Tariquidar
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tariquidar是一种有效的P-糖蛋白(Pgp)抑制剂,非竞争性地抑制与Pgp相关的基础ATPase活性。P-糖蛋白是一个170-kDa的跨膜蛋白,作为药物外排泵将结构上不相关的化合物运出细胞。Tariquidar的化学结构包含叔胺、二甲基和酰胺基,有助于其对Pgp的抑制。三种不同模型的体外试验结果表明,tariquidar抑制Pgp,IC50范围介于15-223 nM之间。然而,在多药耐药相关蛋白介导的多药耐药性肿瘤细胞系中,tariquidar的抑制是Pgp特异性的,且效力减弱。
参考文献:
Fox E, Bates SE. Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor. Expert Rev Anticancer Ther. 2007 Apr;7(4):447-59.Bankstahl JP, Bankstahl M, Römermann K, Wanek T, Stanek J, Windhorst AD, Fedrowitz M, Erker T, Müller M, Löscher W, Langer O, Kuntner C. Tariquidar and elacridar are dose-dependently transported by P-glycoprotein and Bcrp at the blood-brain barrier: a small-animal positron emission tomography and in vitro study. Drug Metab Dispos. 2013 Apr;41(4):754-62. doi: 10.1124/dmd.112.049148. Epub 2013 Jan 10.
- 1. Aleksandra Filipiak-Duliban, Klaudia Brodaczewska, et al. "Spheroid Culture Differentially Affects Cancer Cell Sensitivity to Drugs in Melanoma and RCC Models." Int J Mol Sci. 2022 Jan 21;23(3):1166. PMID:35163092
- 2. Natalia Kasica, Piotr Jakubowski, et al. "P-Glycoprotein Inhibitor Tariquidar Plays an Important Regulatory Role in Pigmentation in Larval Zebrafish." Cells. 2021 Mar 20;10(3):690. PMID:33804686
- 3. Mohammadpour R, Safarian S, et al. "Comparative Endocytosis Mechanisms and Anticancer Effect of HPMA Copolymer- and PAMAM Dendrimer-MTCP Conjugates for Photodynamic Therapy." Macromol Biosci. 2016 Oct 25. PMID:27779358
- 4. Sajja, Ravi K., and Luca Cucullo. "Altered glycaemia differentially modulates efflux transporter expression and activity in hCMEC/D3 cell line." Neuroscience letters 598 (2015): 59-65. PMID:25982326
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 646.73 |
Cas No. | 206873-63-4 |
Formula | C38H38N4O6 |
Synonyms | XR9576, XR 9576, XR-9576,Tariquidar |
Solubility | insoluble in H2O; insoluble in EtOH; ≥16.17 mg/mL in DMSO |
Chemical Name | N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)OC)OC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
表达ABCB1的KB-3-1、KB-8-5-11、表达ABCC1的MCF-7、MCF-7/VP16和表达ABCG2的H460、H460/MX20 |
制备方法 |
该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
≥ 100 nM |
实验结果 |
浓度大于等于100 nM的tariquidar抑制P-gp和BCRP,但不抑制MRP1。在用100 nM和1 μM tariquidar处理的表达ABCB1的细胞中,荧光底物钙黄绿素AM的积累分别增加了14倍和19倍。100 nM浓度tariquidar抑制了大多数P-gp。在表达ABCG2的细胞中,相同浓度的tariquidar将荧光底物mitoxantrone的累积分别增加4倍(P < 0.001)和8倍(P < 0.001)。这些数据表明,tariquidar以相似的效力抑制两种转运蛋白,在100 nM时,其将P-gp的积累恢复到对照的56%,将BCRP的积累恢复到对照的84%。 在表达ABCC1的细胞中,Tariquidar不增加底物的累积。 |
动物实验: [2] | |
动物模型 |
NMRI nu/nu小鼠 |
给药剂量 |
口服, 每10g体重0.1 ml |
实验结果 |
ABCB1调节剂tariquidar影响paclitaxel在裸鼠中的分布。在大脑中,tariquidar与paclitaxel共同给药导致细胞抑制的脑浓度增加2.5至6.7倍。肝脏中,不同的ABCB1调节剂组和对照组之间没有显著的统计学差异。在肾脏中,肾脏中的paclitaxel含量降低至与对照组相似的浓度。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1] Kannan P, Telu S, Shukla S, et al. The “specific” P-glycoprotein inhibitor tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2). ACS chemical neuroscience, 2010, 2(2): 82-89. [2] Hubensack M, Müller C, H?cherl P, et al. Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice. Journal of cancer research and clinical oncology, 2008, 134(5): 597-607. |
描述 | Tariquidar(XR9576)是一种有效的和选择性的非竞争性P-糖蛋白抑制剂,Kd值为5.1 nM。 | |||||
靶点 | P-glycoprotein | |||||
IC50 | 5.1 nM (Kd) |
质量控制和MSDS
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