Tariquidar

别名: XR9576

Tariquidar是一种有效的,选择性的,非竞争性P-glycoprotein抑制剂,在CHrB30细胞系中Kd为5.1 nM,作用于MDR细胞系逆转耐药性。Phase 3。

Tariquidar Chemical Structure

Tariquidar Chemical Structure

CAS: 206873-63-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1613.43 现货
10mg RMB 1415.55 现货
50mg RMB 3846.69 现货
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产品质控

批次: 纯度: 99.81%
99.5

Tariquidar相关产品

相关信号通路图

P-gp抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
KBV1 Function assay 1000 nM 72 hrs Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 487.57 +/- 30.54 nM), IC50=0.00905μM 27504669
OVCAR8 Function assay 1000 nM 72 hrs 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), IC50=0.00518μM 27504669
HEK293 Function assay 1000 nM 72 hrs 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), IC50=0.00495μM 27504669
KBV1 Function assay 1000 nM 72 hrs Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 277.68 +/- 56.61 nM), IC50=0.00066μM 27504669
KB-3-1 Function assay 1000 nM 72 hrs 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), IC50=0.00041μM 27504669
NCI-ADR-RES Function assay 1000 nM 72 hrs 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), IC50=0.01851μM 27504669
OVCAR8 Function assay 1000 nM 72 hrs 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), IC50=0.02373μM 27504669
HEK293 Function assay 1000 nM 72 hrs 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), IC50=0.02477μM 27504669
NCI-ADR-RES Function assay 1000 nM 72 hrs 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), IC50=0.02497μM 27504669
KBV1 Function assay 1000 nM 72 hrs Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.07 +/- 0.19 uM), IC50=0.07μM 27504669
OVCAR8 Function assay 1000 nM 72 hrs 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), IC50=0.08μM 27504669
KB-3-1 Function assay 1000 nM 72 hrs 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), IC50=0.11μM 27504669
NCI-ADR-RES Function assay 1000 nM 72 hrs 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), IC50=0.24μM 27504669
K562/A02 Function assay 5 uM 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 43.75 to 96.91 uM), IC50=1.97μM 28645831
KBV Function assay 10 uM 72 hrs Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=4.46μM 30384042
KBV Function assay 5 uM 72 hrs Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 5 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=5.24μM 30384042
K562/DOX Function assay 1 uM 10 mins Inhibition of P-gp in human K562/DOX cells assessed as increase in rhodamine-123 efflux in human K562 cells at 1 uM incubated for 10 mins hrs by flow cytometry relative to untreated control 28113128
A2780adr Function assay 10 uM 30 mins Inhibition of ABCB1 in human A2780adr cells assessed as increase in accumulation of calcein AM at 10 uM preincubated for 30 mins followed by calcein AM addition measured every 60 secs for 60 mins by fluorescence assay relative to control 29547272
HepG2 Function assay 10 uM 90 mins Inhibition of P-gp mediated efflux in adriamycin-resistant human HepG2 cells assessed as intracellular rhodamine-123 accumulation at 10 uM incubated in dark condition for 90 mins by flow cytometry relative to control 27328029
KB-3-1 Function assay 1000 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), IC50=0.00841μM 27504669
KB-V1 Function assay 200 nM Inhibition of P-gp in human KB-V1 cells assessed as increase in rhodamine 123 accumulation at 200 nM 21657271
MDCK Function assay 30 mins 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, EC50=0.01μM 23374872
CCRF-CEM/VCR1000 Function assay 240 secs Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50=0.03311μM 22452412
MDCK Function assay 30 mins 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, EC50=0.044μM 23374872
MDCK Function assay 30 mins Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay, EC50=0.044μM 24607999
EMT6/AR1.0 Function assay 1 hr Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay, IC50=0.064μM 18083034
EMT6/AR1.0 Function assay 1 hr Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay, IC50=0.06457μM 18083034
CEM/VLB500 Function assay 3 days Reversal of P-gp-mediated multidrug resistance to vinblastine in human CEM/VLB500 cells after 3 days by resazurin assay, EC50=0.068μM 17399990
A2780 Function assay 30 mins Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50=0.12589μM 18083034
Kb-V1 Function assay 10 mins Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay, IC50=0.223μM 21570282
KBV1 Function assay 10 mins Inhibition of ABCB1 in human KBV1 cells after 10 mins by Calcein-AM microplate assay, IC50=0.223μM 24900683
MCF7/Topo Function assay 2 hrs Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 microplate assay, IC50=0.526μM 24900683
MCF7/Topo Function assay 2 hrs Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 staining based fluorescence assay, IC50=0.526μM 30128080
HFE Cytotoxicity assay 72 hrs Cytotoxicity against human HFE cells assessed as cell viability after 72 hrs by MTT assay, IC50=1.28μM 26197160
K562/A02 Function assay 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 measured after 48 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=1.6μM 28645831
K562/A02 Function assay 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=3.02μM 28645831
K562/A02 Function assay 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 6 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=4.97μM 28645831
K562/A02 Function assay 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 12 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=8.28μM 28645831
HCT116 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay, IC50=12.5μM 26197160
MCF7/ADR Cytotoxicity assay 48 hrs Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=13.1μM 27328029
CEM/VLB500 Growth inhibition assay 3 days Growth inhibition of human CEM/VLB500 cells after 3 days by resazurin assay, GI50=13.5μM 17399990
K562/A02 Function assay 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 24 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=14.39μM 28645831
HLF Cytotoxicity assay 48 hrs Cytotoxicity against HLF cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=16.69μM 27328029
SW620 Cytotoxicity assay 48 hrs Cytotoxicity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM 26197160
SW620/AD300 Cytotoxicity assay 48 hrs Cytotoxicity against human SW620/AD300 cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM 26197160
CCD-18Co Cytotoxicity assay 48 hrs Cytotoxicity against human CCD-18Co cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM 26197160
K562/A02 Cytotoxicity assay 48 hrs Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=27.19μM 29631786
K562/A02 Cytotoxicity assay 48 hrs Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay, IC50=27.19μM 28645831
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=31.56μM 29631786
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=31.56μM 28645831
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=37.2μM 27328029
A2780 Function assay Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=0.07244μM 18678495
A2780/ADR Function assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50=0.078μM 19250834
A2780adr Function assay Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay, IC50=0.08μM 21354800
MDCK Function assay Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry, IC50=0.21μM 21354800
KBV1 Function assay Inhibition of ABCB1 in human KBV1 cells assessed as inhibition of calcein-AM efflux, IC50=0.22μM 26774038
KBv1 Function assay Inhibition of ABCB1 overexpressed in human KBv1 cells by flow cytometric-based calcein-AM efflux assay, IC50=0.223μM 19170519
MCF7/Topo Function assay Inhibition of ABCG2 in human MCF7/Topo cells by Hoechst 33342 assay, IC50=0.52μM 26774038
MCF7/Topo Function assay Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay, IC50=0.526μM 21570282
MCF7 MX Function assay Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50=0.68μM 19932960
MDCK Function assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50=0.85μM 19932960
MCF7/Topo Function assay Inhibition of ABCG2 overexpressed in human MCF7/Topo cells by flow cytometric-based mitoxantrone efflux assay, IC50=0.916μM 19170519
MDCK Function assay Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=0.94μM 21354800
MCF7 Function assay Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay, IC50=1.44544μM 18678495
MCF-7 MX Function assay Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=1.5μM 21354800
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
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生物活性

