Chemical

Product number: 18128
Product name: Elacridar
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

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Elacridar Chemical Properties,Usage,Production

Chemical Properties

Yellow Solid

Uses

A prototypical BCRP inhibitor. Inhibits the Bcrp1-mediated transport.

Uses

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)

Biological Activity

elacridar is a potent inhibitor of p-glycoprotein with ic50 values of 193 nm. [1]p-glycoprotein (permeability glycoprotein) is an important membrane protein. it pumps many foreign substances out of cells. p-glycoprotein belongs to the mdr/tap subfamily. p-glycoprotein is transmembrane glycoprotein which is about 170 kda. it is expressed in certain cell types primarily in the pancreas, liver, colon and kidney. it contains 6 transmembrane domains in the n-terminal half of the molecule. it also contains an atp-binding site in the large cytoplasmic domain. p-glycoprotein binds to the substrate at the cytoplasmic side of the protein. when atp binds to the cytoplasmic side, the substrate was excreted from the cell. p-glycoprotein can pump toxins or drugs back into the intestinal lumen, pumps them into bile ducts in liver cells.in some cancer cells, p-glycoprotein is overexpressed. it is involved in multidrug resistance of cancer cells.[2]elacridar can significantly inhibit the activity of p-glycoprotein at 1μm in mdckii cells which overexpress p-glycoprotein.[3] in the parental mdck-ii cells, elacridar at 5μm completely inhibit the polarized sunitinib transport.[4] elacridar did not inhibit the activity of several human cytochromep450 enzymes in vitro. the absolute bioavailability was about 0.47 and 1.3 respectively, when elacridar was given in the orally and microemulsion, intraperitoneally at 10 mg/kg in mice.[3] elacridar also can significantly increase sunitinib brain accumulation levels in mice at 10 mg/kg.[4]

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.

References

[1]. bankstahl jp, bankstahl m, romermann k, wanek t, stanek j, windhorst ad, fedrowitz m, erker t, muller m, loscher w et al: tariquidar and elacridar are dose-dependently transported by p-glycoprotein and bcrp at the blood-brain barrier: a small-animal positron emission tomography and in vitro study. drug metab dispos, 41(4):754-762.
[2]. aller sg, yu j, ward a, weng y, chittaboina s, zhuo r, harrell pm, trinh yt, zhang q, urbatsch il et al: structure of p-glycoprotein reveals a molecular basis for poly-specific drug binding. science 2009, 323(5922):1718-1722.
[3]. sane r, mittapalli rk, elmquist wf: development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. j pharm sci, 102(4):1343-1354.
[4]. tang sc, lagas js, lankheet na, poller b, hillebrand mj, rosing h, beijnen jh, schinkel ah: brain accumulation of sunitinib is restricted by p-glycoprotein (abcb1) and breast cancer resistance protein (abcg2) and can be enhanced by oral elacridar and sunitinib coadministration. int j cancer, 130(1):223-233.

Elacridar Preparation Products And Raw materials

Raw materials

Preparation Products

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Elacridar Suppliers

Americas 1 Canada 1 China 181 Europe 1 India 4 Japan 1 United Kingdom 5 United States 23 Global 217

LGM Pharma

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Target molecule Corp.

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View Lastest Price from Elacridar manufacturers

WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD

Product: Elacridar 143664-11-3
Price: US $0.00/KG
Min. Order: 100g
Purity: 98%+
Supply Ability: 100kg
Release date: 2020-10-21

Henan Aochuang Chemical Co.,Ltd.

Product: Elacridar 143664-11-3
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 1Ton
Release date: 2022-10-13

WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD

Product: Elacridar 143664-11-3
Price: US $0.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 1000g
Release date: 2020-11-03

143664-11-3, ElacridarRelated Search:

4-Methoxybenzyl alcohol (Trifluoromethoxy)benzene Anisole Phenyl salicylate Diphenyl ether Guaiacol Ethylparaben Diphenolic acid Pralmorelin p-Anisaldehyde 4-Methoxybenzyl cyanide Dimethoxymethane 4-Methoxyphenol DL-α-Tocopherol p-Anisidine PHENYL VALERATE ISOXADIFEN-ETHYL Ethyl acetate

elacridar

n-[4-[2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10h-acridine-4-carboxamide

GF 120918

GG 918

GW 0918

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

GF 120918;GF120918;GF-120918

GW-918

CS-1717

N-[4-[2-(3,4-Dihydro-6,7-diMethoxy-isoquinolin-2(1H)-yl)ethyl]phenyl]-9,10-dihydro-5-Methoxy-9-oxo-4-acridinecarboxaMide

1-{2-carbaMoyl-5-[2-(6,7-diMethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]phenyl}-5-Methoxy-9-oxo-9,10-dihydroacridine-4-carboxylic acid

GW 0918 N-[4-[2-(3,4-Dihydro-6,7-diMethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-Methoxy-9-oxo-4-acridinecarboxaMide

Elacridar (GF120918)

GW120918

Elacridar, >=98%

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-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-phenyl)-5-methoxy-9-oxo-9,10-dih

EOS-62436

Elacridar (GW0918)

Elacridar Elacridar

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

Elacridar USP/EP/BP

Ecrita impurity 1

N-(4-(2-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-5-methoxy-9-oxo-9,10-dihydroacridine-4-carb

143664-11-3

C34H33N3O5

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