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Chemical Structure| 206873-63-4 Chemical Structure| 206873-63-4

Structure of Tariquidar
CAS No.: 206873-63-4

Chemical Structure| 206873-63-4

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Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM, reverses drug resistance in MDR cell Lines.

Synonyms: XR9576

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Product Details of Tariquidar

CAS No. :206873-63-4
Formula : C38H38N4O6
M.W : 646.73
SMILES Code : O=C(C1=CC2=CC=CC=C2N=C1)NC3=CC(OC)=C(OC)C=C3C(NC4=CC=C(CCN5CC6=C(C=C(OC)C(OC)=C6)CC5)C=C4)=O
Synonyms :
XR9576
MDL No. :MFCD09837824
InChI Key :LGGHDPFKSSRQNS-UHFFFAOYSA-N
Pubchem ID :148201

Safety of Tariquidar

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • P-gp

    P-gp, Kd:5.1 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
eIMS cells 100 nM 72 h Tariquidar restored BV sensitivity in BV-treated eIMS cells, significantly reducing the GI50 value. PMC7524717
S. mansoni adult worms 10 μM Enhance uptake and retention of TGR inhibitors, improving adult worm killing efficacy PMC10287695
NCI-ADR-RES cells 1 μM 72 h Restored the antiproliferative effect of LY3023414 in ABCB1-overexpressing NCI-ADR-RES cells PMC7606332
MDR19-HEK293 cells 1 μM 72 h Restored the antiproliferative effect of LY3023414 in ABCB1-overexpressing MDR19-HEK293 cells PMC7606332
Plasmodium yoelii NSRNT/ubp1::mCherry 100 nM 10 min Inhibition of MDR1 transport, increasing Fluo-4 accumulation in the parasite cytosol PMC10899652
Plasmodium yoelii NSSIP/ubp1::mCherry 100 nM 10 min Inhibition of MDR1 transport, decreasing Fluo-4 accumulation in the parasite cytosol PMC10899652

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice eIMS xenograft models oral 12 mg/kg twice weekly for 6 weeks Combination treatment with tariquidar and BV prolonged the survival of mice but only slightly slowed tumour growth. PMC7524717
Mice Plasmodium yoelii infected mouse model Intraperitoneal injection 12 mg/kg Once daily for four days Tariquidar in combination with antimalarial drugs significantly reduced parasitemia, reversing UBP1NT-mediated multidrug resistance PMC10899652

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01663545 - Completed - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT01547754 - Terminated - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT01386476 - Completed - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT00042315 Stage IIIb Non-small Cell Lung... More >> Cancer Stage IV Non-small Cell Lung Cancer Less << Phase 3 Terminated - -
NCT00042302 Stage IIIb Non-small Cell Lung... More >> Cancer Stage IV Non-small Cell Lung Cancer Less << Phase 3 Terminated - -
NCT00048633 Breast Neoplasms Phase 2 Completed - United States, Florida ... More >> Florida Oncology Associates Jacksonville, Florida, United States, 32207-5905 United States, Indiana Medical Center of Vincennes Vincennes, Indiana, United States, 47591 United States, Texas Arlington Cancer Center Arlington, Texas, United States, 76012 MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 Less <<
NCT00082368 Cancer Phase 2 Completed - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT00001944 Breast Cancer ... More >> Cancer Lung Cancer Ovarian Cancer Less << Phase 1 Completed - United States, Maryland ... More >> National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 Less <<
NCT00011414 Wilms' Tumor|Sarcoma|Adenaocor... More >>tical Carcinoma|Refractory Cancer|Coldrhood Cancer Less << PHASE1 COMPLETED 2016-01-13 National Institutes of Health ... More >>Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, 20892, United States Less <<
NCT00071058 Adrenal Cortex Neoplasms Phase 2 Completed - United States, Maryland ... More >> National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 Less <<
NCT00071058 - Completed - -
NCT00069160 Lung Neoplasms ... More >> Ovarian Neoplasms Cervix Neoplasms Renal Neoplasms Less << Phase 2 Completed - United States, Maryland ... More >> National Institutes of Health Bethesda, Maryland, United States, 20892 Less <<
NCT00082368 - Completed - -
NCT00069160 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.55mL

0.31mL

0.15mL

7.73mL

1.55mL

0.77mL

15.46mL

3.09mL

1.55mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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