Tariquidar (XR9576)

目录号:S8028

仅限科研使用

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。

Tariquidar (XR9576) Chemical Structure

CAS: 206873-63-4

规格 价格 库存 购买数量
RMB 1415.55 现货
RMB 3846.69 现货
大包装 有超大折扣
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客户使用Selleck生产的Tariquidar (XR9576)发表文献36篇:

产品安全说明书

P-gp抑制剂选择性比较

相关P-gp产品

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 MnXGSpVv[3Srb36gZZN{[Xl? MnnGNVAxOCCwTR?= MoX0O|IhcHK| M1TIVXBwfGWwdHnheIlwdiCxZjD2bY5kemm|dHnu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDNTNvMTDj[YxteyCjc4Pld5Nm\CCjczD2bY5kemm|dHnu[UBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iMD63PEAsNy1iMD6yO{BvVSluIFnDOVA:OC5yMEC0Ne69VQ>? M2DTVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
KBV1 NVrhV4h3TnWwY4Tpc44h[XO|YYm= MofyNVAxOCCwTR?= MXG3NkBpenN? MXnJcohq[mm2aX;uJI9nKGi3bXHuJGFDS0JzIHX4dJJme3OnZDDpckBMSlZzIHPlcIx{KGG|c3Xzd4VlKGG|IIDveIVvfGmjdHnvckBw\iC4aX7jdol{fGmwZT3pcoR2[2WmIHP5eI91d3irY3n0fUBjgSCvZXHzeZJqdmdidnnuZ5Jqe3SrbnWgTWM2OCCjdDCxNFAxKG6PIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XliKGL2ZkA:KDJ5Nz62PEAsNy1iNU[uOlEhdk1rLDDJR|UxRTBwMECwOlbPxE1? NWfGW3NERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
HEK293 MUHGeY5kfGmxbjDhd5NigQ>? MYOxNFAxKG6P NXnNOmpGPzJiaILz NEfiWXFRd3SnboTpZZRqd25ib3[g[I95d3K3YnnjbY4ucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMh\G:6b4L1ZolkcW5iSVO1NEBifCBzMECwJI5OKGGodHXyJFczKGi{czDifUBES0t6IHHzd4F6KCiUdnKgQUA2NjJ6IDuvMUAxNjd2IH7NLUwhUUN3ME2wMlAxPDl3zszN Mne4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
OVCAR8 MnTvSpVv[3Srb36gZZN{[Xl? NFnrWZEyODByIH7N M2LKSlczKGi{cx?= MnLEVI91\W62aXH0bY9vKG:oII\pcoNzcXO2aX7lMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJ6IHPlcIx{KGG|c3Xzd4VlKGG|II\pcoNzcXO2aX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB6LkWzJEswNSBzLkm1JI5OMSxiSVO1NF0xNjByNUG4{txO NXvwfWJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
KB-3-1 NHzuXVFHfW6ldHnvckBie3OjeR?= M2rRWVExODBibl2= MmLEVI91\W62aXH0bY9vKG:oIHPvcINpcWOrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRk0{NTFiY3XscJMh[XO|ZYPz[YQh[XNiY3;sZ4hq[2mwZTDJR|UxKGG2IEGwNFAhdk1iYomgUXRVKGG|c3H5JEhTfmJiPTC4MlgyKCtxLTCzMlgxKG6PKTygTWM2OD1yLkCwPFQy|ryP NULQVnIxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
KBV1 MkPYSpVv[3Srb36gZZN{[Xl? NIPm[GgyODByIH7N MVu3NkBpenN? M2j6OmlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFQkGg[ZhxemW|c3XkJIlvKEuEVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgdI91\W62aXH0bY9vKG:oIHPvcINpcWOrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[nlibXXhd5VzcW6pIHPvcINpcWOrbnWgTWM2OCCjdDCxNFAxKG6PIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XliKGL2ZkA:KDR6Nz61O{AsNy1iM{CuOVQhdk1rLDDJR|UxRTBwMEC5NFXPxE1? M3O2S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
MDCK Mlq4SpVv[3Srb36gZZN{[Xl? NIfHeJI{OCCvaX7z Ml;PRYN1cX[rdImgZZQhSkOUUDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBOTEONIHPlcIx{KHW|aX7nJJJpd2SjbXnu[UAyOjNiYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiM{CgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGVEPTB;MD6wNe69VQ>? M{XpXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{e0PFczLz5{M{O3OFg4OjxxYU6=
NCI-ADR-RES NWrIVGJRTnWwY4Tpc44h[XO|YYm= NWPiSlVwOTByMDDuUS=> Ml;vO|IhcHK| MlmzTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hVkOLLVHEVk1TTVNiY3XscJMh[XO|ZYPz[YQh[XNicH;0[Y51cWG2aX;uJI9nKH[rbnPybZN1cW6nLXnu[JVk\WRiY4n0c5RwgGmlaYT5JIJ6KG2nYYP1dolv\yC4aX7jdol{fGmwZTDJR|UxKGG2IEGwNFAhdk1iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSBqUo\iJF0hOzdzND64NEAsNy1iM{izMlU5KG6PKTygTWM2OD1yLkCxPFUy|ryP NWnQVlBwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
OVCAR8 NXjzTHlvTnWwY4Tpc44h[XO|YYm= NHTMdJMyODByIH7N M2e3fVczKGi{cx?= NF\kRXZRd3SnboTpZZRqd25ib3[gZ49t[2irY3nu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUODDj[YxteyCjc4Pld5Nm\CCjczDjc4xkcGmlaX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB{Nz6yOkAsNy1iOT65OkBvVSluIFnDOVA:OC5yMkO3N:69VQ>? M4\0O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
HEK293 NYHM[YVETnWwY4Tpc44h[XO|YYm= M3LLWFExODBibl2= NVmweHlNPzJiaILz NXi5eXNyUW6qaXLpeIlwdiCxZjDoeY1idiCDQlPCNUB1emGwc3\lZ5Rm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNicH;0[Y51cWG2aX;uJI9nKGSxeH;yeYJq[2mwLXnu[JVk\WRiY4n0c5RwgGmlaYT5JIJ6KG2nYYP1dolv\yCmb4jvdpVjcWOrbjDJR|UxKGG2IEGwNFAhdk1iYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XliKGL2ZkA:KDVyND62OUAsNy1iNESuPVQhdk1rLDDJR|UxRTBwMEK0O|fPxE1? NI\tVZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WwOFY3QSd-Mke1NFQ3Pjl:L3G+
NCI-ADR-RES M{X3OGZ2dmO2aX;uJIF{e2G7 NFfRRnMyODByIH7N M4PZ[lczKGi{cx?= MlnRTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hVkOLLVHEVk1TTVNiY3XscJMh[XO|ZYPz[YQh[XNicH;0[Y51cWG2aX;uJI9nKGOxbHPobYNqdmVvaX7keYNm\CCleYTveI95cWOrdImgZpkhdWWjc4XybY5oKGOxbHPobYNqdmViSVO1NEBifCBzMECwJI5OKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZkhMFK4YjC9JFE3ODdwNUCgL{8uKDR7Nz60NkBvVSluIFnDOVA:OC5yMkS5O:69VQ>? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
CCRF-CEM/VCR1000 M1Sy[GZ2dmO2aX;uJIF{e2G7 M2DTd|I1OCC|ZXPz MlXSTY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpck1u\WSrYYTl[EBl[XWwb4L1ZolkcW5iZX\mcJV5KG[{b32gbJVu[W5iQ1PSSk1ETU1xVlPSNVAxOCClZXzsd{Bi\nSncjCyOFAhe2WlczDifUBHSUOVIH\sc5ch[3m2b33leJJq[yCjbnHsfZNqeyxiSVO1NF0xNjB|M{Gx{txO MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR3MkSxNkc,OjJ2NUK0NVI9N2F-
MDCK Moj3SpVv[3Srb36gZZN{[Xl? MYWzNEBucW6| NVXhfmdMSWO2aY\peJkh[XRiTVTSNUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCPRFPLJINmdGy|IIXzbY5oKGOjbHPlbY4hSU1iYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiM{CgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGVEPTB;MD6wOFTPxE1? M3vySVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{e0PFczLz5{M{O3OFg4OjxxYU6=
MDCK M4DvTGZ2dmO2aX;uJIF{e2G7 Mo\nN|AhdWmwcx?= NFv3RnhKdmirYnn0bY9vKG:oIGCt[4x6[2:ycn;0[YlvKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIF3ER2sh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHPhcINmcW5vQV2geJJidnOyb4L0JIFnfGW{IEOwJI1qdnNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBGSzVyPUCuNFQ1|ryP NELKOmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[wO|k6QSd-MkS2NFc6QTl:L3G+