产品描述 Tariquidar是一种有效的,选择性的,非竞争性P-glycoprotein抑制剂,在CHrB30细胞系中Kd为5.1 nM,作用于MDR细胞系逆转耐药性。Phase 3。
靶点
P-gp [1]
(CHrB30 cells)
5.1 nM(Kd)
体外研究(In Vitro)
体外研究活性 Tariquidar高亲和力结合到P-gp,Bmax为275 pmol/mg。Tariquidar与P-gp底物Vinblastine 和 Paclitaxel非竞争性地相互作用。Tariquidar作用于CHrB30 细胞,增加这些细胞毒素的稳态积累,达到非P-gp表达的AuxB1细胞中观察的水平,EC50为487 nM。Tariquidar可以抑制 P-gp的对Vanadate敏感的ATPase活性,抑制达 60-70%,有效IC50值为43 nM。[1]Tariquidar高浓度时,可以抑制其他耐药机制。1 μM Tariquidar在体外,可以废除ABCG2(BCRP)介导的Camptothecins耐药性。[2]Tariquidar增强几种药物的细胞毒性,包括Doxorubicin, Paclitaxel, Etoposide, 和 Vincristine。处理具有内在耐药性的小鼠结肠癌细胞系MC26,Doxorubicin比0.1 μM Tariquidar (36 vs 7 nM)的IC50值低5倍。处理具有获得性化疗抗性的小鼠乳腺癌,人类小细胞肺癌,和和人类卵巢癌细胞系(EMT6/AR1.0, H69/LX4 和 2780 AD),Doxorubicin 比0.1 μM Tariquidar的IC50值低22-150倍。从培养系统除去Tariquidar后,P-gp的抑制作用持续23小时。[3]Tariquidar恢复Doxorubicin 和 Vinblastine作用于MCF7WT乳腺癌细胞系衍生的多细胞肿瘤球体模型的细胞毒性。[4]
激酶实验 稳态药物累积实验
AuxB1和 CHrB30细胞在12孔(24 mm)组织培养皿中生长至汇合,测量[3H]-Vinblastine 的稳态积累。加入0.1 μ Ci [3H]-Vinblastine 和未标记的Vinblastine开始累积,终浓度为100 nM 。使用 0.1 μ Ci[3H]-Paclitaxel 和未标记的药物测量[3H]-Paclitaxel的累积,终浓度为1 μM 。细胞在37°C下5% CO2环境中温育60分钟,达到稳态,反应体积为1 mL。在10-9-10-6 M浓度范围内 调查调节剂XR9576对[3H]-配体累积的影响。DMSO储存液中加入调节剂,最终溶剂浓度为0.2 %(v/v)。细胞收集后,通过液体闪烁计数和归一化细胞蛋白质含量测量累计的药物。
细胞实验 细胞系 小鼠乳腺癌细胞系MDR EMT6/AR1.0
浓度 ~100 nM Tariquidar
孵育时间 4 天
方法

细胞按每孔800个接种在含100 μL 培养基的96孔板中,在37°C下温育4小时。随后加入不同浓度的调节剂或溶剂对照(50μL/孔),再温育1小时,加入细胞毒性药物。加入细胞毒性药物(50μL),每孔按一式四份得到终浓度的范围。再温育4天 ,通过Sulforhodamine B实验测评贴壁细胞的细胞增殖。

实验图片 检测方法 检测指标 实验图片 PMID
Immunofluorescence MRP7 23393594
体内研究(In Vivo)
体内研究活性 Tariquidar(2-8 mg/kg 口服处理)显著增强Doxorubicin(5 mg/kg, 静脉注射)处理MC26小鼠结肠癌的抗肿瘤活性。Tariquidar和XR9576(6-12 mg/kg 口服处理)合用共处理人类移植瘤, 完全恢复Paclitaxel, Etoposide, 和Vincristine作用于两个高度抗MDR的人类移植瘤(2780AD, H69/LX4)的抗肿瘤活性。[3]
动物实验 Animal Models 携带结肠癌移植瘤MC26的小鼠
Dosages 8 mg/kg
Administration Tariquidar (口服处理)和Doxorubicin (5 mg/kg,静脉注射)共处理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01663545 Completed
Epilepsies Partial
National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC)
July 31 2012 --
NCT01547754 Terminated
HIV-Associated Cognitive Motor Complex
National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC)
January 9 2012 --
NCT01386476 Completed
Drug Resistance
National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC)
June 15 2011 --
NCT00082368 Completed
Cancer
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
May 16 2004 Phase 2

化学信息&溶解度

分子量 646.73 分子式

C38H38N4O6

CAS号 206873-63-4 SDF Download Tariquidar SDF
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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 8 mg/mL ( 12.36 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

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常见问题及建议解决方法

问题 1:
Can you please give me more specific and detailed information of how to dissolve and use this compound (S8028) for in vivo studies?

回答:
Tariquidar in 30% Propylene glycol, 5% Tween 80, 65% D5W at 30mg/ml will be a suspension or emulsion. If you are going to administrate the compound by oral gavage, it is fine. We also have test some vehicles for Tariquidar for i.p injection, and it is soluble in 5% DMSO+45% PEG 300+ddH2O at 2mg/ml clearly. When preparing the solution, please dissolve the compound in DMSO clearly first, then add PEG. After they mixed well, then dilute with water.

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