Irinotecan (CPT-11) HCl Trihydrate

For research use only. Not for use in humans.

目录号:S2217 中文名称:盐酸依立替康三水合物

Irinotecan (CPT-11) HCl Trihydrate Chemical Structure

CAS No. 136572-09-3

Irinotecan (CPT-11)通过抑制Topoisomerase 1(拓扑异构酶1)而防止DNA解链。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1545.43 现货
RMB 571.52 现货
RMB 1722.94 现货
RMB 4332.51 现货
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客户使用Selleck生产的Irinotecan (CPT-11) HCl Trihydrate发表文献59篇:

产品安全说明书

Topoisomerase抑制剂选择性比较

生物活性

产品描述 Irinotecan (CPT-11)通过抑制Topoisomerase 1(拓扑异构酶1)而防止DNA解链。
特性 Irinotecan是一种用于治疗转移性结直肠癌的前药。
靶点
Topo I [1]
体外研究

Irinotecan被羧酸酯酶活化为SN-38,从而能够与其靶点,拓扑异构酶I相互作用。IC50浓度下的Irinotecan在LoVo细胞和HT-29细胞系中诱导相似量的可裂解复合物。SN-38诱导可裂解复合物浓度依赖性形成,这在LoVo细胞和HT-29细胞系中没有明显差异。Irinotecan引起的细胞积聚显著不同,在HT-29细胞中的水平始终高于LoVo细胞。[1] Irinotecan的内酯E环和SN-38在水溶液中可逆水解,内酯形式和羧酸盐形式之间的互变取决于PH和温度。Irinotecan主要通过肝脏活化为SN-38。对于相同浓度的Irinotecan和SN-38葡糖苷酸,在肿瘤和正常组织中,β-葡糖醛酸酶介导的SN-38产率均高于Irinotecan 形成的SN-38产率。[2] Irinotecan在肠道,血浆和肿瘤组织中转化为SN-38。[3] Irinotecan在SCLC细胞系中的活性显著高于NSCLC细胞系,而在组织学分型中没有观察到SN-38有明显的差异。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI8402 MVzDfZRwfG:6aXPpeJkh[XO|YYm= NHPad2M1KGSjeYO= M3XqWGN6fG:2b4jpZ{Bi[3Srdnn0fUBi\2GrboP0JIh2dWGwIHz5cZBpd2KuYYP0JJR2dW:{IHPlcIwhdGmwZTDSVG1KQDRyMjDh[pRmeiB2IHThfZMhd2ZidILlZZRu\W62LjDJR|UxRTBwNUeg{txO M3rrNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{N{S3O|k5Lz5zMke0O|c6QDxxYU6=
Hep3B NVf5NVRZSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmSyO|IhcHK| NHLYWIFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldFNDKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDYWHQh[XO|YYmsJGdKPTBiPTC0Mlc{KM7:TT6= MlXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5OU[5OVYoRjF7N{m2PVU3RC:jPh?=
HepG2 NIT5VlZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFq2OXA4OiCqcoO= NELueIZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDYWHQh[XO|YYmsJGdKPTBiPTC1Mlk1KM7:TT6= M1\JeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{m2PVU3Lz5zOUe5Olk2PjxxYU6=
NCI60 M2nNSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2nhPGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG5EUTZyIHPlcIx{KGK7IGPCVkBie3OjeTygS2k2OCB;IEG0MlEzPTRizszNMi=> NXfuT4lXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwN|U{OzRpPkKxNFM2OzN2PD;hQi=>
Hep3B NVXqe4VHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWO3NkBpenN? NX:wSW9QT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUGWyM1KgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFiWVDDhd5NigSxiR1m1NEA:KDRwN{Og{txONg>? MofCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{myOVQoRjJ{MEe5NlU1RC:jPh?=
HepG2 MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVe3NkBpenN? NU\kc3FiT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFiWVDDhd5NigSxiR1m1NEA:KDVwOUSg{txONg>? NFHlT5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVI2PCd-MkKwO|kzPTR:L3G+
MDA-MB-231 M4\wVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXf5dY5[PzJiaILz MVjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC[VGSgZZN{[XluIFfJOVAhRSB7LkG3JO69VS5? Mnz0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{myOVQoRjJ{MEe5NlU1RC:jPh?=
A549 MVXDfZRwfG:6aXPpeJkh[XO|YYm= MUG3NkBpenN? M3\P[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyIE2gOUDPxE1w MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh4N{CxPUc,OjJ6NkewNVk9N2F-
HCT116 NU\4R4xwS3m2b4TvfIlkcXS7IHHzd4F6 MlfvO|IhcHK| M2P2[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUCgQUA4NjFizszNMi=> NFnISHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki2O|AyQSd-MkK4OlcxOTl:L3G+
MDA-MB-435 NVH0UFZHS3m2b4TvfIlkcXS7IHHzd4F6 M{[xTlczKGi{cx?= MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDF{LkKg{txONg>? NYPVTmtTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4OlcxOTlpPkKyPFY4ODF7PD;hQi=>
