Cat. No.: HY-10550

Tariquidar

(Synonyms: XR9576)

57 Cited Publications

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Based on 57 publication(s) in Google Scholar

Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM).

For research use only. We do not sell to patients.

Purity: 99.45%
CAS No.: 206873-63-4
Formula: C₃₈H₃₈N₄O₆
Molecular Weight:646.73

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tariquidar Chemical Structure

CAS No.: 206873-63-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (57)
Solvent & Solubility
- In Vitro
- In Vivo
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Purity & Documentation
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Biological Activity

Description

Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM)^[1].

IC₅₀ & Target

Kd: 5.1 nM (P-gp)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780 ADR	IC₅₀	0.078 μM Compound: XR-9576	Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay	[PMID: 19250834]
A2780 ADR	IC₅₀	0.08 μM Compound: XR-9576	Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay	[PMID: 21354800]
CCD-18Co	IC₅₀	25 μM Compound: 25, Tariquidar, XR9576	Cytotoxicity against human CCD-18Co cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human CCD-18Co cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 26197160]
ECa-109 cell line	IC₅₀	36.5 nM Compound: TQ	Reversal of VCR -resistance in human Eca-109 cells assessed as vincristine IC50 by measuring cell viability incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM) Reversal of VCR -resistance in human Eca-109 cells assessed as vincristine IC50 by measuring cell viability incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)	[PMID: 36892076]
EMT6	IC₅₀	38 nM Compound: 2 (XR-9576)	Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0 Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0	[PMID: 10098671]
HCT-116	IC₅₀	12.5 μM Compound: 25, Tariquidar, XR9576	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 26197160]
HEK293	IC₅₀	1.52 nM Compound: Tariquidar	Chemo-sensitizing activity against human HEK293 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 2.29 +/-0.35 nM) Chemo-sensitizing activity against human HEK293 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 2.29 +/-0.35 nM)	[PMID: 34496204]
HEK293	IC₅₀	16.1 nM Compound: Tariquidar	Chemo-sensitizing activity against human HEK293 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 15.36 +/-6.18 nM) Chemo-sensitizing activity against human HEK293 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 15.36 +/-6.18 nM)	[PMID: 34496204]
HEK293	IC₅₀	2.55 nM Compound: Tariquidar	Chemo-sensitizing activity against human HEK293 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.67 +/-0.39 nM) Chemo-sensitizing activity against human HEK293 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.67 +/-0.39 nM)	[PMID: 34496204]
HEK293	IC₅₀	20.21 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human HEK293/MDR19 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 260 +/-74.23 nM) Chemo-sensitizing activity against ABCB1-overexpressing human HEK293/MDR19 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 260 +/-74.23 nM)	[PMID: 34496204]
HEK293	IC₅₀	24.77 nM Compound: Tariquidar	Inhibition of human ABCB1 transfected in HEK293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 504.65 +/- 44.94 nM) Inhibition of human ABCB1 transfected in HEK293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 504.65 +/- 44.94 nM)	[PMID: 27504669]
HEK293	IC₅₀	3.21 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human HEK293/MDR19 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 787.11 +/-227.51 nM) Chemo-sensitizing activity against ABCB1-overexpressing human HEK293/MDR19 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 787.11 +/-227.51 nM)	[PMID: 34496204]
HEK293	IC₅₀	4.24 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human HEK293/MDR19 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 1.31 +/-0.2 microM) Chemo-sensitizing activity against ABCB1-overexpressing human HEK293/MDR19 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 1.31 +/-0.2 microM)	[PMID: 34496204]
HEK293	IC₅₀	4.95 nM Compound: Tariquidar	Potentiation of doxorubicin-induced cytotoxicity against HEK293 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 5.28 +/- 0.74 nM) Potentiation of doxorubicin-induced cytotoxicity against HEK293 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 5.28 +/- 0.74 nM)	[PMID: 27504669]
