Tariquidar (Synonyms: XR9576)

目录号: HY-10550 纯度: 99.45%: FAQs
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摩尔计算器

Tariquidar (XR9576) 是一种有效的特异性P-glycoprotein (P-gp)抑制剂，K_d 为 5.1 nM。

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Tariquidar Chemical Structure

CAS No. : 206873-63-4

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5 mg	￥453	In-stock
10 mg	￥780	In-stock
50 mg	￥2580	In-stock
100 mg	￥4600	In-stock
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Other Forms of Tariquidar:

Tariquidar methanesulfonate, hydrate In-stock
Tariquidar dimesylate 询价
Tariquidar dihydrochloride 询价

MCE 顾客使用本产品发表的 49 篇科研文献

: Tariquidar purchased from MCE. Usage Cited in: Eur J Med Chem. 2017 Feb 15;127:586-598. [Abstract]; Fluorescence ratio values in K562/DOX cells incubated with Rhd 123 in the absence (control) and in the presence of Verapamil (ver.) and Tariquidar (tar.) tested at 3.0 μM and 1.0 μM concentrations respectively.

: Tariquidar purchased from MCE. Usage Cited in: RSC Adv. 2016,6, 69083-69093.; Western blot analysis on MCF-7/ADR cells after being treated by (A) control (without treatment), (B) free DOX, (C) CMC/CaCO₃/DOX, (D) BCMC/CaCO₃/DOX, (E) CMC/CaCO₃/DOX/TQR, and (F) BCMC/CaCO₃/DOX/TQR for 24 h.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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]

细胞效力
(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]
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]
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	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	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	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	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	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]
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	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	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]

体外研究
(In Vitro)

Tariquidar (XR9576) 是 P-gp 介导的[³H]-Vinblastine 和[³H]-Paclitaxel 转运的有效调节剂，因为它增加了 P-gp 的稳态积累CH^rB30 细胞中的这些细胞毒性达到在不表达 P-gp 的 AuxB1 细胞中观察到的水平 (EC₅₀=487±50 nM)。[³H]-Tariquidar 以最高亲和力结合 CH^rB30 膜 (K_d=5.1±0.9 nM，n=7) 结合能力 (B_max) 为 275±15 pmol/mg 膜蛋白。与亲本细胞系相比，[³H]-长春碱的积累通过调节剂 Tariquidar (EC₅₀=487±50) 以剂量依赖性方式增加纳米)。MDR 调节剂 Tariquidar 能够抑制 60-70% 的钒酸盐敏感 ATPase 活性，有效的 IC₅₀ 值为 43±9 nM^[1]。Tariquidar (XR9576) 增强多种药物的细胞毒性，包括多柔比星、紫杉醇、依托泊苷和长春新碱；在 25 -80 nM XR9576 存在的情况下，可实现抗性的完全逆转。Tariquidar 是[³H]Azidopine 对 P-gp 进行光亲和标记的有效抑制剂，表明与蛋白质^[2]直接相互作用。

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

体内研究
(In Vivo)

在携带固有抗性 MC26 结肠肿瘤的小鼠中，联合使用 Tariquidar (XR9576) 可增强多柔比星的抗肿瘤活性，而不会显著增加毒性；在 2.5-4.0 mg/kg 静脉内或口服给药时观察到最大增强作用。此外，与 Tariquidar (6-12 mg/kg po) 共同给药可完全恢复紫杉醇、依托泊苷和长春新碱对两种高度耐药 MDR 人类肿瘤裸鼠异种移植物 (2780AD，H69/LX4) 的抗肿瘤活性。Tariquidar 还显著增强阿霉素对 (体内皮下注射) MC26 肿瘤的抗肿瘤活性^[2]。

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

Clinical Trial

分子量

646.73

Formula

C₃₈H₃₈N₄O₆

CAS 号

206873-63-4

性状

固体

颜色

Off-white to yellow

中文名称

他立喹达

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 16 mg/mL (24.74 mM; 超声助溶 (<60 ℃)；酸性条件溶解 (HCL 调节，pH=3) ; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

查看完整储备液配制表

* 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°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.87 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.45%

选择批次：

Data Sheet (657 KB) SDS (393 KB)

COA (293 KB) HNMR (237 KB) RP-HPLC (268 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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]

Tariquidar 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tariquidar206873-63-4XR9576他立喹达XR 9576XR-9576P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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Tariquidar (Synonyms: XR9576)

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Tariquidar (Synonyms: XR9576)

Customer Review

Other Forms of Tariquidar:

Tariquidar 相关抗体

MCE 顾客使用本产品发表的 49 篇科研文献

Tariquidar 相关产品

•相关化合物库:

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