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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.

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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

Shanghai Luofa Biochemical Technology Co., Ltd.
Tel
021-51111890 15317326293
Email
sales@molnova.com
Country
China
ProdList
4196
Advantage
58
Guangzhou Tomums Life Science Co., Ltd.
Tel
020-31155029 18902330969
Fax
020-31155029
Email
sales@tomums.cn
Country
China
ProdList
4698
Advantage
58
Wuhan DKY Technology Co.,Ltd.
Tel
027-81302411 15377658509
Email
zs@dkybpc.com
Country
China
ProdList
2057
Advantage
58
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
021-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6013
Advantage
61
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
zhangsn@titansci.com
Country
China
ProdList
14113
Advantage
59
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2127
Advantage
70
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202 13764082696;
Email
info@hanhongsci.com
Country
China
ProdList
42982
Advantage
64
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32344
Advantage
50
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4647
Advantage
58
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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:


  • 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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