Tariquidar (XR9576)

For research use only. Not for use in humans.

目录号：S8028

CAS No. 206873-63-4

Tariquidar (XR9576) 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K_d为5.1 nM，作用于MDR细胞系逆转耐药性。Phase 3。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1789.66	现货
10mg	RMB 1415.55	现货
50mg	RMB 3846.69	现货
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客户使用Selleck生产的Tariquidar (XR9576)发表文献31篇：

Nat Commun, 2021, 12(1):617

PubMed: 33504784 ( click the link to review the publication )

Front Oncol, 2021, 11:620907

PubMed: 33738259 ( click the link to review the publication )

Mol Syst Biol, 2020, 16(3):e9195

PubMed: 32187448 ( click the link to review the publication )

Cancers (Basel), 2020, 30;12(5) pii: E1123

PubMed: 32365878 ( click the link to review the publication )

Neurosurgery, 2020, 1;86(5):742-751

PubMed: 31225627 ( click the link to review the publication )

Sci Rep, 2020, 26;10(1):8671

PubMed: 32457334 ( click the link to review the publication )

Blood Adv, 2020, 4(20):5062-5077

PubMed: 33080008 ( click the link to review the publication )

J Clin Invest, 2019, 129(10):4377-4392

PubMed: 31498151 ( click the link to review the publication )

Cancer Res, 2019, 10.1158/0008-5472.CAN-18-1888

PubMed: 30630822 ( click the link to review the publication )

J Control Release, 2019, 317:67-77

PubMed: 31756395 ( click the link to review the publication )

Breast Cancer Res, 2019, 21(1):7

PubMed: 30654824 ( click the link to review the publication )

Mol Cancer Res, 2019, 17(11):2196-2207

PubMed: 31444231 ( click the link to review the publication )

Front Physiol, 2019, 10:616

PubMed: 31178753 ( click the link to review the publication )

Cancer Biol Ther, 2019, 10.1080/15384047.2019.1683324

PubMed: 31709896 ( click the link to review the publication )

Molecules, 2019, 24(3)

PubMed: 30717494 ( click the link to review the publication )

Oncogene, 2018, 37(2):208-217

PubMed: 28925391 ( click the link to review the publication )

Cell Chem Biol, 2018, 25(2):135-142

PubMed: 29276047 ( click the link to review the publication )

Sci Rep, 2018, 8(1):11429

PubMed: 30061701 ( click the link to review the publication )

Acta Pharmacol Sin, 2018, 39(6):1048-1063

PubMed: 29620050 ( click the link to review the publication )

Ann Biomed Eng, 2018, 46(6):899-911

PubMed: 29484528 ( click the link to review the publication )

Bioinformation, 2018, 587-593

PubMed: 31223218 ( click the link to review the publication )

Nat Chem Biol, 2017, 13(2):168-173

PubMed: 27918558 ( click the link to review the publication )

Toxicol In Vitro, 2017, 44:241-247

PubMed: 28746893 ( click the link to review the publication )

Leuk Lymphoma, 2017, 58(12):2916-2925

PubMed: 28509582 ( click the link to review the publication )
Int J Ophthalmol, 2017, 10(7):1055-1063

PubMed: 28730106 ( click the link to review the publication )

Oncotarget, 2017, 8(5):7678-7690

PubMed: 28032595 ( click the link to review the publication )

J Med Chem, 2016, 59(13):6353-69

PubMed: 27328029 ( click the link to review the publication )

Biochem Pharmacol, 2016, 101:40-53

PubMed: 26686578 ( click the link to review the publication )

Am J Transl Res, 2015, 7(6):1009-20

PubMed: 26279746 ( click the link to review the publication )

Vet Parasitol, 2015, 211(1-2):80-8

PubMed: 25986327 ( click the link to review the publication )

Mol Med Rep, 2015, 12(6):8093-100

PubMed: 26496964 ( click the link to review the publication )

产品安全说明书

P-gp抑制剂选择性比较

生物活性

产品描述

Tariquidar (XR9576) 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K_d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

Tariquidar高亲和力结合到P-gp，B_max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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
KB-3-1	M3XnRWZ2dmO2aX;uJIF{e2G7	MnvQNVAxOCCwTR?=	M2e2VlczKGi{cx?=	MUXQc5RmdnSrYYTpc44hd2ZidnnuZ5Jqe3SrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRk0{NTFiY3XscJMh[XO\|ZYPz[YQh[XNidnnuZ5Jqe3SrbnWgTWM2OCCjdDCxNFAxKG6PIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XliKGL2ZkA:KDBwN{igL{8uKDBwMkegcm0qNCCLQ{WwQVAvODByNEJOwG0>	NIrTZYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WwOFY3QSd-Mke1NFQ3Pjl:L3G+
KBV1	Mn;TSpVv[3Srb36gZZN{[Xl?	NXTqeJFZOTByMDDuUS=>	NUO4PVR1PzJiaILz	M4TqbGlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFQkGg[ZhxemW\|c3XkJIlvKEuEVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgdI91\W62aXH0bY9vKG:oII\pcoNzcXO2aX7lMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGK7IH3lZZN2emmwZzD2bY5kemm\|dHnu[UBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iMke3MlY5KCtxLTC1Ok43OSCwTTmsJGlEPTB;MD6wNFA3Ps7:TR?=	M17PTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
HEK293	MX7GeY5kfGmxbjDhd5NigQ>?	M{TpU\|ExODBibl2=	NHm1RZA4OiCqcoO=	MWXQc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOg[I95d3K3YnnjbY4hUUN3MDDheEAyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG\|c3H5JEhTfmJiPTC1MlI5KCtxLTCwMlc1KG6PKTygTWM2OD1yLkCwOFk2\|ryP	M3HWcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
OVCAR8	MUfGeY5kfGmxbjDhd5NigQ>?	NUPycmJNOTByMDDuUS=>	NH7IRlU4OiCqcoO=	NHvZdlNRd3SnboTpZZRqd25ib3[geolv[3Krc4TpcoUucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXkODUkigZ4VtdHNiYYPz[ZN{\WRiYYOgeolv[3Krc4TpcoUhUUN3MDDheEAyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmgLHJ3[iB;IEiuOVMhMy9vIEGuPVUhdk1rLDDJR\|UxRTBwMEC1NVjPxE1?	M4i5fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
KB-3-1	MUXGeY5kfGmxbjDhd5NigQ>?	NHPPTYYyODByIH7N		NHLtOFNRd3SnboTpZZRqd25ib3[gZ49t[2irY3nu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDNTNvMTDj[YxteyCjc4Pld5Nm\CCjczDjc4xkcGmlaX7lJGlEPTBiYYSgNVAxOCCwTTDifUBOXFRiYYPzZZkhMFK4YjC9JFgvQDFiKz:tJFMvQDBibl2pMEBKSzVyPUCuNFA5PDIQvF2=	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
KBV1	MYfGeY5kfGmxbjDhd5NigQ>?	MYCxNFAxKG6P	MXO3NkBpenN?	Mn3nTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO\|ZXSgbY4hU0KYMTDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZiY3;sZ4hq[2mwZT3pcoR2[2WmIHP5eI91d3irY3n0fUBjgSCvZXHzeZJqdmdiY3;sZ4hq[2mwZTDJR\|UxKGG2IEGwNFAhdk1iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSBqUo\iJF0hPDh5LkW3JEswNSB\|MD61OEBvVSluIFnDOVA:OC5yMEmwOe69VQ>?	MnniQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
MDCK	M1HaS2Z2dmO2aX;uJIF{e2G7		NHvzZnE{OCCvaX7z	NIDCTINC[3Srdnn0fUBifCCEQ2LQJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKE2GQ1ugZ4VtdHNidYPpcochemixZHHtbY5mKDF{MzDhd{B{fWK\|dILheIUhcW6ldXLheIVlKG[xcjCzNEBucW6\|IIDybY9zKHSxIIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB\|MDDtbY5{KGK7IH\seY9zd22ndILpZ{BidmGueYPpd{whTUN3ME2wMlAy\|ryP	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5NEi3Nkc,OjN\|N{S4O\|I9N2F-
NCI-ADR-RES	Mo\ySpVv[3Srb36gZZN{[Xl?	NXPn[VM{OTByMDDuUS=>	NXnSSm5HPzJiaILz	M{XxfGlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFQkGg[ZhxemW\|c3XkJIlvKE6FST3BSHIuWkWVIHPlcIx{KGG\|c3Xzd4VlKGG\|IIDveIVvfGmjdHnvckBw\iC4aX7jdol{fGmwZT3pcoR2[2WmIHP5eI91d3irY3n0fUBjgSCvZXHzeZJqdmdidnnuZ5Jqe3SrbnWgTWM2OCCjdDCxNFAxKG6PIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XliKGL2ZkA:KDN5MUSuPFAhMy9vIEO4N{42QCCwTTmsJGlEPTB;MD6wNVg2Oc7:TR?=	MneyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
OVCAR8	MoDUSpVv[3Srb36gZZN{[Xl?	MWWxNFAxKG6P	M3;ybVczKGi{cx?=	NEX0RplRd3SnboTpZZRqd25ib3[gZ49t[2irY3nu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUODDj[YxteyCjc4Pld5Nm\CCjczDjc4xkcGmlaX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB{Nz6yOkAsNy1iOT65OkBvVSluIFnDOVA:OC5yMkO3N:69VQ>?	M4Lsc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
HEK293	M37ycGZ2dmO2aX;uJIF{e2G7	MVuxNFAxKG6P	NELEdnQ4OiCqcoO=	MVrJcohq[mm2aX;uJI9nKGi3bXHuJGFDS0JzIITyZY5{\mWldHXkJIlvKEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{Bxd3SnboTpZZRqd25ib3[g[I95d3K3YnnjbY4ucW6mdXPl[EBkgXSxdH;4bYNqfHliYomgcYVie3W{aX7nJIRwgG:{dXLpZ4lvKEmFNUCgZZQhOTByMDDuUUBi\nSncjC3NkBpenNiYomgR2NMQCCjc4PhfUApWn[kIE2gOVA1NjZ3IDuvMUA1PC57NDDuUUktKEmFNUC9NE4xOjR5N988US=>	MnroQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
NCI-ADR-RES	MlnDSpVv[3Srb36gZZN{[Xl?	NFGxVJUyODByIH7N	MniyO\|IhcHK\|	M1PWUWlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFQkGg[ZhxemW\|c3XkJIlvKE6FST3BSHIuWkWVIHPlcIx{KGG\|c3Xzd4VlKGG\|IIDveIVvfGmjdHnvckBw\iClb3zjbIlkcW6nLXnu[JVk\WRiY4n0c5RwgGmlaYT5JIJ6KG2nYYP1dolv\yClb3zjbIlkcW6nIFnDOVAh[XRiMUCwNEBvVSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6KCiUdnKgQUAyPjB5LkWwJEswNSB2OUeuOFIhdk1rLDDJR\|UxRTBwMEK0PVfPxE1?	MlLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
CCRF-CEM/VCR1000	Mnu3SpVv[3Srb36gZZN{[Xl?		MYWyOFAhe2Wlcx?=	M4G4[mlvcGmkaYTpc44hd2ZiUD3ncJlkd3C{b4TlbY4udWWmaXH0[YQh\GG3bn;yeYJq[2mwIHXm[ox2gCCocn;tJIh2dWGwIFPDVmYuS0WPL2\DVlExODBiY3XscJMh[W[2ZYKgNlQxKHOnY4OgZpkhTkGFUzDmcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OC5yM{OxNe69VQ>?	NHnYcHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS1NlQyOid-MkK0OVI1OTJ:L3G+
MDCK	NVXpZ2VmTnWwY4Tpc44h[XO\|YYm=		NXfyc3Y5OzBibXnudy=>	M17ZT2FkfGm4aYT5JIF1KE2GUkGgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hVUSFSzDj[YxteyC3c3nu[{Bk[WylZXnuJGFOKGG\|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDNyIH3pcpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkh\my3b4LvcYV1emmlIHHuZYx6e2m\|LDDFR\|UxRTBwMES0{txO	M{DIUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{e0PFczLz5{M{O3OFg4OjxxYU6=
MDCK	MojxSpVv[3Srb36gZZN{[Xl?		M{PCflMxKG2rboO=	NXXKZ5J1UW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDNSGNMKGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCxZjDjZYxk\WmwLVHNJJRz[W6\|cH;yeEBi\nSncjCzNEBucW6\|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhTUN3ME2wMlA1PM7:TR?=	NYizNFNCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NFc6QTlpPkK0OlA4QTl7PD;hQi=>
EMT6/AR1.0	MU\GeY5kfGmxbjDhd5NigQ>?		M1PNSFEhcHJ?	M3TCTGlvcGmkaYTpc44hd2ZibX;1d4UhWGeyIHnuJGVOXDZxQWKxMlAh[2WubIOgZYZ1\XJiMTDodkBjgSCmYYXuc5J2[mmlaX6gZYNkfW23bHH0bY9vKGG\|c3H5MEBKSzVyPUCuNFY1\|ryP	NUDYOJR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwPFMxOzRpPkG4NFg{ODN2PD;hQi=>
EMT6/AR1.0	M1HuN2Z2dmO2aX;uJIF{e2G7		MnG4NUBpeg>?	MXXJcohq[mm2aX;uJI9nKG2xdYPlJHBoeCCrbjDFUXQ3N0GUMT6wJINmdGy\|IHHmeIVzKDFiaIKgZpkh\GG3bn;yeYJq[2mwIHHjZ5VufWyjdHnvckBie3OjeTygTWM2OD1yLkC2OFU4\|ryP	NUC3cmF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwPFMxOzRpPkG4NFg{ODN2PD;hQi=>
CEM/VLB500	NUDGb2dOTnWwY4Tpc44h[XO\|YYm=		MWCzJIRigXN?	MYLS[ZZmenOjbDDv[kBRNWeyLX3l[IlifGWmIH31cJRq\HK3ZzDy[ZNqe3SjbnPlJJRwKH[rbnLsZZN1cW6nIHnuJIh2dWGwIFPFUU9XVEJ3MECgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KHKnc3H6eZJqdiCjc4PhfUwhTUN3ME2wMlA3QM7:TR?=	NETXT5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{O5PVk6OCd-MUezPVk6QTB:L3G+
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CCD-18Co	MWXDfZRwfG:6aXPpeJkh[XO\|YYm=		Mnf4OFghcHK\|	MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDR2QuOTiFbzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI2\|ryP	Ml3iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOUexOlAoRjJ4MUm3NVYxRC:jPh?=
