Irinotecan (CPT-11) HCl Trihydrate

For research use only.

Catalog No.S2217

58 publications

Irinotecan (CPT-11) HCl Trihydrate Chemical Structure

CAS No. 136572-09-3

Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.

Selleck's Irinotecan (CPT-11) HCl Trihydrate has been cited by 58 publications

Purity & Quality Control

Choose Selective Topoisomerase Inhibitors

Biological Activity

Description Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.
Features Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets
Topo I [1]
In vitro

Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. Irinotecan induces similar amounts of cleavable complexes at its IC50 in LoVo cells and HT-29 cell lines. SN-38 induces a concentration-dependent formation of cleavable complexes, which is not significantly different in LoVo cells and HT-29 cell lines. Cell accumulation of Irinotecan is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. [1] The lactone E-ring of Irinotecan and SN-38 hydrolyses reversibly in aqueous solutions, and the interconversion between the lactone and carboxylate forms is dependent on pH and temperature. Liver is primarily responsible for the activation of Irinotecan to SN-38. At equal concentrations of Irinotecan and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from Irinotecan in both tumour and normal tissue. [2] Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues. [3] Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI8402 M4\Tb2N6fG:2b4jpZ4l1gSCjc4PhfS=> M4rvWVQh\GG7cx?= MYXDfZRwfG:6aXOgZYN1cX[rdImgZYdicW6|dDDoeY1idiCueX3wbI9jdGG|dDD0eY1weiClZXzsJIxqdmViUmDNTVg1ODJiYX\0[ZIhPCCmYYnzJI9nKHS{ZXH0cYVvfC5iSVO1NF0xNjV5IN88US=> M37ke|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{N{S3O|k5Lz5zMke0O|c6QDxxYU6=
Hep3B NGT5fmtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NUnN[XdiPzJiaILz M2\jV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwN2Ih[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGjUWEBie3OjeTygS2k2OCB;IESuO|Mh|ryPLh?= M13aOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{m2PVU3Lz5zOUe5Olk2PjxxYU6=
HepG2 NVW3O4JySW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYfBeppOPzJiaILz NEH2V4hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDYWHQh[XO|YYmsJGdKPTBiPTC1Mlk1KM7:TT6= NH\LRmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe5Olk2Pid-MUm3PVY6PTZ:L3G+
NCI60 NVnJOIhGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYrHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2k3OCClZXzsd{BjgSCVQmKgZZN{[XluIFfJOVAhRSBzND6xNlU1KM7:TT6= NH3wWlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUCzOVM{PCd-MkGwN|U{OzR:L3G+
Hep3B MmDBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEjHZnI4OiCqcoO= NX3GflBkT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUGWyM1KgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFiWVDDhd5NigSxiR1m1NEA:KDRwN{Og{txONg>? MkjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{myOVQoRjJ{MEe5NlU1RC:jPh?=
HepG2 NHLBN5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVG3NkBpenN? MUnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC3NkBpenNiYomgXHRVKGG|c3H5MEBIUTVyIE2gOU46PCEQvF2u NHPkOFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVI2PCd-MkKwO|kzPTR:L3G+
MDA-MB-231 NYntfJJ3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3[5SlczKGi{cx?= NE\DOJZIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDYWHQh[XO|YYmsJGdKPTBiPTC5MlE4KM7:TT6= MlXYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{myOVQoRjJ{MEe5NlU1RC:jPh?=
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MCF7 MYPBcpRqfHWvb4KgZZN{[Xl? NWXyOVB3PCCqcoO= NX34PYY2SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxO{41ODNizszNMi=> NUPGPWdjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyNFc4PDhpPkG4NlA4PzR6PD;hQi=>
LS174T NHPreFREgXSxdH;4bYNqfHliYYPzZZk> M17xUFk3KGi{cx?= M3\qUGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxUOTd2VDDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS5zNjFOwG0v MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh3MUO5O|YoRjF6NUGzPVc3RC:jPh?=