K562 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MV23NkBpenN? MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYX\0[ZIhPzJiaILzMEBIUTVyIE2gNU46KM7:TT6= MmPiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2MkCxO|UoRjJ3NEKwNVc2RC:jPh?=
A549 M2DFRWFvfGm2dX3vdkBie3OjeR?= NYraWHFYPCCqcoO= MoG0RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB4LkWyPEDPxE1w NX7GWnMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyNFc4PDhpPkG4NlA4PzR6PD;hQi=>
LOVO MWjBcpRqfHWvb4KgZZN{[Xl? NHO3bGk1KGi{cx?= Mn[5RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF;WU{Bk\WyuczDh[pRmeiB2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB7LkCxOUDPxE1w MoWwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{MEe3OFgoRjF6MkC3O|Q5RC:jPh?=
MCF7 NXP1fYUzSW62aYT1cY9zKGG|c3H5 NGDJXnA1KGi{cx?= MlfkRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzNz60NFMh|ryPLh?= M2PocFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkC3O|Q5Lz5zOEKwO|c1QDxxYU6=
LS174T NXjkNlc1S3m2b4TvfIlkcXS7IHHzd4F6 M1fJVFk3KGi{cx?= NFHxT5JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNWzF5NGSgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFwMU[g{txONg>? NUHUZo1DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1NVM6PzZpPkG4OVE{QTd4PD;hQi=>
KB3-1 MoDCR5l1d3SxeHnjbZR6KGG|c3H5 NGrjcWpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSjNvMTDj[YxteyCkeTDNWHQhdWW2aH;kMEBKSzVyIE2gNE43QCEQvF2u MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd5MUmzNEc,OTh5N{G5N|A9N2F-
KBH5.0 M1XEfGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHnrfWVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSkh3LkCgZ4VtdHNiYomgUXRVKG2ndHjv[EwhUUN3MDC9JFcvPCEQvF2u NGPUbmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe3NVk{OCd-MUi3O|E6OzB:L3G+
KBV1 MX7DfZRwfG:6aXPpeJkh[XO|YYm= NYf1T4hKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0KYMTDj[YxteyCkeTDNWHQhdWW2aH;kMEBKSzVyIE2gOFAh|ryPLh?= NWS2bFRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3O|E6OzBpPkG4O|cyQTNyPD;hQi=>
MDA-MB-435 NVuwOWs3S3m2b4TvfIlkcXS7IHHzd4F6 MoHpO|IhcHK| NULRcXc{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNU4yPCEQvF2u NF;rNHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO3NVE5Oyd-MkCzO|EyQDN:L3G+
A549 NFzIUVVEgXSxdH;4bYNqfHliYYPzZZk> NUP1VIdoPzJiaILz MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC0MlYyKM7:TT6= MoK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|N{GxPFMoRjJyM{exNVg{RC:jPh?=
LoVo MVfDfZRwfG:6aXPpeJkh[XO|YYm= MYm3NkBpenN? NE[1WVhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNd1[xIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA1Njl7IN88UU4> NX2xbopJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzO|EyQDNpPkKwN|cyOTh|PD;hQi=>
A549 NYDNWGVNS3m2b4TvfIlkcXS7IHHzd4F6 M4jZTVMh\GG7cx?= NIT2RoxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUCgQUA3NjRizszNMi=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODl2MkS5NEc,OjB7NEK0PVA9N2F-
LoVo NHfOTnVEgXSxdH;4bYNqfHliYYPzZZk> MXGzJIRigXN? NVrjSWJZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVG:YbzDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hQC56IN88UU4> NHX2VXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEm0NlQ6OCd-MkC5OFI1QTB:L3G+
MDA-MB-435 MVXDfZRwfG:6aXPpeJkh[XO|YYm= NUPIbo9yOyCmYYnz MlzTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMUeg{txONg>? M4GxSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOUSyOFkxLz5{MEm0NlQ6ODxxYU6=
A375 MnWzR5l1d3SxeHnjbZR6KGG|c3H5 M{XVVlczKGi{cx?= M3jqVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcjDicJVmKGG|c3H5MEBKSzVyIE2gNE4xODRizszNMi=> MkHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|QoRjJzM{SxOlc1RC:jPh?=
PC3 NUnxNmFWS3m2b4TvfIlkcXS7IHHzd4F6 M4HETVczKGi{cx?= NH;6XoZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcjDicJVmKGG|c3H5MEBKSzVyIE2gNE4xODRizszNMi=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN2MU[3OEc,OjF|NEG2O|Q9N2F-
LNCAP NWHmdIY1S3m2b4TvfIlkcXS7IHHzd4F6 MoXmO|IhcHK| MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjC3NkBpenNiYomgZYxidWG{IHLseYUh[XO|YYmsJGlEPTBiPTCwMlAxQSEQvF2u M2\L[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{SxOlc1Lz5{MUO0NVY4PDxxYU6=
MESSA MYrDfZRwfG:6aXPpeJkh[XO|YYm= M1jrT|czKGi{cx?= MkT6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWVUW0FiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcjDicJVmKGG|c3H5MEBKSzVyIE2gNE4xOSEQvF2u NWjNbHJNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFE3PzRpPkKxN|QyPjd2PD;hQi=>
H460 MU\DfZRwfG:6aXPpeJkh[XO|YYm= NW\sc5JQPzJiaILz M1vSfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGg1PjBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcjDicJVmKGG|c3H5MEBKSzVyIE2gNE4xOTVizszNMi=> MoPpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|QoRjJzM{SxOlc1RC:jPh?=
H69 MYPDfZRwfG:6aXPpeJkh[XO|YYm= NYrTUHEzPzJiaILz MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIOlkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxKD1iMD6wNlIh|ryPLh?= NWf5RYpORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFE3PzRpPkKxN|QyPjd2PD;hQi=>
MES-SA/Dx5 NHTIc3pEgXSxdH;4bYNqfHliYYPzZZk> NVzCZ5JlPzJiaILz NIDXclBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTVNvU1GvSJg2KGOnbHzzJI93\XKneIDy[ZN{cW6pIF3EVlEh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcjDicJVmKGG|c3H5MEBKSzVyIE2gNE4xOjJizszNMi=> NGfQT2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO0NVY4PCd-MkGzOFE3PzR:L3G+
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Rh41 MknJdWhVWyCjc4PhfS=> NUnkO|A4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 MkTGdWhVWyCjc4PhfS=> Mn\1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohV3K2aH;nc45idCB|RDD2bYFjcWyrdImgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ NECyZ|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) NGfXN|lyUFSVIHHzd4F6 NYPlR2dZeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiT4L0bI9od26jbDCzSEB3cWGkaXzpeJkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= NXjnOYg4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 M1\wZpFJXFNiYYPzZZk> NUnXWoVKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> MojoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MUPxTHRUKGG|c3H5 NVTicoZ7eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 MYDxTHRUKGG|c3H5 M{jpWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz MnywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 MVLxTHRUKGG|c3H5 NYr4R5N6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NIfmfIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 MkHIdWhVWyCjc4PhfS=> NVyzVYpIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 M4jKRpFJXFNiYYPzZZk> M3;CN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG5DOTZ2MzDj[Yxtew>? Mo\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC M3L3epFJXFNiYYPzZZk> NVm4cGczeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M1rSNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32 Ml3kdWhVWyCjc4PhfS=> NXyzUmZ{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 NHTmN2ZyUFSVIHHzd4F6 M{PPT5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOThiY3XscJM> NX\Ve4VpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 M4XnWZFJXFNiYYPzZZk> MXrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> M4HIN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 NXG0UldbeUiWUzDhd5NigQ>? NInxNXByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCRcoToc4dwdmGuIEPEJJZq[WKrbHn0fUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= M3Py[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AMPK / p-AMPK / mTOR / p-mTOR / p70S6K / p-p70S6K; 

