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Zosuquidar trihydrochloride

Catalog No. T6018 CAS 167465-36-3

Synonyms: Zosuquidar (LY335979) 3HCl, RS 33295-198 trihydrochloride, RS 33295-198 (D06387) 3HCl, Zosuquidar 3HCl, LY-335979 trihydrochloride

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

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Zosuquidar trihydrochloride Chemical Structure

Zosuquidar trihydrochloride, CAS 167465-36-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 40.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 90.00
50 mg	In stock	$ 378.00
1 mL * 10 mM (in DMSO)	In stock	$ 90.00

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Purity: 100%

Purity: 99.55%

Purity: 99.49%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
Targets&IC50	P-gp:60 nM(Ki)
In vitro	LY335979 competitively inhibits equilibrium binding of [3H]vinblastine to Pgp by blocking [3H]azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes. [1] LY335979 alone shows the cytotoxicity to drug-sensitive and MDR cell lines with IC50 ranging from 6 μM-16 μM and produces its ability to completely reverse the resistance of the oncolytics (vinblastine, doxorubicin, or etoposide) to the MDR cell lines P388/ADR, MCF7/ADR, 2780AD, or UCLA-P3.003VLB at concentration of 0.1 and 0.5 μM. [1] LY335979 significantly restores drug sensitivity in P-gp-expressing leukemia cell lines including K562/HHT40, K562/HHT90, K562/DOX and HL60/DNR, and enhances the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AML blasts with active P-gp. [2] A latest paper indicates that LY335979 completely inhibits apically directed transport of (Z)-endoxifen in the ABCB1-transduced cells. [3]
In vivo	Zosuquidar trihydrochloride is only moderately active as an inhibitor of P-gp at the blood-brain. Zosuquidar trihydrochloride at an oral dose of 25 mg/kg increases the brain concentrations by about 2.5-fold at 1 h and 5-fold at 24 h after paclitaxel administrationbarrier[4]. Zosuquidar enhances the brain uptake of nelfinavir in a dose-dependent manner. Brain tissue/plasma nelfinavir concentration ratios increase from 0.06±0.03 in the absence of zosuquidar administration and 0.09±0.02 between 2 and 6 h after a 2 mg/kg intravenous dose of zosuquidar to 0.85±0.19 after 6h and 1.58±0.67 after 20 mg/kg zosuquidar[5].
Kinase Assay	ATPase Assay : P-Glycoprotein ATPase activity is measured by the liberation of inorganic phosphate from ATP. The assay is measured in a 96-well plate for 90 min at 37 °C. Membranes (8 μg-10 μg protein) are incubated in a total volume of 100 μL of buffer A containing 5 mM sodium azide, 1 mM ouabain, 1 mM EGTA, 3 mM ATP, an ATP regenerating system composed of 5 mM phosphoenolpyruvate, and 3.6 units/mL pyruvate kinase in the presence and absence of 1 mM sodium vanadate. Pgp-ATPase activity is defined as the vanadate-sensitive portion of the total ATPase activity. Plates are read 3 minutes after the addition of the detection solution. The absorbance is measured at 690 nm by a microtiter dish reader. A phosphate standard curve is used to calculate the μMol of phosphate formed. Samples are measured in triplicate.
Cell Research	Cell viability is determined using a modified 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction method. Cells are harvested during logarithmic growth phase, and seeded in 96-well plates. The cells are then cultured for 72 hours in the presence of oncolytics with or without modulators. MCF-7 and MCF-7/ADR cells are incubated 24 hours before the addition of the drug with and without the LY335979. LY335979 is prepared as 2 mM DMSO stocks and added to wells to give final concentrations ranging from 0.05 to 5 μM. After 72 hours, 20 μL of freshly prepared 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (5 mg/mL in Dulbecco's PBS) is added to each well and incubated for 4 hours in a 37 °C incubator containing 5% CO2. Cells are pelleted in a Sorvall RT6000B centrifuge, 70 μL of medium is carefully removed from each well, and 100 μL of 2-propanol/0.04 N HC1 is added. Cells are resuspended 5-10 times with a Multipipettor or until no particulate matter is visible. Plates are immediately read on a Titertek Multiskan MCC/340 microplate reader Flow Laboratories with a test wavelength of 570 nm and a reference wavelength of 630 nm. Controls are measured in quadruplicate and modulators are measured in duplicate. Cytotoxicity analyses are also performed using the CeliTiter 96 AQueous assay kit.(Only for Reference)

Synonyms	Zosuquidar (LY335979) 3HCl, RS 33295-198 trihydrochloride, RS 33295-198 (D06387) 3HCl, Zosuquidar 3HCl, LY-335979 trihydrochloride
Molecular Weight	636.99
Formula	C32H31F2N3O2·3HCl
CAS No.	167465-36-3

Storage

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

Solubility Information

DMSO: 31.9 mg/mL (50 mM)

References and Literature

1. Dantzig AH, et al. Cancer Res. 1996, 56(18), 4171-4179. 2. Tang R, et al. BMC Cancer. 2008, 8,51. 3. Iusuf D, J Pharmacol Exp Ther. 2011, 337(3), 710-717. 4. Kemper EM, et al. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol. 2004 Feb;53(2):173-8. 5. Anderson BD, et al. Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats. Drug Metab Dispos. 2006 Apr;34(4):653-9.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-COVID-19 Compound Library Ion Channel Inhibitor Library Clinical Compound Library NO PAINS Compound Library

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Keywords

Zosuquidar trihydrochloride 167465-36-3 Membrane transporter/Ion channel Neuroscience P-gp LY335979 Trihydrochloride CEM/VLB100 Pgp 2780AD Multidrug resistance protein 1 Zosuquidar Zosuquidar (LY335979) 3HCl CD243 Zosuquidar (LY335979) anti-tumor activity RS 33295-198 trihydrochloride LY 335979 P388/ADR LY335979 RS 33295-198 (D06387) 3HCl P-glycoprotein UCLA-P3.003VLB 2780 RS 33295-198 (D06387) LY-335979 Trihydrochloride RS 33295-198 Zosuquidar 3HCl ABCB1 LY 335979 Trihydrochloride MCF7 acute myelogenous leukemia MDR1 HL60 UCLA-P3 Zosuquidar Trihydrochloride P388 MCF7/ADR LY-335979 trihydrochloride RS 33295-198 Trihydrochloride CCRF-CEM K562 LY-335979 Inhibitor Cluster of differentiation 243 AML inhibit inhibitor

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