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K562/A02	NFLI[4dEgXSxdH;4bYNqfHliYYPzZZk>		MUW0PEBpenN?	NYfnXm4yS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4Mj;BNFIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{Nz6xPe69VQ>?	M3rUZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkS1PFMyLz5{OE[0OVg{OTxxYU6=
K562	M4jmNWN6fG:2b4jpZ4l1gSCjc4PhfS=>		M3;5e\|Q5KGi{cx?=	M4P6WmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OzFwNUdOwG0>	NFPISpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[zNVc5Pid-Mkm2N\|E4QDZ:L3G+
K562	Mk\1R5l1d3SxeHnjbZR6KGG\|c3H5		NX3B[I5GPDhiaILz	M2foTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2zNU42Ps7:TR?=	M2TJUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkS1PFMyLz5{OE[0OVg{OTxxYU6=
HepG2	M2Htb2N6fG:2b4jpZ4l1gSCjc4PhfS=>		Ml7kOFghcHK\|	MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBi\HKrYX35Z4lvNXKnc3nzeIFvfCCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVM4NjMQvF2=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN{OECyPUc,Ojd\|MkiwNlk9N2F-
KB-V1	MlfMSpVv[3Srb36gZZN{[Xl?	M4[2dFIxOCCwTR?=		MYXJcohq[mm2aX;uJI9nKFBvZ4CgbY4hcHWvYX6gT2IuXjFiY3XscJMh[XO\|ZYPz[YQh[XNiaX7jdoVie2ViaX6gdohw\GGvaX7lJFEzOyCjY3P1cZVt[XSrb36gZZQhOjByIH7N	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3N{K3NUc,OjF4NUeyO\|E9N2F-
SK-N-MC	MorxdWhVWyCjc4PhfS=>			Mmi5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO=	NVfGbZR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH	M{DWZpFJXFNiYYPzZZk>			NHrQNWxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=>	M2PrflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643	MmLqdWhVWyCjc4PhfS=>			Ml3adWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?=	Ml;JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
K562/DOX	NXSwboxoTnWwY4Tpc44h[XO\|YYm=	MYGxJJVO	NIG1XZUyOCCvaX7z	NHPXVZpKdmirYnn0bY9vKG:oIGCt[5AhcW5iaIXtZY4hUzV4Mj;EU3gh[2WubIOgZZN{\XO\|ZXSgZZMhcW6lcnXhd4UhcW5icnjv[IFucW6nLUGyN{Bm\m[udYigbY4hcHWvYX6gT\|U3OiClZXzsd{BifCBzIIXNJIlv[3WkYYTl[EBnd3JiMUCgcYlveyCqcoOgZpkh\myxdzDjfZRwdWW2comgdoVt[XSrdnWgeI8hfW62cnXheIVlKGOxboTyc4w>	NYX5TXRSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNVMyOjhpPkK4NVE{OTJ6PD;hQi=>
A2780adr	NUjiU\|dwTnWwY4Tpc44h[XO\|YYm=	M4DmZ\|ExKHWP	MYCzNEBucW6\|	NEXudmxKdmirYnn0bY9vKG:oIFHCR2IyKGmwIHj1cYFvKEF{N{iwZYRzKGOnbHzzJIF{e2W\|c3XkJIF{KGmwY4LlZZNmKGmwIHHjZ5VufWyjdHnvckBw\iClYXzj[YlvKEGPIHH0JFExKHWPIIDy[Ylv[3WkYYTl[EBnd3JiM{CgcYlveyCob3zsc5dm\CCkeTDjZYxk\WmwIFHNJIFl\Gm2aX;uJI1m[XO3cnXkJIV3\XK7IE[wJJNm[3NiZn;yJFYxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6KHKnbHH0bZZmKHSxIHPvcpRzd2x?	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV2N{K3Nkc,Ojl3NEeyO\|I9N2F-
HepG2	M2rqZWZ2dmO2aX;uJIF{e2G7	NYDJbVhyOTBidV2=	MUO5NEBucW6\|	NVvTfFJbUW6qaXLpeIlwdiCxZjDQMYdxKG2nZHnheIVlKGWoZnz1fEBqdiCjZILpZY16[2mwLYLld4l{fGGwdDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdnS{YXPlcIx2dGG{IILoc4RidWmwZT2xNlMh[WOldX31cIF1cW:wIHH0JFExKHWPIHnuZ5Vj[XSnZDDpckBl[XKtIHPvcoRqfGmxbjDmc5IhQTBibXnud{BjgSCobH;3JIN6fG:vZYTyfUBz\WyjdHn2[UB1dyClb370do9t	MlzyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd\|MkiwNlkoRjJ5M{K4NFI6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Immunofluorescence	MRP7 ; PubMed: 23393594 PLoS One HEK/MRP7 cells were treated with 0.3 µM tariquidar for different periods of time. The subcellular localization of MRP7 was analyzed by immunofluorescence. MRP7 staining is shown in green. DAPI (blue) counterstains the nuclei.	23393594