PubMed: 25973791     


Western blot showing the protein levels of AMPK, p-AMPK, mTOR, p-mTOR, p70S6K, and p-p70S6K in LoVo and LoVo-R8 with or without irinotecan. 

NFκB p65 / phospho-NFκB p65 / NFκB p50 / IκBα / p27Kip1; 

PubMed: 22206574     


For Western blot analysis (B), cytoplasmic proteins were analyzed using antibodies against NFκB p65 and p50, phospho-NFκB p65, IκBα and p27Kip1. In the presence of irinotecan, there was a loss of cytoplasmic NF-κBp65, but in the presence of sorafenib, this loss was greatly reduced, corresponding to a decrease in phosphorylation of NF-κBp65. In addition, compared to treatment with sorafenib or irinotecan alone, there was increased expression of IκBα following treatment with sorafenib and irinotecan. Lastly, following treatment with irinotecan and sorafenib irinotecan combination, there was decreased expression of p27Kip1 compared to sorafenib treatment alone.

TopI / pAKT / pMEK / pERK / p-p38 MAPK / pJNK2; 

PubMed: 29237470     


a Gimatecan significantly inhibited the expression of TopI, pAKT, pMEK, and pERK, and activated the expression of p-p38 MAPK and pJNK2 in SNU-1 cells. b Gimatecan significantly inhibited the expression of pAKT and pERK in NCI-N87 cells. Cells were starved in serum-free medium overnight, exposed to gimatecan or irinotecan for 48 h and harvested at 70–80% confluence. Total protein of SNU-1 and NCI-N87 was extracted and the expression of TopI, pAKT, pMEK, pERK, p-p38 MAPK and pJNK2 were assessed by western-blotting 

25973791 22206574 29237470
Immunofluorescence
NFκB; 

PubMed: 22206574     


BT12 cells were incubated with sorafenib or vehicle for 30 minutes followed by treatment with irinotecan for an additional 2 hours. For indirect immunofluorescence (A), cells were fixed and stained with antibodies to NF-κB followed by fluorescent labeled secondary antibodies. Concurrent DAPI stain was used to localize the nuclei (lower panel). Slides were visualized using a fluorescent microscope and random fields were photographed. The cytoplasmic staining seen in untreated and sorafenib treated cells was significantly reduced following treatment with irinotecan. However, the addition of sorafenib enabled the cells to maintain cytoplasmic staining in the presence of irinotecan. 

22206574
Growth inhibition assay
Cell viability; 

PubMed: 25973791     


The sensitivity of eight colon cancer cell lines to irinotecan was measured using the CCK-8 assay. For the CCK-8 assay, cells were exposed to irinotecan at given concentrations for 72 h before measurement. The cell viability was presented as the percentage relative to untreated cells.

25973791
体内研究 在COLO320异种移植物中,Irinotecan诱导92%的最大生长抑制。[5]单剂量Irinotecan显著增加胃,十二指肠,结肠和肝脏中拓扑异构酶I与DNA的共价结合数量。同时,与对照组相比,Irinotecan治疗组的结肠黏膜细胞中DNA链断裂数量明显较高。[6]

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)

细胞实验:

[1]

- 合并
  • Cell lines: LoVo 和HT-29 细胞
  • Concentrations: 0 μM -100 μM
  • Incubation Time: 48小时
  • Method:

    指数生长的细胞(LoVo和HT-29细胞)以每种细胞系的最佳接种数量(LoVo 细胞2×10<sup>4</sup>;HT-29细胞10<sup>5</sup>)接种于20 cm<sup>2</sup> Petri培养皿。2天后,用逐渐增加浓度的Irinotecan或SN-38处理一个细胞倍增时间(LoVo 细胞24小时,HT-29细胞40 小时)。0.15 M NaCl洗涤后,细胞进一步在正常培养基中生长两个倍增时间,从胰蛋白酶-EDTA的支撑物中分离,并在血细胞计数器上计数。IC50值的估算如下:与不含Irinotecan 或SN-38培养的细胞相比,引起50%生长抑制的Irinotecan 或SN-38浓度。


    (Only for Reference)
动物实验:

[5]

- 合并
  • Animal Models: 负荷COLO 320和WiDr异种移植物的雌性裸鼠
  • Dosages: 20 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (147.67 mM)
Water 1 mg/mL (1.47 mM)
Ethanol '7 mg/mL

* 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 677.18
化学式

C33H38N4O6.HCl.3H2O

CAS号 136572-09-3
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

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

Topoisomerase Signaling Pathway Map

相关Topoisomerase产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID