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

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

製品番号: HY-50671 純度: 99.50%: Data Sheet SDS COA 取扱説明書
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Technical Support

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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 167465-36-3

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 126	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 126	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$90	在庫あり	Estimated Time of Arrival: December 31
10 mg	$130	在庫あり	Estimated Time of Arrival: December 31
50 mg	$320	在庫あり	Estimated Time of Arrival: December 31
100 mg	$480	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 16 publication(s) in Google Scholar

Other Forms of Zosuquidar trihydrochloride:

Zosuquidar 在庫あり
Zosuquidar trihydrochloride (Standard) お問い合わせ

顧客検証

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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生物活性
純度とドキュメンテーション
参考文献
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製品説明

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]

体外実験

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.

体内実験

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).

分子量

636.99

分子式

C₃₂H₃₄Cl₃F₂N₃O₂

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

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

溶剤 & 溶解度

体外:

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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

Animal weight
(per animal)

Dosing volume
(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).

純度とドキュメンテーション

純度: 99.50%

Select Batch:

データシート (281 KB) SDS (393 KB)

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

取扱説明書 (2659 KB)

参考文献

[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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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)

カスタマーレビュー

Other Forms of Zosuquidar trihydrochloride:

Zosuquidar trihydrochloride 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Zosuquidar trihydrochloride 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Zosuquidar trihydrochloride Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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