KB3-1 M{fVeGN6fG:2b4jpZ4l1gSCjc4PhfS=> MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRlMuOSClZXzsd{BjgSCPVGSgcYV1cG:mLDDJR|UxKD1iMD62PEDPxE1w MoDCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5N{G5N|AoRjF6N{exPVMxRC:jPh?=
KBH5.0 MlPvR5l1d3SxeHnjbZR6KGG|c3H5 M1zwdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDUDVwMDDj[YxteyCkeTDNWHQhdWW2aH;kMEBKSzVyIE2gO{41KM7:TT6= NF33O2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe3NVk{OCd-MUi3O|E6OzB:L3G+
KBV1 NVnvOWczS3m2b4TvfIlkcXS7IHHzd4F6 NEj4V|hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSlZzIHPlcIx{KGK7IF3UWEBu\XSqb3SsJGlEPTBiPTC0NEDPxE1w MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd5MUmzNEc,OTh5N{G5N|A9N2F-
MDA-MB-435 MWjDfZRwfG:6aXPpeJkh[XO|YYm= MUK3NkBpenN? NF6zTVZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFM2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxMlE1KM7:TT6= M3fvU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{exNVg{Lz5{MEO3NVE5OzxxYU6=
A549 MV\DfZRwfG:6aXPpeJkh[XO|YYm= MVK3NkBpenN? MmnKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOE43OSEQvF2u M3m2RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{exNVg{Lz5{MEO3NVE5OzxxYU6=
LoVo NHzOZ|BEgXSxdH;4bYNqfHliYYPzZZk> NVfMRmpDPzJiaILz M3zqS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxwXm9iY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFQvQTlizszNMi=> NVPkXXRERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzO|EyQDNpPkKwN|cyOTh|PD;hQi=>
A549 NXvsO4g4S3m2b4TvfIlkcXS7IHHzd4F6 MWOzJIRigXN? NXXMR2Z2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hPi52IN88UU4> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODl2MkS5NEc,OjB7NEK0PVA9N2F-
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A549 NVrKUYVqS3m2b4TvfIlkcXS7IHHzd4F6 MoG0O|IhcHK| MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHPvcI9zcW2ndILpZ{Bie3OjeTygTWM2OCB;IEmuOFgh|ryPLh?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl7NEi0O{c,OjZ7OUS4OFc9N2F-
KB MUjDfZRwfG:6aXPpeJkh[XO|YYm= M4XvWFczKGi{cx?= M{DrSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHPvcI9zcW2ndILpZ{Bie3OjeTygTWM2OCB;IEmuPFI5KM7:TT6= M4jHPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUm0PFQ4Lz5{Nkm5OFg1PzxxYU6=
KB M{\FN2N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml7jO|IhcHK| NHTNeYpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NEA:KDdwOUmg{txONg>? NX7XbFEyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFU6OTJpPkK4Nlg2QTF{PD;hQi=>
A549 NILwPYFEgXSxdH;4bYNqfHliYYPzZZk> M2rBb|czKGi{cx?= NIXKRmdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxKD1iOD6zJO69VS5? Mn3GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEW5NVIoRjJ6Mki1PVEzRC:jPh?=
MCF7 MUjDfZRwfG:6aXPpeJkh[XO|YYm= NF7FSZk4OiCqcoO= MoX0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NEA:KDFzLkOg{txONg>? M3SxVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6Mki1PVEzLz5{OEK4OVkyOjxxYU6=
MDA-MB-231 MnztR5l1d3SxeHnjbZR6KGG|c3H5 M33OdlczKGi{cx?= NYDacY9bS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NEA:KDF3Lk[g{txONg>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6NUmxNkc,Ojh{OEW5NVI9N2F-
HCT116 MnfzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M1vPWFczKGi{cx?= NFnUT4ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOk4{KM7:TT6= NGH2b4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO1NVU6OCd-MkizOVE2QTB:L3G+
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A549 NIDjWZdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mnn5O|IhcHK| MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDJyIN88UU4> M{X0R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{WxOVkxLz5{OEO1NVU6ODxxYU6=
KB NH:4PHhEgXSxdH;4bYNqfHliYYPzZZk> M2f2bVczKGi{cx?= NH3UdZNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gO{46QSEQvF2u NY\LRWFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PFk5QTFpPkK4O|g6QDlzPD;hQi=>
A549 NIfoNIlEgXSxdH;4bYNqfHliYYPzZZk> NUWzSlZrPzJiaILz NHLUW5NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUA5NjNzIN88UU4> NF7qeG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe4PVg6OSd-Mki3PFk5QTF:L3G+