体内研究

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]

激酶实验： ^[1]	- 合并稳态药物累积实验: 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： ^[3]	- 合并 Cell lines: 小鼠乳腺癌细胞系MDR EMT6/AR1.0 Concentrations: ~100 nM Tariquidar Incubation Time: 4 天 Method: 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。 (Only for Reference)
动物实验： ^[3]	- 合并 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 (Only for Reference)

参考文献

[4] Walker J, et al. Eur J Cancer, 2004, 40(4), 594-605.

- 合并

溶解度 (25°C)

体外	DMSO	52 mg/mL (80.4 mM)
	Water	Insoluble
	Ethanol	Insoluble

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Tariquidar (XR9576) SDF

分子量	646.73
化学式	C₃₈H₃₈N₄O₆
CAS号	206873-63-4
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

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）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

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

计算重置

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，注：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：取 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。

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。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	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	Drug: Tariquidar\|Drug: Tc-94m Sestamibi	Cancer	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	May 16 2004	Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

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.

研究领域

产品类型

定制您的化合物库

Tariquidar (XR9576)

客户使用Selleck生产的Tariquidar (XR9576)发表文献31篇：

产品安全说明书

P-gp抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Tariquidar (XR9576) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

技术支持

常见问题及建议解决方法

P-gp Signaling Pathway Map

相关P-gp产品