Tariquidar (XR9576)

For research use only. Not for use in humans.

目录号:S8028

Tariquidar (XR9576) Chemical Structure

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Kd为5.1 nM,作用于MDR细胞系逆转耐药性。Phase 3。

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客户使用Selleck生产的Tariquidar (XR9576)发表文献34篇:

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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-3-1 NFX6d2RHfW6ldHnvckBie3OjeR?= NEHTWlkyODByIH7N M4O4UlczKGi{cx?= M1vx[XBwfGWwdHnheIlwdiCxZjD2bY5kemm|dHnu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDNTNvMTDj[YxteyCjc4Pld5Nm\CCjczD2bY5kemm|dHnu[UBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iMD63PEAsNy1iMD6yO{BvVSluIFnDOVA:OC5yMEC0Ne69VQ>? MonuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
KBV1 Ml3xSpVv[3Srb36gZZN{[Xl? NXTSVINNOTByMDDuUS=> NHP1NJQ4OiCqcoO= MnPFTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hU0KYMTDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZidnnuZ5Jqe3SrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[nlibXXhd5VzcW6pII\pcoNzcXO2aX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB{N{euOlghMy9vIEW2MlYyKG6PKTygTWM2OD1yLkCwNFY3|ryP MlriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
HEK293 NHfUW2tHfW6ldHnvckBie3OjeR?= NUHISoZQOTByMDDuUS=> Ml3IO|IhcHK| NIm1TIRRd3SnboTpZZRqd25ib3[g[I95d3K3YnnjbY4ucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMh\G:6b4L1ZolkcW5iSVO1NEBifCBzMECwJI5OKGGodHXyJFczKGi{czDifUBES0t6IHHzd4F6KCiUdnKgQUA2NjJ6IDuvMUAxNjd2IH7NLUwhUUN3ME2wMlAxPDl3zszN MkPNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
OVCAR8 M2jtVmZ2dmO2aX;uJIF{e2G7 M4T6WlExODBibl2= M4\2[VczKGi{cx?= NXX5R2NkWG:2ZX70bYF1cW:wIH;mJJZqdmO{aYP0bY5mNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWK4JINmdGy|IHHzd4V{e2WmIHHzJJZqdmO{aYP0bY5mKEmFNUCgZZQhOTByMDDuUUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5JEhTfmJiPTC4MlU{KCtxLTCxMlk2KG6PKTygTWM2OD1yLkCwOVE5|ryP NE[0dlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WwOFY3QSd-Mke1NFQ3Pjl:L3G+
KB-3-1 NYTHV4xYTnWwY4Tpc44h[XO|YYm= NX\KOlR2OTByMDDuUS=> NH3wXFlRd3SnboTpZZRqd25ib3[gZ49t[2irY3nu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDNTNvMTDj[YxteyCjc4Pld5Nm\CCjczDjc4xkcGmlaX7lJGlEPTBiYYSgNVAxOCCwTTDifUBOXFRiYYPzZZkhMFK4YjC9JFgvQDFiKz:tJFMvQDBibl2pMEBKSzVyPUCuNFA5PDIQvF2= NEW3O2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WwOFY3QSd-Mke1NFQ3Pjl:L3G+
KBV1 NVvPOI9bTnWwY4Tpc44h[XO|YYm= M13yTVExODBibl2= MmTGO|IhcHK| MWTJcohq[mm2aX;uJI9nKGi3bXHuJGFDS0JzIHX4dJJme3OnZDDpckBMSlZzIHPlcIx{KGG|c3Xzd4VlKGG|IIDveIVvfGmjdHnvckBw\iClb3zjbIlkcW6nLXnu[JVk\WRiY4n0c5RwgGmlaYT5JIJ6KG2nYYP1dolv\yClb3zjbIlkcW6nIFnDOVAh[XRiMUCwNEBvVSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6KCiUdnKgQUA1QDdwNUegL{8uKDNyLkW0JI5OMSxiSVO1NF0xNjByOUC1{txO MmjlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