EMT6/AR1.0 NVizOG9DTnWwY4Tpc44h[XO|YYm= NVewW5RzOSCqch?= NYDqPIRWUW6qaXLpeIlwdiCxZjDtc5V{\SCSZ4CgbY4hTU2WNj;BVlEvOCClZXzsd{Bi\nSncjCxJIhzKGK7IHTheY5wenWkaXPpckBi[2O3bYXsZZRqd25iYYPzZZktKEmFNUC9NE4xPjUQvF2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB6M{CzOEc,OThyOEOwN|Q9N2F-
EMT6/AR1.0 NIX6VJlHfW6ldHnvckBie3OjeR?= MWOxJIhz NF7KWHVKdmirYnn0bY9vKG:oIH3veZNmKFCpcDDpckBGVVR4L1HSNU4xKGOnbHzzJIFnfGW{IEGgbJIh[nliZHH1co9zfWKrY3nuJIFk[3WvdXzheIlwdiCjc4PhfUwhUUN3ME2wMlA3PDV5zszN NHLGeXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC4N|A{PCd-MUiwPFMxOzR:L3G+
CEM/VLB500 MmDlSpVv[3Srb36gZZN{[Xl? M2XDVlMh\GG7cx?= MoTHVoV3\XK|YXygc4YhWC2pcD3t[YRq[XSnZDDteYx1cWS{dXegdoV{cXO2YX7j[UB1dyC4aX7icIF{fGmwZTDpckBpfW2jbjDDSW0wXkyENUCwJINmdGy|IHHmeIVzKDNiZHH5d{BjgSC{ZYPhfpVzcW5iYYPzZZktKEWFNUC9NE4xPjkQvF2= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzN7OUm5NEc,OTd|OUm5PVA9N2F-
KBV1 MVzGeY5kfGmxbjDhd5NigQ>? NGq3bZUyODByIH7N NHvBWFA4OiCqcoO= MknRTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hU0KYMTDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[nlibXXhd5VzcW6pIHTvfI9zfWKrY3nuJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB3LkC3JEswNSByLkG5JJVOMSxiSVO1NF0xNjB5zszN M3HNS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
A2780 NHvBeJpHfW6ldHnvckBie3OjeR?= M3y3SmlvcGmkaYTpc44hd2ZiUD3ndEBqdiCqdX3hckBi\HKrYX35Z4lvNXKnc3nzeIFvfCCDMke4NEBk\WyuczDifUBJd2WlaIP0JFM{OzR{IHHzd4F6NCCLQ{WwQVAvODd{NEVOwG0> NEnXTok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[3PFQ6PSd-MUi2O|g1QTV:L3G+
A2780/ADR M3LGTGZ2dmO2aX;uJIF{e2G7 NGXBOpFKdmirYnn0bY9vKG:oIGCt[4x6[2:ycn;0[YlvNW2nZHnheIVlKG23bITp[JJ2\yC{ZYPpd5RidmOnIHnuJIFlemmjbYnjbY4uemW|aYP0ZY51KGi3bXHuJGEzPzhyL1HEVkBk\WyuczDifUBk[WylZXnuJGFOKGG|c3H5MEBKSzVyPUCuNFc5|ryP NWXy[IdlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOVA5OzRpPkG5NlUxQDN2PD;hQi=>
A2780adr NF73VohHfW6ldHnvckBie3OjeR?= NVrXUpdKUW6qaXLpeIlwdiCxZjDQMYdxKGW6cILld5Nm\CCrbjDBNlc5OGGmcjDj[YxteyCkeTDjZYxk\WmwIFHNJIFk[3WvdXzheIlwdiCjc4PhfUwhUUN3ME2wMlA5|ryP NWTaSXZ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOVQ5ODBpPkKxN|U1QDByPD;hQi=>
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Assay
Methods Test Index PMID
Immunofluorescence MRP7 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]

  • 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]

  • 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。

动物实验:

[3]

  • 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

溶解度(25°C)

体外

* 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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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。

摩尔浓度计算器

质量 浓度 体积 分子量

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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.