Zosuquidar trihydrochloride (Synonyms: RS 33295-198 trihydrochloride; LY-335979 trihydrochloride)

Name: Zosuquidar trihydrochloride
Brand: MedChemExpress
SKU: HY-50671
Rating: 5.0 (16 reviews)

Cat. No.: HY-50671 Purity: 99.50%: Data Sheet
COA

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Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (K_i=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.

For research use only. We do not sell to patients.

CAS No. : 167465-36-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 16 publication(s) in Google Scholar

Other Forms of Zosuquidar trihydrochloride:

Zosuquidar In-stock
Zosuquidar trihydrochloride (Standard) Get quote

16 Publications Citing Use of MCE Zosuquidar trihydrochloride

Cell Proliferation/Viability Assay

Others

In Vivo Efficacy Study

: Zosuquidar trihydrochloride purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2021 Apr 15;13(4):559.; TPT (200 μM) accumulation after co-treatment with Zosuquidar (1 μM), Ko143 (1 μM), and the combination of both (1 μM each) in ADR and MX100 cells.

: Zosuquidar trihydrochloride purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2021 Apr 15;13(4):559.; Change in tumor volume after co-treatment of TPT with compounds 2 and LL347 versus TPT-only, vehicle-only, and positive controls (co-treatment with the combination of Zosuquidar (2 mg/kg) and Ko143) twice a week.

: Zosuquidar trihydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110506. [Abstract]; Effect of Mdr1 inhibitor Zosuquidar (LY, 2 μM) and control MRP1 inhibitor MK-571 (MK, 50 μM) on maraviroc accumulation in MDCKII-parental and MDCKII-MRP1 cells.

: Zosuquidar trihydrochloride purchased from MedChemExpress. Usage Cited in: Blood Adv. 2020 Oct 27;4(20):5062-5077. [Abstract]; HoxA9/Meis1 AML cells were treated with 10, 100, 500, and 1000 nM reserpine, tariquidar (Tari), or zosuquidar (Zosu), with or without Bir (200 nM), for 24 hours.

: Zosuquidar trihydrochloride purchased from MedChemExpress. Usage Cited in: J Pharm Biomed Anal. 2012 Jul;66:232-9. [Abstract]; Effect of pharmacological inhibition of drug efflux transporters on brain distribution of FLZ in rats. The rats receive 35 mg/kg FLZ via tail vein injection 10 min after intravenous administration of 20 mg/kg Zosuquidar or 7.5 mg/kg ko143.

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Description

IC₅₀ & Target

Ki: 59nM (P-glycoprotein)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	0.02 μM Compound: LY-335979	TP_TRANSPORTER: inhibition of Nelfinavir transepithelial transport (basal to apical) (Nelfinavir: 0.02 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Nelfinavir transepithelial transport (basal to apical) (Nelfinavir: 0.02 uM) in Caco-2 cells	[PMID: 10820137]
Caco-2	IC₅₀	0.024 μM Compound: LY-335979	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	[PMID: 10820137]
Caco-2	IC₅₀	0.05 μM Compound: LY-335979	TP_TRANSPORTER: inhibition of Indinavir transepithelial transport (basal to apical) (Indinavir: 0.05 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Indinavir transepithelial transport (basal to apical) (Indinavir: 0.05 uM) in Caco-2 cells	[PMID: 10820137]
Caco-2	IC₅₀	0.08 μM Compound: LY-335979	TP_TRANSPORTER: inhibition of Indinavir transepithelial transport (basal to apical) (Indinavir: 0.05 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Indinavir transepithelial transport (basal to apical) (Indinavir: 0.05 uM) in Caco-2 cells	[PMID: 10820137]

In Vitro

Zosuquidar (0.3 μM; 48 h) enhances the cytotoxicity of DNR (substrates for P-glycoproteins) in P-glycoproteins active cell lines^[2].
Zosuquidar (5-16 μM; 72 h) treatment alone shows high cytotoxic concentration to drug-sensitive and MDR cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[2]

Cell Line:	K562 and HL60 cells
Concentration:	0.3 μM
Incubation Time:	48 hours
Result:	Enhanced the cytotoxicity of DNR (substrates for P-glycoproteins) in K562/DOX cells more than 45.5-fold.

Cell Cytotoxicity Assay^[1]

Cell Line:	CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells
Concentration:	5-16 μM
Incubation Time:	72 hours
Result:	Showed IC₅₀s of 6, 7, 15, 8, 7, 15, 11, 16, >5, >5 μM for CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells, respectively.

In Vivo

Zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) treatment shows a significant increase in life span^[1].
Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice implanted with P388/ADR tumors^[1]
Dosage:	30, 10, 3, or 1 mg/kg
Administration:	Intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 days
Result:	Exihibited a significantly increased survival compared to the group treated with Doxorubicin alone (P<0.001).

Animal Model:	Mice implanted with P388 or P388/ADR murine leukemia cells^[1]
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; 30 mg/kg; once daily; 5 days
Result:	Observed significant antitumor activity against the MDR P388/ADR cell lines when mice were treated with a combined dose of 30 mg/kg LY335979 and 1 mg/kg Doxorubicin (P=0.1).

Molecular Weight

636.99

Formula

C₃₂H₃₄Cl₃F₂N₃O₂

CAS No.

167465-36-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

FC1([C@H]2[C@@H]1C3=C([C@@H](C4=CC=CC=C42)N5CCN(CC5)C[C@H](COC6=C7C=CC=NC7=CC=C6)O)C=CC=C3)F.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 20 mg/mL (31.40 mM; Need ultrasonic)

DMSO : 1 mg/mL (1.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5699 mL	7.8494 mL	15.6988 mL
5 mM	0.3140 mL	1.5699 mL	3.1398 mL
10 mM	0.1570 mL	0.7849 mL	1.5699 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

Zosuquidar is dissolved in 20% ethanol-saline^[5].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.50%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (254 KB) HNMR (281 KB) RP-HPLC (242 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. A H Dantzig, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9. [Content Brief]

[2]. Ruoping Tang, et al. Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML). BMC Cancer. 2008 Feb 13;8:51. [Content Brief]

[3]. Larry D Cripe, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. 2010 Nov 18;116(20):4077-85. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.5699 mL	7.8494 mL	15.6988 mL	39.2471 mL
H₂O	5 mM	0.3140 mL	1.5699 mL	3.1398 mL	7.8494 mL
	10 mM	0.1570 mL	0.7849 mL	1.5699 mL	3.9247 mL
	15 mM	0.1047 mL	0.5233 mL	1.0466 mL	2.6165 mL
	20 mM	0.0785 mL	0.3925 mL	0.7849 mL	1.9624 mL
	25 mM	0.0628 mL	0.3140 mL	0.6280 mL	1.5699 mL
	30 mM	0.0523 mL	0.2616 mL	0.5233 mL	1.3082 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Zosuquidar trihydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Zosuquidar trihydrochloride (Synonyms: RS 33295-198 trihydrochloride; LY-335979 trihydrochloride)

Customer Review

Other Forms of Zosuquidar trihydrochloride:

Zosuquidar trihydrochloride Related Antibodies

16 Publications Citing Use of MCE Zosuquidar trihydrochloride

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References

Customer Review

Zosuquidar trihydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Zosuquidar trihydrochloride Related Classifications

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