MDCK M4exUGZ2dmO2aX;uJIF{e2G7 MV:zNEBucW6| NHjEe4xC[3Srdnn0fUBifCCEQ2LQJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKE2GQ1ugZ4VtdHNidYPpcochemixZHHtbY5mKDF{MzDhd{B{fWK|dILheIUhcW6ldXLheIVlKG[xcjCzNEBucW6|IIDybY9zKHSxIIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGK7IH\seY9zd22ndILpZ{BidmGueYPpd{whTUN3ME2wMlAy|ryP NX\Dc4g3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|Q5PzJpPkKzN|c1QDd{PD;hQi=>
NCI-ADR-RES M3TPOmZ2dmO2aX;uJIF{e2G7 M2\EVVExODBibl2= M{S1UVczKGi{cx?= NXzkbZYyUW6qaXLpeIlwdiCxZjDoeY1idiCDQlPCNUBmgHC{ZYPz[YQhcW5iTlPJMWFFWi2URWOgZ4VtdHNiYYPz[ZN{\WRiYYOgdI91\W62aXH0bY9vKG:oII\pcoNzcXO2aX7lMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGK7IH3lZZN2emmwZzD2bY5kemm|dHnu[UBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iM{exOE45OCBtLz2gN|g{NjV6IH7NLUwhUUN3ME2wMlAyQDVzzszN MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
OVCAR8 NFzhPVdHfW6ldHnvckBie3OjeR?= NWnSO5A4OTByMDDuUS=> NV\mNWlqPzJiaILz MmDmVI91\W62aXH0bY9vKG:oIHPvcINpcWOrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[XO|ZYPz[YQh[XNiY3;sZ4hq[2mwZTDJR|UxKGG2IEGwNFAhdk1iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSBqUo\iJF0hOjdwMk[gL{8uKDlwOU[gcm0qNCCLQ{WwQVAvODJ|N{ROwG0> M4LwcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
HEK293 NI[yXWdHfW6ldHnvckBie3OjeR?= MojTNVAxOCCwTR?= Mmf6O|IhcHK| MknJTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMheG:2ZX70bYF1cW:wIH;mJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHL5JI1m[XO3cnnu[{Bld3ixcoXibYNqdiCLQ{WwJIF1KDFyMECgcm0h[W[2ZYKgO|IhcHK|IHL5JGNEUzhiYYPzZZkhMFK4YjC9JFUxPC54NTCrM{0hPDRwOUSgcm0qNCCLQ{WwQVAvODJ2N{hOwG0> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
NCI-ADR-RES NXvxXoN1TnWwY4Tpc44h[XO|YYm= Mnm5NVAxOCCwTR?= NH;zXGM4OiCqcoO= NX7ORZNYUW6qaXLpeIlwdiCxZjDoeY1idiCDQlPCNUBmgHC{ZYPz[YQhcW5iTlPJMWFFWi2URWOgZ4VtdHNiYYPz[ZN{\WRiYYOgdI91\W62aXH0bY9vKG:oIHPvcINpcWOrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[nlibXXhd5VzcW6pIHPvcINpcWOrbnWgTWM2OCCjdDCxNFAxKG6PIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XliKGL2ZkA:KDF4MEeuOVAhMy9vIES5O{41OiCwTTmsJGlEPTB;MD6wNlQ6P87:TR?= NV;kdnVKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
CCRF-CEM/VCR1000 MUXGeY5kfGmxbjDhd5NigQ>? Mlv5NlQxKHOnY4O= M2\qOWlvcGmkaYTpc44hd2ZiUD3ncJlkd3C{b4TlbY4udWWmaXH0[YQh\GG3bn;yeYJq[2mwIHXm[ox2gCCocn;tJIh2dWGwIFPDVmYuS0WPL2\DVlExODBiY3XscJMh[W[2ZYKgNlQxKHOnY4OgZpkhTkGFUzDmcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OC5yM{OxNe69VQ>? NGfEdng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS1NlQyOid-MkK0OVI1OTJ:L3G+
MDCK MkLHSpVv[3Srb36gZZN{[Xl? NGS0ZZQ{OCCvaX7z NXLHSWRjSWO2aY\peJkh[XRiTVTSNUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCPRFPLJINmdGy|IIXzbY5oKGOjbHPlbY4hSU1iYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiM{CgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGVEPTB;MD6wOFTPxE1? NHv1ZnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3OFg4Oid-MkOzO|Q5PzJ:L3G+
MDCK M3e0U2Z2dmO2aX;uJIF{e2G7 NVTVR3N[OzBibXnudy=> NWGxNG9bUW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDNSGNMKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDjZYxk\WmwLVHNJJRz[W6|cH;yeEBi\nSncjCzNEBucW6|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhTUN3ME2wMlA1PM7:TR?= MnPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MEe5PVkoRjJ2NkC3PVk6RC:jPh?=
EMT6/AR1.0 M3K0XGZ2dmO2aX;uJIF{e2G7 MYCxJIhz NVG3NFN[UW6qaXLpeIlwdiCxZjDtc5V{\SCSZ4CgbY4hTU2WNj;BVlEvOCClZXzsd{Bi\nSncjCxJIhzKGK7IHTheY5wenWkaXPpckBi[2O3bYXsZZRqd25iYYPzZZktKEmFNUC9NE4xPjUQvF2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB6M{CzOEc,OThyOEOwN|Q9N2F-
EMT6/AR1.0 NV7QU5lDTnWwY4Tpc44h[XO|YYm= M1G1eVEhcHJ? M330O2lvcGmkaYTpc44hd2ZibX;1d4UhWGeyIHnuJGVOXDZxQWKxMlAh[2WubIOgZYZ1\XJiMTDodkBjgSCmYYXuc5J2[mmlaX6gZYNkfW23bHH0bY9vKGG|c3H5MEBKSzVyPUCuNFY1PTgQvF2= MorWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyOEOwN|QoRjF6MEizNFM1RC:jPh?=
CEM/VLB500 MVzGeY5kfGmxbjDhd5NigQ>? Mne0N{Bl[Xm| M4W4R3JmfmW{c3HsJI9nKFBvZ4CtcYVlcWG2ZXSgcZVtfGmmcoXnJJJme2m|dHHuZ4UhfG9idnnuZoxie3SrbnWgbY4hcHWvYX6gR2VON1[OQkWwNEBk\WyuczDh[pRmeiB|IHThfZMh[nlicnXzZZp2emmwIHHzd4F6NCCHQ{WwQVAvODZ6zszN NF;Yfo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{O5PVk6OCd-MUezPVk6QTB:L3G+
KBV1 NXW3Uld1TnWwY4Tpc44h[XO|YYm= NUPXVGlyOTByMDDuUS=> M1fucFczKGi{cx?= MmrnTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hU0KYMTDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[nlibXXhd5VzcW6pIHTvfI9zfWKrY3nuJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB3LkC3JEswNSByLkG5JJVOMSxiSVO1NF0xNjB5zszN NXLIZ3d1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
A2780 NFz4d4lHfW6ldHnvckBie3OjeR?= NGrYfpdKdmirYnn0bY9vKG:oIGCt[5AhcW5iaIXtZY4h[WS{aXHtfYNqdi2{ZYPpd5RidnRiQUK3PFAh[2WubIOgZpkhUG:nY3jzeEA{OzN2MjDhd5NigSxiSVO1NF0xNjB5MkS0{txO MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDZ5OES5OUc,OTh4N{i0PVU9N2F-
A2780/ADR MmDsSpVv[3Srb36gZZN{[Xl? NXOxWZRPUW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdi2vZXTpZZRm\CCvdXz0bYRzfWdicnXzbZN1[W6lZTDpckBi\HKrYX35Z4lvNXKnc3nzeIFvfCCqdX3hckBCOjd6MD;BSHIh[2WubIOgZpkh[2GuY3XpckBCVSCjc4PhfUwhUUN3ME2wMlA4QM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ3MEizOEc,OTl{NUC4N|Q9N2F-
A2780adr MWfGeY5kfGmxbjDhd5NigQ>? Mon0TY5pcWKrdHnvckBw\iCSLXfwJIV5eHKnc4Pl[EBqdiCDMke4NIFleiClZXzsd{BjgSClYXzj[YlvKEGPIHHjZ5VufWyjdHnvckBie3OjeTygTWM2OD1yLkC4{txO MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN3NEiwNEc,OjF|NUS4NFA9N2F-