HEK293	IC₅₀	7.62 nM Compound: Tariquidar	Effect on Colchicine-induced cytotoxicity against HEK293 cells by measuring colchicine IC50 at 1 uM after 72 hrs by CCK8 assay (Rvb = 8.42 +/- 3 nM) Effect on Colchicine-induced cytotoxicity against HEK293 cells by measuring colchicine IC50 at 1 uM after 72 hrs by CCK8 assay (Rvb = 8.42 +/- 3 nM)	[PMID: 32347726]
HEK-293T	IC₅₀	5.22 μM Compound: Tariquidar	Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36242992]
Hepatocyte	IC₅₀	25 μM Compound: 25, Tariquidar, XR9576	Cytotoxicity against rat hepatocytes assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against rat hepatocytes assessed as cell viability after 72 hrs by MTT assay	[PMID: 26197160]
HepG2	IC₅₀	37.2 μM Compound: Tariquidar	Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay	[PMID: 27328029]
HK-2	IC₅₀	8.03 μM Compound: Tqd	Cytotoxicity against human HK-2 cells assessed as cell survival measured after 72 hrs incubation by MTT assay Cytotoxicity against human HK-2 cells assessed as cell survival measured after 72 hrs incubation by MTT assay	[PMID: 38704938]
HUVEC	IC₅₀	40.26 μM Compound: Tqd	Cytotoxicity against HUVEC cells assessed as cell survival measured after 72 hrs incubation by MTT assay Cytotoxicity against HUVEC cells assessed as cell survival measured after 72 hrs incubation by MTT assay	[PMID: 38704938]
K562	IC₅₀	>100 μM Compound: Tari	Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
K562	IC₅₀	18.42 μM Compound: Tar	Cytotoxicity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 31202598]
K562	IC₅₀	31.56 μM Compound: Tariquidar	Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 29631786]
K562	IC₅₀	31.56 μM Compound: XR9576	Cytotoxicity against human K562 cells after 48 hrs by MTT assay Cytotoxicity against human K562 cells after 48 hrs by MTT assay	[PMID: 28645831]
K562/A02	IC₅₀	>100 μM Compound: Tari	Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
K562/A02	IC₅₀	27.19 μM Compound: Tariquidar	Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 29631786]
K562/A02	IC₅₀	27.19 μM Compound: XR9576	Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay	[PMID: 28645831]
K562/A02	IC₅₀	30.1 μM Compound: Tar	Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as cell growth inhibition after 48 hrs by MTT assay Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 31202598]
KB 3-1	IC₅₀	0.11 μM Compound: Tariquidar	Potentiation of doxorubicin-induced cytotoxicity against human KB-3-1 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.15 +/- 0.04 uM) Potentiation of doxorubicin-induced cytotoxicity against human KB-3-1 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.15 +/- 0.04 uM)	[PMID: 27504669]
KB 3-1	IC₅₀	0.41 nM Compound: Tariquidar	Potentiation of vincristine-induced cytotoxicity against human KB-3-1 cells assessed as vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.78 +/- 0.27 nM) Potentiation of vincristine-induced cytotoxicity against human KB-3-1 cells assessed as vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.78 +/- 0.27 nM)	[PMID: 27504669]
KB 3-1	IC₅₀	1.04 nM Compound: Tariquidar	Chemo-sensitizing activity against human KB 3-1 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 1.19 +/-0.39 nM) Chemo-sensitizing activity against human KB 3-1 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 1.19 +/-0.39 nM)	[PMID: 34496204]
KB 3-1	IC₅₀	11.53 nM Compound: Tariquidar	Chemo-sensitizing activity against human KB 3-1 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 13.78 +/-7.63 nM) Chemo-sensitizing activity against human KB 3-1 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 13.78 +/-7.63 nM)	[PMID: 34496204]
KB 3-1	IC₅₀	2.45 nM Compound: Tariquidar	Chemo-sensitizing activity against human KB 3-1 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.29 +/-0.75 nM) Chemo-sensitizing activity against human KB 3-1 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.29 +/-0.75 nM)	[PMID: 34496204]
KB 3-1	IC₅₀	8.41 nM Compound: Tariquidar	Potentiation of colchicine-induced cytotoxicity against human KB-3-1 cells assessed as colchicine IC50 at 1000 nM by MTT assay (Rvb = 8.81 +/- 3.80 nM) Potentiation of colchicine-induced cytotoxicity against human KB-3-1 cells assessed as colchicine IC50 at 1000 nM by MTT assay (Rvb = 8.81 +/- 3.80 nM)	[PMID: 27504669]