MCF7 M1rs[GN6fG:2b4jpZ4l1gSCjc4PhfS=> NUm4e5BNPzJiaILz NUS1bJpoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOTFwM{Kg{txONg>? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd6OUi5NUc,Ojh5OEm4PVE9N2F-
MDA-MB-231 NH;CXXhEgXSxdH;4bYNqfHliYYPzZZk> MmCxO|IhcHK| MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSBzNT61OkDPxE1w M1vOWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{i5PFkyLz5{OEe4PVg6OTxxYU6=
KB NYXnR2VKS3m2b4TvfIlkcXS7IHHzd4F6 MnfiO|IhcHK| MnjKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2Ih[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IEeuPVkh|ryPLh?= M2fSUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUK3O|kxLz5{OEmyO|c6ODxxYU6=
A549 NWjVdod7S3m2b4TvfIlkcXS7IHHzd4F6 MYC3NkBpenN? NFn0TGxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUA5NjNizszNMi=> MoT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7Mke3PVAoRjJ6OUK3O|kxRC:jPh?=
MCF7 M{jESGN6fG:2b4jpZ4l1gSCjc4PhfS=> MVi3NkBpenN? NEmxTpdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUAyOS5|IN88UU4> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl{N{e5NEc,Ojh7Mke3PVA9N2F-
MDA-MB-231 NV;3[2dnS3m2b4TvfIlkcXS7IHHzd4F6 NXrtOZd[PzJiaILz MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSBzNT62JO69VS5? M1:wbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUK3O|kxLz5{OEmyO|c6ODxxYU6=
Maver2 NGrrTY9CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1nFW|czKGi{cx?= NYfnWph4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNZZZmejJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvPzRizszNMi=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF3MEOzOUc,OjlzNUCzN|U9N2F-
NB4 MVXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MUC3NkBpenN? M1jzOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlK0JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzIN88UU4> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF3MEOzOUc,OjlzNUCzN|U9N2F-
Capan1 NEPtdm5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mlr2O|IhcHK| NEHXdIRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPhdIFvOSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNU42KM7:TT6= M{XkNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUWwN|M2Lz5{OUG1NFM{PTxxYU6=
NCI-H460 NXfXdJg1SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MXu3NkBpenN? MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCyMlQh|ryPLh?= NUDrWGFMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOVA{OzVpPkK5NVUxOzN3PD;hQi=>
DU145 NVvIV|RLSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVjE[4hUPzJiaILz MkTQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMj64JO69VS5? NXnRO2dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOVA{OzVpPkK5NVUxOzN3PD;hQi=>
A2780 MmK0RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? Mn[5O|IhcHK| MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB|Lkig{txONg>? NWrVOlByRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOVA{OzVpPkK5NVUxOzN3PD;hQi=>
HepG2 MWnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVe3NkBpenN? M1XBTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IESg{txONg>? NXvJdll1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOVA{OzVpPkK5NVUxOzN3PD;hQi=>
A431 M2j0NGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MUm3NkBpenN? NF\F[WJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0N|Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IESuNUDPxE1w MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF3MEOzOUc,OjlzNUCzN|U9N2F-
U2932 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NH:2fZk4OiCqcoO= MlTJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkmzNkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iND60JO69VS5? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF3MEOzOUc,OjlzNUCzN|U9N2F-
HT-29 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{Pi[VczKGi{cx?= MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB2Lkig{txONg>? NEnQelg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG1NFM{PSd-MkmxOVA{OzV:L3G+
HeLa NHXvSodCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Ml;tO|IhcHK| NF7MOmJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IEWuPEDPxE1w NFzlcm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG1NFM{PSd-MkmxOVA{OzV:L3G+