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K562/A02 MVrGeY5kfGmxbjDhd5NigQ>? MoXOOFghcHK| M{XuNGlvcGmkaYTpc44hd2ZiQVLDRlEhcW5iaIXtZY4hUzV4Mj;BNFIh[2WubIOgZZN{\XO|ZXSgZZMheG:2ZX70bYF1cW:wIH;mJIFlemmjbYnjbY4ucW6mdXPl[EBkgXSxdH;4bYNqfHliYomgcYVie3W{aX7nJGFFWiCLQ{WwJJRz\WG2ZXSg[o9zKDR6IHjyd{Bnd2yub4fl[EBjgSClb33wc5Vv\CC5YYPoc5V1KG2nYYP1doVlKGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZkhMFK4YjC9JFUyNjN2IDuvMUA2NjFidV2pMEBKSzVyPUG0MlM6|ryP NITzS|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[0OVg{OSd-Mki2OFU5OzF:L3G+
HLF NYDOW5BLS3m2b4TvfIlkcXS7IHHzd4F6 MnXiOFghcHK| NHn6Tm5EgXSxdH;4bYNqfHliYXfhbY5{fCCKTF[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yPi54Od88US=> M2rQblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{K4NFI6Lz5{N{OyPFAzQTxxYU6=
SW620 MYTDfZRwfG:6aXPpeJkh[XO|YYm= MlnpOFghcHK| MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUK1{txO M3nteFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUm3NVYxLz5{NkG5O|E3ODxxYU6=
SW620/AD300 M1HxdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NEXoWXE1QCCqcoO= M3rVSmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyL1HEN|AxKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MkZOwG0> M2fSbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUm3NVYxLz5{NkG5O|E3ODxxYU6=
CCD-18Co MnmyR5l1d3SxeHnjbZR6KGG|c3H5 MmC4OFghcHK| MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDR2QuOTiFbzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI2|ryP NVPqSVBlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPVcyPjBpPkK2NVk4OTZyPD;hQi=>
K562/A02 NYrnSHIzS3m2b4TvfIlkcXS7IHHzd4F6 MoDVOFghcHK| NIDHTohEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{L1GwNkBk\WyuczDveoVz\XiycnXzd4lv\yCSLXfwJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI4NjF7zszN M{HmN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkOxO|g3Lz5{OU[zNVc5PjxxYU6=
K562/A02 NIS5bVVEgXSxdH;4bYNqfHliYYPzZZk> NYr1TXgyPDhiaILz NXTKU4FoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4Mj;BNFIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{Nz6xPe69VQ>? Mni4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4NEW4N|EoRjJ6NkS1PFMyRC:jPh?=
K562 NXrQeoZxS3m2b4TvfIlkcXS7IHHzd4F6 NHe1WHY1QCCqcoO= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVMyNjV4zszN NF\iWGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[zNVc5Pid-Mkm2N|E4QDZ:L3G+
K562 NH;yfm9EgXSxdH;4bYNqfHliYYPzZZk> MV20PEBpenN? MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;M{GuOVbPxE1? NETl[FM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[0OVg{OSd-Mki2OFU5OzF:L3G+
HepG2 MVPDfZRwfG:6aXPpeJkh[XO|YYm= MX[0PEBpenN? M1K4[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGGmcnnhcZlkcW5vcnXzbZN1[W62IHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OzdwMt88US=> NV\DW5hFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezNlgxOjlpPkK3N|I5ODJ7PD;hQi=>
KB-V1 NFTrUXRHfW6ldHnvckBie3OjeR?= NWXz[ppiOjByIH7N M1TVb2lvcGmkaYTpc44hd2ZiUD3ndEBqdiCqdX3hckBMSi2YMTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBzcG:mYX3pcoUhOTJ|IHHjZ5VufWyjdHnvckBifCB{MECgcm0> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3N{K3NUc,OjF4NUeyO|E9N2F-