KB-V1	IC₅₀	14.95 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human KB-V1 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 758.22 +/-156.56 nM) Chemo-sensitizing activity against ABCB1-overexpressing human KB-V1 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 758.22 +/-156.56 nM)	[PMID: 34496204]
KB-V1	IC₅₀	2.13 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-expressing human KB-V1 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.73 +/-0.42 microM) Chemo-sensitizing activity against ABCB1-expressing human KB-V1 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.73 +/-0.42 microM)	[PMID: 34496204]
KB-V1	IC₅₀	2.22 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human KB-V1 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 1745 +/-293.01 nM) Chemo-sensitizing activity against ABCB1-overexpressing human KB-V1 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 1745 +/-293.01 nM)	[PMID: 34496204]
MCF7	IC₅₀	0.68 μM Compound: XR-9576	Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining	[PMID: 19932960]
MCF7	IC₅₀	1.5 μM Compound: XR-9576	Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining	[PMID: 21354800]
MCF7	IC₅₀	8.11 μM Compound: Tariquidar	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36242992]
MDCK	EC₅₀	0.01 μM Compound: Tariquidar	Activity at BCRP (unknown origin) expressed in MDCK cells using rhodamine 123 as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis Activity at BCRP (unknown origin) expressed in MDCK cells using rhodamine 123 as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis	[PMID: 23374872]
MDCK	EC₅₀	0.044 μM Compound: Tariquidar	Activity at MDR1 (unknown origin) expressed in MDCK cells using calcein AM as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis Activity at MDR1 (unknown origin) expressed in MDCK cells using calcein AM as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis	[PMID: 23374872]
MDCK	EC₅₀	0.044 μM Compound: Tariquidar	Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay	[PMID: 24607999]
MDCK	IC₅₀	>100 μM Compound: XR9576	Cytotoxicity against dog MDCK cells after 48 hrs by MTT assay Cytotoxicity against dog MDCK cells after 48 hrs by MTT assay	[PMID: 35247755]
MDCK	IC₅₀	0.21 μM Compound: XR-9576	Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry	[PMID: 21354800]
MDCK	IC₅₀	0.85 μM Compound: XR-9576	Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay	[PMID: 19932960]
MDCK	IC₅₀	0.94 μM Compound: XR-9576	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK-II	IC₅₀	>100 μM Compound: Tari	Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
MDCK-II	IC₅₀	83.64 μM Compound: Tari	Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
MDR	EC₅₀	16.3 nM Compound: 2 (XR-9576)	Potency tested against multidrug resistance (MDR) cell lines expressing P-gp (P-glycoprotein) Potency tested against multidrug resistance (MDR) cell lines expressing P-gp (P-glycoprotein)	[PMID: 10098671]
NCI/ADR-RES	EC₅₀	18.71 nM Compound: Tariquidar	Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity incubated for 48 hrs by MTT assay Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity incubated for 48 hrs by MTT assay	[PMID: 36242992]
NCI/ADR-RES	IC₅₀	0.048 μM Compound: Tariquidar	Reversal of P-gp mediated multidrug resistance in doxorubicin-resistant human MCF-7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs by CCK-8 assay (Rvb = 12.66 +/- 1.45 microM) Reversal of P-gp mediated multidrug resistance in doxorubicin-resistant human MCF-7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs by CCK-8 assay (Rvb = 12.66 +/- 1.45 microM)	[PMID: 38364715]
NCI/ADR-RES	IC₅₀	0.116 μM Compound: Tariquidar	Cytotoxicity against DOX-resistant human MCF7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs in presence of doxorubicin by CCK8 assay Cytotoxicity against DOX-resistant human MCF7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs in presence of doxorubicin by CCK8 assay	[PMID: 36645980]
NCI/ADR-RES	IC₅₀	0.23 μM Compound: Tariquidar	Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay	[PMID: 37229830]
NCI/ADR-RES	IC₅₀	0.24 μM Compound: Tariquidar	Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.54 +/- 0.60 uM) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.54 +/- 0.60 uM)	[PMID: 27504669]
NCI/ADR-RES	IC₅₀	1.24 μM Compound: Tariquidar	Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 10 uM incubated for 48 hrs by MTT assay Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 10 uM incubated for 48 hrs by MTT assay	[PMID: 36242992]