MM487 MmXMRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4P1d|ExKHWP MXG3NkBpenN? NX32fJk5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVQ5PyClZXzsd{BifCBzMDD1UUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5JJJmdGG2aY\lJJRwKGOxboTyc4wtKEmFNUCgQUA6NjRizszNMi=> NILyWYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG1NFM{PSd-MkmxOVA{OzV:L3G+
MM432 NV;L[ZRnSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NFrETnoyOCC3TR?= NH;6ZZU4OiCqcoO= NI\vZoxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3NOFMzKGOnbHzzJIF1KDFyIIXNJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmgdoVt[XSrdnWgeI8h[2:wdILvcEwhUUN3MDC9JFExKM7:TT6= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF3MEOzOUc,OjlzNUCzN|U9N2F-
A2780/DX Mlj2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUC3NkBpenN? MofvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NE9FYCClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNlAvOSEQvF2u NVzLeIttRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOVA{OzVpPkK5NVUxOzN3PD;hQi=>
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SK-N-MC MYrxTHRUKGG|c3H5 MlyydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NF;HWlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 M2j3V5FJXFNiYYPzZZk> NU\MUnJyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MoG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NF;xdFZyUFSVIHHzd4F6 Mln3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| NUW4c5F4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 NFjReJFyUFSVIHHzd4F6 NIjS[WVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= M1j4SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NHfwdYNyUFSVIHHzd4F6 Ml3IdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUmIyPjR|IHPlcIx{ M3X6[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NFWwUoFyUFSVIHHzd4F6 NH7IO4dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy| M2rUS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32 NGTlWnlyUFSVIHHzd4F6 MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 M{Toe5FJXFNiYYPzZZk> NVzXV4hVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? MnHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NHLROVRyUFSVIHHzd4F6 MlHBdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ M3;TOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 NWr3R3RmeUiWUzDhd5NigQ>? M3\4bJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KE:{dHjv[49v[WxiM1Sgeoli[mmuaYT5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M2XMd|xiKHSjcnfleF0oZ2KuYX7rK{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
In vivo In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. [5] A single dose of Irinotecan significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver. Concomitantly, the Irinotecan-treated group shows significantly higher amounts of DNA strand breaks in colon mucosa cells compared to the control group. [6]

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: LoVo and HT-29 cells
  • Concentrations: 0 μM -100 μM
  • Incubation Time: 48 hours
  • Method:

    Exponentially growing cells (LoVo and HT-29 cells) are seeded in 20 cm2 Petri dishes with an optimal cell number for each cell line (2 × 104 for LoVo cells, 105 for HT-29 cells). They are treated 2 days later with increasing concentrations of Irinotecan or SN-38 for one cell doubling time (24 hours for LoVo cells, 40 hours for HT-29 cells). After washing with 0.15 M NaCl, the cells are further grown for two doubling times in normal medium, detached from the support with trypsin-EDTA and counted in a hemocytometer. The IC50 values are then estimated as the Irinotecan or SN-38 concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinotecan or SN-38.


    (Only for Reference)
Animal Research:

[5]

- Collapse
  • Animal Models: Female nude mice with COLO 320 and WiDr xenografts.
  • Dosages: 20 mg/kg
  • Administration: Intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 677.18
Formula

C33H38N4O6.HCl.3H2O

CAS No. 136572-09-3
Storage powder
in solvent
Synonyms N/A
Smiles CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID