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LY335979 (Zosuquidar 3HCL) Sale

(Synonyms: 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride) 目录号 : GC16609

A modulator of P-gp

LY335979 (Zosuquidar 3HCL) Chemical Structure

Cas No.:167465-36-3

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5mg
¥945.00
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10mg
¥1,440.00
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50mg
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100mg
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

ATPase assay

P-Glycoprotein ATPase activity was measured by the liberation of inorganic phosphate from ATP. The assay was measured in a 96-well plate for 90 mins at 37 °C. Membranes (8 ~ 10 μg protein) were 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 was defined as the vanadate-sensitive portion of the total ATPase activity. Plates were read 3 mins after the addition of the detection solution. The absorbance was measured at 690 nm by a microtiter dish reader. A phosphate standard curve was used to calculate the μmol of phosphate formed. Samples were measured in triplicate.

Cell experiment [1]:

Cell lines

CEM/VLB100, MCF-7/ADR, 2780AD, P388/ADR and UCLA-P3.003VLB cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.1 ~ 2 μM

Applications

LY335979 was an effective modulator, with maximal activity in reversing the sensitivity of resistant cells to the various anticancer drugs (Vinblastine, Doxorubicin, Btoposide and Taxol) at the concentrations of 0.1 ~ 2 μM. At the concentration of 0.05 μM, the modulator activity of LY335979 was diminished by about 50%.

Animal experiment [1]:

Animal models

Nude mice bearing UCLA-P3.003VLB tumor cells

Dosage form

30 mg/kg; i.p.

Applications

In a Pgp-expressing human non-small cell lung carcinoma xenograft model, the combination therapy of 20 mg/kg Taxol and 30 mg/kg LY335979 significantly suppressed solid tumor growth at days 12 and 19. In addition, no increased weight loss was observed.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

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

产品描述

LY335979 is a selective inhibitor of P-Gp with IC50 value of 1.2 nM [1, 2].

P-gp (P-glycoprotein) is a member of ATP-binding cassette (ABC) transporters and plays a pivotal role in pumping many foreign substances out of cells. It has been reported that abnormal expression of P-Gp is correlated with the multidrug resistance of tumor cells [3].

LY335979 is a potent P-Gp inhibitor and has a different selectivity with the reported P-Gp inhibitor cyclosporin A or verapamil. In drug-resistant cell line HL60/VCR with highly expression of P-Gp, LY335979 exhibited highly restore ability of P-Gp than cyclosporin A or verapamil and the IC 50 value of 1.2 nM [1]. When tested with a panel of cell lines over-expressed P-Gp (CEM/VLB100, MCF-7/ADR, 2780AD, P388/ADR, and UCLA-P3.003VLB), administration of LY335979 reversed the cells resistance to Vinblastine, Doxorubicin, Btoposide and Taxol by inhibiting P-Gp activity [2].

In female nude mice model with UCLA-P3.003VLB MDR tumor cells subcutaneous xenograft, pre-treated with LY335979 (30mg/kg) restored tumor cells sensitivity to Taxol (20 mg/kg) which combination markedly suppressed solid tumor growth compared with control group [2].

References:
1.  Green, L.J., P. Marder, and C.A. Slapak, Modulation by LY335979 of P-glycoprotein function in multidrug-resistant cell lines and human natural killer cells. Biochem Pharmacol, 2001. 61(11): p. 1393-9.
2.  Dantzig, A.H., et al., Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res, 1996. 56(18): p. 4171-9.
3.   Hu, T., et al., Reversal of P-glycoprotein (P-gp) mediated multidrug resistance in colon cancer cells by cryptotanshinone and dihydrotanshinone of Salvia miltiorrhiza. Phytomedicine, 2014. 21(11): p. 1264-72.

Chemical Properties

Cas No. 167465-36-3 SDF
别名 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride
化学名 (R)-1-(4-((1aR,6s,10bS)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c][7]annulen-6-yl)piperazin-1-yl)-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride
Canonical SMILES FC1([C@H](C2=CC=CC=C23)[C@@H]1C4=CC=CC=C4[C@H]3N5CCN(C[C@H](COC6=C7C(N=CC=C7)=CC=C6)O)CC5)F.Cl.Cl.Cl
分子式 C32H34Cl3F2N3O2 分子量 637.0
溶解度 ≥ 17.1mg/mL in DMSO 储存条件 Store at -20°C,unstable in solution, ready to use.
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.5699 mL 7.8493 mL 15.6986 mL
5 mM 0.314 mL 1.5699 mL 3.1397 mL
10 mM 0.157 mL 0.7849 mL 1.5699 mL
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