CONTACT US
Home > Inhibitors/Agonists> > Tariquidar
Tariquidar

Tariquidar

  • CAT Number: I002592
  • CAS Number: 206873-63-4
  • Molecular Formula: C₃₈H₃₈N₄O₆
  • Molecular Weight: 646.73
  • Purity: ≥95%
Inquiry Now

Tariquidar（Cat No.:I002592）, also known as XR9576, is a potent and selective inhibitor of P-glycoprotein (P-gp), a drug efflux pump involved in multidrug resistance (MDR) in cancer cells. It exhibits a high affinity (Kd) of 5.1 nM for P-gp inhibition in the CHrB30 cell line. By blocking the activity of P-gp, Tariquidar effectively reverses drug resistance in MDR cell lines, enhancing the intracellular accumulation of chemotherapeutic drugs and increasing their efficacy.

Catalog Number I002592
CAS Number 206873-63-4
Synonyms

N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide

Molecular Formula

C₃₈H₃₈N₄O₆

Purity 95%
Target P-gp
Solubility in DMSO > 10 mM
Storage 2-8°C
IC50 5.1 nM (Kd)
IUPAC Name N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide
InChI InChI=1S/C38H38N4O6/c1-45-33-18-25-14-16-42(23-28(25)19-34(33)46-2)15-13-24-9-11-29(12-10-24)40-38(44)30-20-35(47-3)36(48-4)21-32(30)41-37(43)27-17-26-7-5-6-8-31(26)39-22-27/h5-12,17-22H,13-16,23H2,1-4H3,(H,40,44)(H,41,43)
InChIKey LGGHDPFKSSRQNS-UHFFFAOYSA-N
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
Reference

</br>1:Tariquidar sensitizes multiple myeloma cells to proteasome inhibitors via reduction of hypoxia-induced P-gp-mediated drug resistance. Muz B, Kusdono HD, Azab F, de la Puente P, Federico C, Fiala M, Vij R, Salama NN, Azab AK.Leuk Lymphoma. 2017 May 16:1-10. doi: 10.1080/10428194.2017.1319052. [Epub ahead of print] PMID: 28509582 </br>2:Preparation of multilocation reduction-sensitive core crosslinked folate-PEG-coated micelles for rapid release of doxorubicin and tariquidar to overcome drug resistance. Yi X, Zhao D, Zhang Q, Xu J, Yuan G, Zhuo R, Li F.Nanotechnology. 2017 Feb 24;28(8):085603. doi: 10.1088/1361-6528/aa5715. Epub 2017 Jan 5. PMID: 28055982 </br>3:Understanding the role of tariquidar, a potent Pgp inhibitor, in combination trials with cytotoxic drugs: What is missing? Srinivas NR.Cancer Chemother Pharmacol. 2016 Nov;78(5):1097-1098. Epub 2016 May 13. No abstract available. PMID: 27178178 </br>4:The reversal of multidrug resistance in ovarian carcinoma cells by co-application of tariquidar and paclitaxel in transferrin-targeted polymeric micelles. Zou W, Sarisozen C, Torchilin VP.J Drug Target. 2017 Mar;25(3):225-234. doi: 10.1080/1061186X.2016.1236113. Epub 2016 Oct 3. PMID: 27616277 </br>5:Whole-Body Distribution and Radiation Dosimetry of 11C-Elacridar and 11C-Tariquidar in Humans. Bauer M, Blaickner M, Philippe C, Wadsak W, Hacker M, Zeitlinger M, Langer O.J Nucl Med. 2016 Aug;57(8):1265-8. doi: 10.2967/jnumed.116.175182. Epub 2016 Apr 14. PMID: 27081167 </br>6:3D-QSAR AND CONTOUR MAP ANALYSIS OF TARIQUIDAR ANALOGUES AS MULTIDRUG RESISTANCE PROTEIN-1 (MRP1) INHIBITORS. Kakarla P, Inupakutika M, Devireddy AR, Gunda SK, Willmon TM, Ranjana KC, Shrestha U, Ranaweera I, Hernandez AJ, Barr S, Varela MF.Int J Pharm Sci Res. 2016 Feb;7(2):554-572. Epub 2016 Feb 1. PMID: 26913287 Free PMC Article</br>7:Image-Based Analysis to Predict the Activity of Tariquidar Analogs as P-Glycoprotein Inhibitors: The Importance of External Validation. Shayanfar S, Shayanfar A, Ghandadi M.Arch Pharm (Weinheim). 2016 Feb;349(2):124-31. doi: 10.1002/ardp.201500333. Epub 2015 Dec 28. PMID: 26708190 </br>8:Tariquidar Is an Inhibitor and Not a Substrate of Human and Mouse P-glycoprotein. Weidner LD, Fung KL, Kannan P, Moen JK, Kumar JS, Mulder J, Innis RB, Gottesman MM, Hall MD.Drug Metab Dispos. 2016 Feb;44(2):275-82. doi: 10.1124/dmd.115.067785. Epub 2015 Dec 10. PMID: 26658428 Free PMC Article</br>9:Mapping the Binding Site of the Inhibitor Tariquidar That Stabilizes the First Transmembrane Domain of P-glycoprotein. Loo TW, Clarke DM.J Biol Chem. 2015 Dec 4;290(49):29389-401. doi: 10.1074/jbc.M115.695171. Epub 2015 Oct 26. PMID: 26507655 Free PMC Article</br>10:Pharmacokinetic and pharmacodynamic study of tariquidar (XR9576), a P-glycoprotein inhibitor, in combination with doxorubicin, vinorelbine, or docetaxel in children and adolescents with refractory solid tumors. Fox E, Widemann BC, Pastakia D, Chen CC, Yang SX, Cole D, Balis FM.Cancer Chemother Pharmacol. 2015 Dec;76(6):1273-83. doi: 10.1007/s00280-015-2845-1. Epub 2015 Oct 20. PMID: 26486517

Request a Quote

Contact Us at MuseChem

We are committed to providing you with reliable, cost-effective solutions for your chemical needs, while ensuring your safety and comfort. Our team of experts is always available to answer your questions and help you navigate the complexities of the chemical industry.

Whether you're looking for a specific product or need help with a custom synthesis project, we're here to help you discover a new world of chemical possibilities. Contact us today to learn more about how we can assist you with all of your chemical needs.

Our goal is to make the process of ordering chemicals as seamless and hassle-free as possible. Let us know how we can assist you, and we'll get back to you as soon as possible. We look forward to hearing from you!