NCI/ADR-RES	IC₅₀	13.1 μM Compound: Tariquidar	Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay	[PMID: 27328029]
NCI/ADR-RES	IC₅₀	18.51 nM Compound: Tariquidar	Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 3714.80 +/- 383.58 nM) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 3714.80 +/- 383.58 nM)	[PMID: 27504669]
NCI/ADR-RES	IC₅₀	24.97 nM Compound: Tariquidar	Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM)	[PMID: 27504669]
NCI/ADR-RES	IC₅₀	31.9 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human NCI/ADR-RES cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 5.57 +/-0.96 microM) Chemo-sensitizing activity against ABCB1-overexpressing human NCI/ADR-RES cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 5.57 +/-0.96 microM)	[PMID: 34496204]
NCI/ADR-RES	IC₅₀	58.52 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human NCI/ADR-RES cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 2.63 +/-0.62 microM) Chemo-sensitizing activity against ABCB1-overexpressing human NCI/ADR-RES cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 2.63 +/-0.62 microM)	[PMID: 34496204]
NCI/ADR-RES	IC₅₀	6.82 nM Compound: Tariquidar	Chemo-sensitizing activity against ABCB1-overexpressing human NCI/ADR-RES cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 7.09 +/-0.89 microM) Chemo-sensitizing activity against ABCB1-overexpressing human NCI/ADR-RES cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 7.09 +/-0.89 microM)	[PMID: 34496204]
NCI/ADR-RES	IC₅₀	98.55 μM Compound: Tariquidar	Antiproliferative activity against human multidrug resistant NCI-ADR-RES cells overexpressing P-gp assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human multidrug resistant NCI-ADR-RES cells overexpressing P-gp assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36242992]
OVCAR-8	IC₅₀	0.08 μM Compound: Tariquidar	Potentiation of doxorubicin-induced cytotoxicity against human OVCAR8 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.12 +/- 0.03 uM) Potentiation of doxorubicin-induced cytotoxicity against human OVCAR8 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.12 +/- 0.03 uM)	[PMID: 27504669]
OVCAR-8	IC₅₀	2.61 nM Compound: Tariquidar	Chemo-sensitizing activity against human OVCAR-8 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.62 +/-0.31 nM) Chemo-sensitizing activity against human OVCAR-8 cells assessed as paclitaxel IC50 at 1 uM measured after 72 hrs in presence of paclitaxel by CCK8 assay (Rvb = 2.62 +/-0.31 nM)	[PMID: 34496204]
OVCAR-8	IC₅₀	23.73 nM Compound: Tariquidar	Potentiation of colchicine-induced cytotoxicity against human OVCAR8 cells assessed as colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 27.26 +/- 9.96 nM) Potentiation of colchicine-induced cytotoxicity against human OVCAR8 cells assessed as colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 27.26 +/- 9.96 nM)	[PMID: 27504669]
OVCAR-8	IC₅₀	28.46 nM Compound: Tariquidar	Chemo-sensitizing activity against human OVCAR-8 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 28.73 +/-10.04 nM) Chemo-sensitizing activity against human OVCAR-8 cells assessed as colchicine IC50 at 1 uM measured after 72 hrs in presence of colchicine by CCK8 assay (Rvb = 28.73 +/-10.04 nM)	[PMID: 34496204]
OVCAR-8	IC₅₀	4.62 nM Compound: Tariquidar	Chemo-sensitizing activity against human OVCAR-8 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 6.01 +/-0.77 nM) Chemo-sensitizing activity against human OVCAR-8 cells assessed as vincristine IC50 at 1 uM measured after 72 hrs in presence of vincristine by CCK8 assay (Rvb = 6.01 +/-0.77 nM)	[PMID: 34496204]
OVCAR-8	IC₅₀	5.18 nM Compound: Tariquidar	Potentiation of vincristine-induced cytotoxicity against human OVCAR8 cells assessed as vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 8.53 +/- 1.95 nM) Potentiation of vincristine-induced cytotoxicity against human OVCAR8 cells assessed as vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 8.53 +/- 1.95 nM)	[PMID: 27504669]
SW-620	IC₅₀	25 μM Compound: 25, Tariquidar, XR9576	Cytotoxicity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 26197160]
SW-620	IC₅₀	25 μM Compound: 25, Tariquidar, XR9576	Cytotoxicity against human SW620/AD300 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human SW620/AD300 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 26197160]

In Vitro

Tariquidar (XR9576) is a potent modulator of P-gp mediated [³H]-Vinblastine and [³H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CH^rB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC₅₀=487±50 nM). [³H]-Tariquidar binds to CH^rB30 membranes with the highest affinity (K_d=5.1±0.9 nM, n=7) and a binding capacity (B_max) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [³H]-Vinblastine is increased in a dose-dependent fashion by the modulators Tariquidar (EC₅₀=487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC₅₀ value of 43±9 nM^[1]. Tariquidar (XR9576) potentiates the cytotoxicity of several drugs including Doxorubicin, Paclitaxel, Etoposide, and Vincristine; complete reversal of resistance is achieved in the presence of 25-80 nM XR9576. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [³H]Azidopine implying a direct interaction with the protein^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar (XR9576) potentiates the antitumor activity of Doxorubicin without a significant increase in toxicity; maximum potentiation is observed at 2.5-4.0 mg/kg dosed either i.v. or p.o. In addition, coadministration of Tariquidar (6-12 mg/kg p.o.) fully restores the antitumor activity of Paclitaxel, Etoposide, and Vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. Tariquidar is found to also significantly potentiate the antitumor activity of doxorubicin against s.c. MC26 tumors in vivo^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 206873-63-4
Appearance Solid
Molecular Weight 646.73
Formula C₃₈H₃₈N₄O₆
Color Off-white to yellow
SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (57)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayWBCell Imaging/StainingFlow Cytometry

Sort by:

Journal Impact Factor

Cell

Prolonged sleep deprivation induces a cytokine-storm-like syndrome in mammals. [Abstract]

2023 Dec 7;186(25):5500-5516.e21. PMID: 38016470

Tariquidar purchased from MedChemExpress. Usage Cited in: Cell. 2023 Dec 7;186(25):5500-5516.e21. [Abstract]

Survival curves of mice under SD (SR means 48 h of recovery after SD) with i.p. administration of tariquidar (n = 5) or vehicle (n = 5).
Sci Bull

2016 Apr;61(7):552-560.
Cancer Res

Targeted KRASG12V Degradation in vivo Elicits Lung Adenocarcinoma Regression with Subsequent Relapse from Dysregulated Proteolysis. [Abstract]

2026 May 27:10.1158/0008-5472.CAN-25-5172. PMID: 42200804
Small

Active Transportation of Liposome Enhances Tumor Accumulation, Penetration, and Therapeutic Efficacy. [Abstract]

2020 Nov;16(44):e2004172. PMID: 33030305

Tariquidar purchased from MedChemExpress. Usage Cited in: Small. 2020 Nov;16(44):e2004172. [Abstract]

In vitro tumor penetration of the DOX-loaded liposomes in BxPC3 MTS. The BxPC3 MTS were prestained with or without a Pg-p inhibitor Tariquidar (10 nM) for 3 h. Subsequently, the MTS were cultured with DOX-loaded liposomes for 6 h. The MTS were visualized using CLSM in Z-stacks with 25 µm intervals. DOX (red).
J Control Release

Impact of P-gp and BCRP on pulmonary drug disposition assessed by PET imaging in rats. [Abstract]

2022 Sep:349:109-117. PMID: 35798092
J Control Release

PET imaging to assess the impact of P-glycoprotein on pulmonary drug delivery in rats. [Abstract]

2022 Feb:342:44-52. PMID: 34971693
Cell Death Discov

Compound 968 reverses adriamycin resistance in breast cancer MCF-7ADR cells via inhibiting P-glycoprotein function independently of glutaminase. [Abstract]

2021 Aug 5;7(1):204. PMID: 34354052

Tariquidar purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Aug 5;7(1):204. [Abstract]

MCF-7^ADR cells were treated with ADR (2μM) alone or together with Tariquidar (TQ; 0.5 μM) for 48h. Cell viability was detected using the CCK8 assays.
Antioxidants (Basel)

The Long-Term DEHP Exposure Confers Multidrug Resistance of Triple-Negative Breast Cancer Cells through ABC Transporters and Intracellular ROS. [Abstract]

2021 Jun 11;10(6):949. PMID: 34208283

Tariquidar purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]

Tariquidar (1.5 μM; 72 h). Western blotting results show the specific inhibition of both MRP1/ABCC1 and MDR1/ABCB1 after tariquidar treatment for 72 h in both control and DEHP-exposed MDA-MB-231 clones.

Tariquidar purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]

Tariquidar (1.5 μM; 2 h). Enhanced Dox accumulation was observed following 2 h of Tariquidar pretreatment in DEHP-exposed MDA-MB-231 clones #1 and #2, analyzed by a BD Accuri TW C6 flow cytometer.
Phytother Res

20(R)-Ginsenoside Rg3 Suppresses P-Glycoprotein-Mediated Multidrug Resistance in A549/Taxol Cells by Targeting MDM2-IκB-α Signaling Axis. [Abstract]

2026 Apr;40(4):1935-1950. PMID: 41630373
Commun Chem

Exploring bat-inspired cyclic tryptophan diketopiperazines as ABCB1 Inhibitors. [Abstract]

2024 Jul 13;7(1):158. PMID: 39003409
Eur J Med Chem

Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents. [Abstract]

2018 Mar 10:147:7-20. PMID: 29421572
Eur J Med Chem

N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy. [Abstract]

2017 Feb 15:127:586-598. PMID: 28113128
Pharmaceutics

Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression. [Abstract]

2021 Feb 26;13(3):306. PMID: 33652886
Mar Drugs

Stonikacidin A, an Antimicrobial 4-Bromopyrrole Alkaloid Containing L-Idonic Acid Core from the Northwestern Pacific Marine Sponge Lissodendoryx papillosa. [Abstract]

2024 Aug 30;22(9):396. PMID: 39330277
Mar Drugs

New Bioactive β-Resorcylic Acid Derivatives from the Alga-Derived Fungus Penicillium antarcticum KMM 4685. [Abstract]

2023 Mar 14;21(3):178. PMID: 36976227
Mar Drugs

New Marine Fungal Deoxy-14,15-Dehydroisoaustamide Resensitizes Prostate Cancer Cells to Enzalutamide. [Abstract]

2023 Jan 14;21(1):54. PMID: 36662227
Mar Drugs

New Guanidine Alkaloids Batzelladines O and P from the Marine Sponge Monanchora pulchra Induce Apoptosis and Autophagy in Prostate Cancer Cells. [Abstract]

2022 Nov 25;20(12):738. PMID: 36547885
Mar Drugs

Cytotoxic N-Methylpretrichodermamide B Reveals Anticancer Activity and Inhibits P-Glycoprotein in Drug-Resistant Prostate Cancer Cells. [Abstract]

2022 Sep 23;20(10):597. PMID: 36286421
Crit Rev Anal Chem

A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]

2022;52(7):1557-1571. PMID: 33691566
Int J Mol Sci

Stalling the Enemy: Targeting Nsp13 for Next-Generation SARS-CoV-2 Antivirals. [Abstract]

2026 Mar 11;27(6):2587. PMID: 41898448
Int J Mol Sci

Identification and Empiric Evaluation of New Inhibitors of the Multidrug Transporter P-Glycoprotein (ABCB1). [Abstract]

2023 Mar 10;24(6):5298. PMID: 36982374
Int J Mol Sci

Salvage Chemotherapy with Cisplatin, Ifosfamide, and Paclitaxel in Aggressive Variant of Metastatic Castration-Resistant Prostate Cancer. [Abstract]

2022 Nov 29;23(23):14948. PMID: 36499277
J Drug Deliv Sci Technol

May 2022, 103323.
Pharmaceuticals (Basel)

Functionalized Lipid Nanocarriers for Simultaneous Delivery of Docetaxel and Tariquidar to Chemoresistant Cancer Cells. [Abstract]

2023 Feb 24;16(3):349. PMID: 36986449
Eur J Pharmacol

Suppression of hypoxia-induced CAV1 autophagic degradation enhances nanoalbumin-paclitaxel transcytosis and improves therapeutic activity in pancreatic cancer. [Abstract]

2024 Apr 15:969:176431. PMID: 38395374
Eur J Pharm Sci

Population pharmacokinetic modeling to establish the role of P-glycoprotein on ciprofloxacin distribution to lung and prostate following intravenous and intratracheal administration to Wistar rats. [Abstract]

2019 Jan 15:127:319-329. PMID: 30423435
Hepatol Commun

Inhibition of the transmembrane transporter ABCB1 overcomes resistance to doxorubicin in patient-derived organoid models of HCC. [Abstract]

2024 May 2;8(5):e0437. PMID: 38696353
RSC Adv

2016,6, 69083-69093.
Mol Pharm

Pharmacokinetic Modeling of ( R)-[11C]verapamil to Measure the P-Glycoprotein Function in Nonhuman Primates. [Abstract]

2021 Jan 4;18(1):416-428. PMID: 33315404
J Cereb Blood Flow Metab

Complete inhibition of ABCB1 and ABCG2 at the blood-brain barrier by co-infusion of erlotinib and tariquidar to improve brain delivery of the model ABCB1/ABCG2 substrate [11C]erlotinib. [Abstract]

2021 Jul;41(7):1634-1646. PMID: 33081568
Mol Pharm

Pharmacokinetic Modeling of [18F]MC225 for Quantification of the P-Glycoprotein Function at the Blood-Brain Barrier in Non-Human Primates with PET. [Abstract]

2020 Sep 8;17(9):3477-3486. PMID: 32787277
Mol Pharm

Inhibition of ABCB1 and ABCG2 at the Mouse Blood-Brain Barrier with Marketed Drugs To Improve Brain Delivery of the Model ABCB1/ABCG2 Substrate [11C]erlotinib. [Abstract]

2019 Mar 4;16(3):1282-1293. PMID: 30694684
J Cereb Blood Flow Metab

Age dependency of cerebral P-glycoprotein function in wild-type and APPPS1 mice measured with PET. [Abstract]

2020 Jan;40(1):150-162. PMID: 30354871
J Cereb Blood Flow Metab

Regulation of P-glycoprotein expression in brain capillaries in Huntington's disease and its impact on brain availability of antipsychotic agents risperidone and paliperidone. [Abstract]

2016 Aug;36(8):1412-23. PMID: 26661162
Antimicrob Agents Chemother

Simultaneous Semimechanistic Population Analyses of Levofloxacin in Plasma, Lung, and Prostate To Describe the Influence of Efflux Transporters on Drug Distribution following Intravenous and Intratracheal Administration. [Abstract]

2015 Nov 30;60(2):946-54. PMID: 26621623
Pharm Res

Tumor Targeting Synergistic Drug Delivery by Self-Assembled Hybrid Nanovesicles to Overcome Drug Resistance. [Abstract]

2017 Jan;34(1):148-160. PMID: 27738951
Antiviral Res

Valspodar limits human cytomegalovirus infection and dissemination. [Abstract]

2021 Sep:193:105124. PMID: 34197862
ACS Chem Neurosci

Evaluation of [18F]F-CNBI and [18F]F-CNPI PET Probes in GSK-3β Transgenic Mice. [Abstract]

2025 Sep 3;16(17):3340-3353. PMID: 40815164
Sci Rep

New diterpenes from the marine sponge Spongionella sp. overcome drug resistance in prostate cancer by inhibition of P-glycoprotein. [Abstract]

2022 Aug 9;12(1):13570. PMID: 35945234
Sci Rep

LUCS (Light-Up Cell System), a universal high throughput assay for homeostasis evaluation in live cells. [Abstract]

2017 Dec 22;7(1):18069. PMID: 29273711
Langmuir

Self-assembled polymer/inorganic hybrid nanovesicles for multiple drug delivery to overcome drug resistance in cancer chemotherapy. [Abstract]

2015 May 12;31(18):5115-22. PMID: 25927163
J Nat Prod

Meroantarctines A-C, Meroterpenoids with Rearranged Skeletons from the Alga-Derived Fungus Penicillium antarcticum KMM 4685 with Potent p-Glycoprotein Inhibitory Activity. [Abstract]

2022 Dec 23;85(12):2746-2752. PMID: 36413729
Nucl Med Biol

A new method measuring the interaction of radiotracers with the human P-glycoprotein (P-gp) transporter. [Abstract]

2018 May:60:29-36. PMID: 29529532
PLoS One

RIPK2 induces docetaxel resistance in prostate cancer through the NF-κB/P-gp signaling pathway. [Abstract]

2026 Jan 21;21(1):e0341445. PMID: 41563982
J Nanopart Res

(2018) 20:176.
PLoS One

Inflammatory cytokine production in tumor cells upon chemotherapy drug exposure or upon selection for drug resistance. [Abstract]

2017 Sep 15;12(9):e0183662. PMID: 28915246
Mol Imaging Biol

SNAPshots of the MCHR1: a Comparison Between the PET-Tracers [18F]FE@SNAP and [11C]SNAP-7941. [Abstract]

2019 Apr;21(2):257-268. PMID: 29948643
Eur J Drug Metab Pharmacokinet

Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration. [Abstract]

2018 Oct;43(5):599-606. PMID: 29616423
Xenobiotica

The potential role of human multidrug resistance protein 1 (MDR1) and multidrug resistance-associated protein 2 (MRP2) in the transport of Huperzine A in vitro. [Abstract]

2020 Mar;50(3):354-362. PMID: 31132291
bioRxiv

2025 Sep 20.
bioRxiv

Development of PROTACs for targeted degradation of oncogenic TRK fusions. [Abstract]

2025 Jun 24:2025.06.18.660465. PMID: 40666929
Res Sq

2025 May 16.
Research Square Preprint

2024 Feb 6.
Research Square Print

2022 Jul.
RWTH Aachen University

2021 Oct.
Research Square Preprint

2021 Mar.
J Biomed Nanotechnol

Folate-Targeted Redox-Responsive Polymersomes Loaded with Chemotherapeutic Drugs and Tariquidar to Overcome Drug Resistance. [Abstract]

2018 Oct 1;14(10):1705-1718. PMID: 30041718

Solvent & Solubility

In Vitro:

DMSO : 16 mg/mL (24.74 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5462 mL

7.7312 mL

15.4624 mL

5 mM

0.3092 mL

1.5462 mL

3.0925 mL

10 mM

0.1546 mL

0.7731 mL

1.5462 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

Tariquidar is freshly prepared on each experimental day in 2.5% aqueous dextrose solution^[4].

Protocol 2

Tariquidar is dissolved in DMSO and adding heated 5% glucose solution (w/v) to a final DMSO concentration ≤ 2% (v/v)^[5].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

Cells (EMT6 AR1.0 8×10²/well; A2780 5×10³/well; 2780AD 6×10³/well) are seeded into 96-well plates. After ~4 h, varying concentrations of Tariquidar are added, and cells are incubated for an additional 4 days (EMT6 AR1.0) or 6 days (2780AD) before quantification of cell growth and calculation of IC₁₀ values (concentration resulting in 10% inhibition of cell growth)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
MC26 tumor slurry is implanted s.c. in BALB/c mice (day 0). The animals are then randomized, 24 h later, into groups of 15-18 and treated once with various regimens. Tariquidar or vehicle is administered either i.v. via a lateral tail vein or p.o. with Doxorubicin (5 mg/kg) or vehicle i.v. The modulator is administered either i.v. at 2-4 mg/kg (10 mL/kg) at the same time as Doxorubicin or p.o. at 2-8 mg/kg (10 mL/kg) 1 h before the Cytotoxic drug. GG918 is administered p.o. 1 h before doxorubicin. All of the animals are weighed twice weekly. The animals are killed by cervical dislocation on day 14, and the tumors are excised and weighed. The data are analyzed by Student’s t test.
Rats^[2]
Male CD rats (3 animals per time point) are dosed i.v. with paclitaxel alone [15 min infusion at 10 mg/kg in Tween 80:ethanol:5% dextrose (5:10:85% v/v/v)] or in combination with Tariquidar (10 mg/kg). Tariquidar is administered as a bolus (i.v.) dose 15 min before infusion of Paclitaxel. Blood samples are collected by cardiac puncture using heparinized syringes at various times between 0.083 and 48 h and are centrifuged to prepare plasma, which is stored at −20°C until analysis. Paclitaxel concentration in plasma samples is measured by a LC-MS/MS assay.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Martin C, et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol, 1999, 128(2), 403-411. [Content Brief]

[2]. Mistry P, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res, 2001, 61(2), 749-758. [Content Brief]

[3]. Zimmermann ES, et al. Simultaneous Semimechanistic Population Analyses of Levofloxacin in Plasma, Lung, and Prostate To Describe the Influence of Efflux Transporters on Drug Distribution following Intravenous and Intratracheal Administration. Antimicrob Agents Chemother. 2015 Nov 30;60(2):946-54. [Content Brief]

[4]. Kao YH, et al. Regulation of P-glycoprotein expression in brain capillaries in Huntington's disease and its impact on brain availability of antipsychotic agents risperidone and paliperidone. J Cereb Blood Flow Metab. 2016 Aug;36(8):1412-23. [Content Brief]

[5]. Matzneller P, et al. Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration. Eur J Drug Metab Pharmacokinet. 2018 Apr 3. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5462 mL	7.7312 mL	15.4624 mL	38.6560 mL
	5 mM	0.3092 mL	1.5462 mL	3.0925 mL	7.7312 mL
	10 mM	0.1546 mL	0.7731 mL	1.5462 mL	3.8656 mL
	15 mM	0.1031 mL	0.5154 mL	1.0308 mL	2.5771 mL
	20 mM	0.0773 mL	0.3866 mL	0.7731 mL	1.9328 mL

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Tariquidar

Anti-Infection Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Rare Diseases Drug Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Tariquidar

Biological Activity

Chemical Information

Publications (57)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tariquidar

Anti-Infection Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Rare Diseases Drug Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Tariquidar

Biological Activity

Chemical Information

Publications (57)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tariquidar Related Classifications

Cat. No.: HY-10550