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YHO-13177
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YHO-13177图片
CAS NO:912287-56-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
YHO-13177是高活性乳腺癌耐药蛋白多药转运通道(BCRP)抑制剂,可增强SN-38活性且对P-gp无作用。
生物活性

YHO-13177 is a potent and specific inhibitor ofBCRP; potentiated the cytotoxicity of SN-38 incancercells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells. IC50 value: Target:BCRP inhibitorin vitro: YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human coloncancerHCT116 (HCT116/BCRP) cells and SN-38–resistant human lungcancerA549 (A549/SN4) cells that expressBCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiated the cytotoxicity of SN-38 in human lungcancerNCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreaticcancerAsPC-1 cells that intrinsically expressedBCRP. In contrast, it had no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells and multidrug resistance-related protein 1–mediated doxorubicin resistance in MRP1-transfected human epidermoidcancerKB-3-1 cells. YHO-13177 increased the intracellular accumulation of Hoechst 33342, a substrate ofBCRP, at 30 minutes and partially suppressed the expression ofBCRPprotein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1]. in vivo: In mice, YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models [1].

分子量

370.47

性状

Solid

Formula

C20H22N2O3S

CAS 号

912287-56-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL(89.97 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6993 mL13.4964 mL26.9927 mL
5 mM0.5399 mL2.6993 mL5.3985 mL
10 mM0.2699 mL1.3496 mL2.6993 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。