SK-N-MC MWDxTHRUKGG|c3H5 M2Thc5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz M3rsN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH NUH5[Gp3eUiWUzDhd5NigQ>? NWLz[FZNeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> Mlf5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 MX;xTHRUKGG|c3H5 NGDTN3NyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
K562/DOX M4DvOmZ2dmO2aX;uJIF{e2G7 MmjZNUB2VQ>? NXz3[2lROTBibXnudy=> MlTzTY5pcWKrdHnvckBw\iCSLXfwJIlvKGi3bXHuJGs2PjJxRF;YJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKHKqb3ThcYlv\S1zMkOg[YZndHW6IHnuJIh2dWGwIFu1OlIh[2WubIOgZZQhOSC3TTDpcoN2[mG2ZXSg[o9zKDFyIH3pcpMhcHK|IHL5JIZtd3diY4n0c41mfHK7IILlcIF1cX[nIITvJJVvfHKnYYTl[EBkd262cn;s NYTrU|BvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNVMyOjhpPkK4NVE{OTJ6PD;hQi=>
A2780adr MXLGeY5kfGmxbjDhd5NigQ>? NVHET5oxOTBidV2= M3fBdFMxKG2rboO= NGH0eVJKdmirYnn0bY9vKG:oIFHCR2IyKGmwIHj1cYFvKEF{N{iwZYRzKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHHjZ5VufWyjdHnvckBw\iClYXzj[YlvKEGPIHH0JFExKHWPIIDy[Ylv[3WkYYTl[EBnd3JiM{CgcYlveyCob3zsc5dm\CCkeTDjZYxk\WmwIFHNJIFl\Gm2aX;uJI1m[XO3cnXkJIV3\XK7IE[wJJNm[3NiZn;yJFYxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6KHKnbHH0bZZmKHSxIHPvcpRzd2x? MnvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NEeyO|IoRjJ7NUS3NlczRC:jPh?=
HepG2 Mk\ZSpVv[3Srb36gZZN{[Xl? NV;KTnE{OTBidV2= MnjuPVAhdWmwcx?= NVi2Z|ZbUW6qaXLpeIlwdiCxZjDQMYdxKG2nZHnheIVlKGWoZnz1fEBqdiCjZILpZY16[2mwLYLld4l{fGGwdDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdnS{YXPlcIx2dGG{IILoc4RidWmwZT2xNlMh[WOldX31cIF1cW:wIHH0JFExKHWPIHnuZ5Vj[XSnZDDpckBl[XKtIHPvcoRqfGmxbjDmc5IhQTBibXnud{BjgSCobH;3JIN6fG:vZYTyfUBz\WyjdHn2[UB1dyClb370do9t MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN{OECyPUc,Ojd|MkiwNlk9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Immunofluorescence
MRP7 ; 

PubMed: 23393594     


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]

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)

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)

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

分子量 646.73
化学式

C38H38N4O6

CAS号 206873-63-4
储存条件 粉状
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 g 每只动物给药体积 ul 动物数量
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

计算器

摩尔浓度计算器

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

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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

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。

  • * 必填项

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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P-gp Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID