SN-38

Catalog No.S4908 Synonyms: NK012

For research use only.

SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.

SN-38 Chemical Structure

CAS No. 86639-52-3

Selleck's SN-38 has been cited by 45 publications

Purity & Quality Control

Choose Selective ADC Cytotoxin Inhibitors

Biological Activity

Description SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
Targets
Topo I [1]
(Cell-free assay)
In vitro

SN-38, a biological active metabolite of irinotecan hydrochloride (CPT-11). SN-38 causes the strongest inhibition of DNA topoisomerase I, followed by CPT and then CPT-11. CPT-11 dose dependently shifts the position of relaxed DNA in the direction of nicked DNA, but SN-38 and CPT shows no effect on the position of relaxed DNA. SN-38 dose-dependently and time-dependently inhibit DNA synthesis. Respective IC50 values of SN-38, in DNA synthesis is 0.077 μM. The inhibitory effect of SN-38 on RNA synthesis is less than that on DNA synthesis and it does not inhibit protein synthesis. SN-38 caused frequent DNA single-strand breaks in P388 cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human DU145 prostate cell line M3TNXXBzd2yrZnXyZZRqd25iYYPzZZk> MmnyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBxem:|dHH0[UBk\WyuIHzpcoUtKEmFNUC9NVMhdk1? MnzFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB2OUiyNVYoRjFyNEm4NlE3RC:jPh?=
human MCF-7 breast cell line MlH6VJJwdGmoZYLheIlwdiCjc4PhfS=> NHTYT4dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSk04KGK{ZXHzeEBk\WyuIHzpcoUtKEmFNUC9NE4{PyEQvF2= MljuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB2OUiyNVYoRjFyNEm4NlE3RC:jPh?=
human SKOV-3 ovarian cell line MmjEVJJwdGmoZYLheIlwdiCjc4PhfS=> MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[tN{BwfmG{aXHuJINmdGxibHnu[UwhUUN3ME2wMlczKM7:TR?= NXXtNIdoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUC0PVgzOTZpPkGwOFk5OjF4PD;hQi=>
human breast cancer cell line (SK-BR-3) MmniR5l1d3SxeHnjxsBie3OjeR?= Mn3YTY4hXmm2cn:gZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmViKGPLMWJTNTNrLDDJR|UxRTRibl2= MoOwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF|M{S1OlkoRjFzM{O0OVY6RC:jPh?=
human lung cancer cell line (H128) M2L1cGN6fG:2b4jpZ:Kh[XO|YYm= NUf1XGE1UW5iVnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdHWwZzDjZY5k\XJiY3XscEBtcW6nIDjINVI5MSxiSVO1NF03KG6P M{n2U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzM{O0OVY6Lz5zMUOzOFU3QTxxYU6=
human stomach cancer cell line (MKN45) NUjQToU4S3m2b4TvfIlkyqCjc4PhfS=> M2DpbmlvKF[rdILvJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJN1d22jY3igZ4Fv[2W{IHPlcIwhdGmwZTCoUWtPPDVrLDDJR|UxRThibl2= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTN|NEW2PUc,OTF|M{S1Olk9N2F-
human ovarian cancer cell line (SK-OV-3) NFrZRXBEgXSxdH;4bYPDqGG|c3H5 MYrJckBXcXS{bzDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDveoFzcWGwIHPhcoNmeiClZXzsJIxqdmViKGPLMW9XNTNrLDDJR|UxRTFzIH7N M{K4ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzM{O0OVY6Lz5zMUOzOFU3QTxxYU6=
human colon cancer cell line (WiDr) NHXOOHVEgXSxdH;4bYPDqGG|c3H5 NXvDfYk2UW5iVnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4h[2:ub36gZ4Fv[2W{IHPlcIwhdGmwZTCoW4lFeiluIFnDOVA:OTRibl2= NF:xTFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUOzOFU3QSd-MUGzN|Q2Pjl:L3G+
human lung cancer cell line (A549) NFz6dGlEgXSxdH;4bYPDqGG|c3H5 NWjmbnJ3UW5iVnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdHWwZzDjZY5k\XJiY3XscEBtcW6nIDjBOVQ6MQ>? NX;uTJNkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUGzN|Q2PjlpPkGxN|M1PTZ7PD;hQi=>
NSCLC-H460 M{XNWWN6fG:2b4jpZ:Kh[XO|YYm= NI\NNVREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBvd25vc33hcIwu[2WubDDseY5oKGOjcnPpco9u[SClZXzsJIxqdmViSES2NEApVlOFTFOtTFQ3OCluIFnDOVA:QDBibl2= M{XvcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzNU[zPVI2Lz5zMUW2N|kzPTxxYU6=
PC-3 carcinoma cell line MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlfUR49v[2WwdILheIlwdiC{ZYH1bZJm\CC2bzDpcohq[mm2IHfyc5d1cCCxZjDoeY1idiCycn;zeIF1\SCSQz2zJINiemOrbn;tZUBk\WyuIHzpcoUtKEmFNUC9N|UvPiCwTR?= NF73SY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUS1OFI{OCd-MUW0OVQzOzB:L3G+
human HCT116 colon cancer cell line MlfMSpVv[3Srb36gZZN{[Xl? NFvuNZJKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiCKQ2SxNVYh[2:ub36gZ4Fv[2W{IHPlcIwhdGmwZTygTWM2OD15IH7N NYTaWmF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4NFg1PTZpPkG1PFA5PDV4PD;hQi=>
human Bel-7402 liver cancer cell line MWHGeY5kfGmxbjDhd5NigQ>? M4rxSWlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKEKnbD23OFAzKGyrdnXyJINidmOncjDj[YxtKGyrbnWsJGlEPTB;Mz6xPUDPxE1? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPThyOES1Okc,OTV6MEi0OVY9N2F-
human tumor HL60 cell-line MWfGeY5kfGmxbjDhd5NigQ>? M{XqVFMh\GG7cx?= NUnIWlBNUW5vdnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIZweiCqdX3hckB1fW2xcjDIUFYxKGOnbHytcIlv\SC5YYOg[IV1\XKvaX7l[EB2e2mwZzDTVmIh[XO|YYmgZYZ1\XJiMzDkZZl{KG:oIHnuZ5Vj[XSrb36sJGlEPTB;MUmgcm0> NWXhe2JORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW5NVM6QTZpPkG1PVE{QTl4PD;hQi=>
human H460 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TUbmlvcGmkaYTpc44hd2ZiaIXtZY4hUDR4MDDj[YxtKGe{b4f0bEwhUUN3ME24NEBvVQ>? NYLxd5BYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[5NVM4ODZpPkG2PVE{PzB4PD;hQi=>
MDA-MB-435 MkDoSpVv[3Srb36gZZN{[Xl? NIPuXYhKdmirYnn0bY9vKGGpYXnud5QhVUSDLV3CMVQ{PSCVIHj1cYFvKGK{ZXHzeEBk[W6lZYKgZ4VtdHNiaX6geIhmKGGkc3XuZ4Uhd2ZiYXzieY1qdixiSVO1NEA:KDBwMEC1JO69VS5? NFi4UpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC1NlgxOid-MUGwOVI5ODJ:L3G+
MDA-MB-435 NHfKTldHfW6ldHnvckBie3OjeR?= NX7I[ZU{UW6qaXLpeIlwdiCjZ3HpcpN1KE2GQT3NRk01OzViUzDoeY1idiCkcnXhd5Qh[2GwY3XyJINmdGy|IHnuJJRp\SCycnXz[Y5k\SCxZjCzNEBu\y:vTDDIV2EtKEmFNUCgQUAxNjB3IN88UU4> NF36WXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC1NlgxOid-MUGwOVI5ODJ:L3G+
PC-6/SN2-5H NFLiNZJHfW6ldHnvckBie3OjeR?= NVO3[YozXFChVGLBUnNRV1KWRWK6JJVxfGGtZTDpckBu\W2kcnHu[UB3\XOrY3zlJIZzd21iUFOtOk9UVjJvNVigZ4VtdHNuIFvtJF0hPCEQvF2u NE\oUIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMU[4PFk5Oid-MUG2PFg6QDJ:L3G+
HT-29 M331RmZ2dmO2aX;uJIF{e2G7 NWnvVWkzUW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJJJmeXWrcnXkJIFo[Wmwc4SgTHQuOjliaIXtZY4h[2:ub36gZ4Fv[2W{IHPlcIx{NCCLQ{WwJF0hOC5yMkezJO69VS5? NGPq[Gs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMk[xO|kzPyd-MUK2NVc6Ojd:L3G+
SaoS2 Ml;vSpVv[3Srb36gZZN{[Xl? M4PHWXRRZ1SUQV7TVG9TXEWUOjDkdpVoKHKnc3nzeIFv[2VqSX3heIlvcWJibXXzfYxifGVrIHnuJGJEWlBvZYjwdoV{e2mwZzDTZY9UOiClZXzsd{whUUN3MDC9JFAvOTd4IN88UU4> NGjBS|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUC1PVg5OSd-MUWwOVk5QDF:L3G+
DU145 MV\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVK5OkBpenN? MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESXMUS1JINmdGy|IHHmeIVzKDl4IHjyd{whUUN3MDC9JFAvODB2IN88UU4> M{fnTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6Mke2NVQyLz5zOEK3OlE1OTxxYU6=
MIA PaCa MknhRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2SyVVk3KGi{cx?= NGW3OJFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRUBR[UOjIHPlcIx{KGGodHXyJFk3KGi{czygTWM2OCB;IECuNFA3KM7:TT6= NELUSYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEK3OlE1OSd-MUiyO|YyPDF:L3G+
HT29 NGfJbpFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4O5W|k3KGi{cx?= NYnWNlUxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWFI6KGOnbHzzJIFnfGW{IEm2JIhzeyxiSVO1NEA:KDBwMEGyJO69VS5? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ5NkG0NUc,OTh{N{[xOFE9N2F-
H460 MkjwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXvDeYJPOSCqch?= MmLCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKNE[wJINmdGy|IHHmeIVzKDFiaIKgc4Yh\HK3ZzDlfJBwe3W{ZTDt[YF{fXKnZDDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjJ{IN88UU4> NUPFXYVVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0NlQyOzNpPkG4OFI1OTN|PD;hQi=>
HT29 NXW2fllJSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3fzVVEhcHJ? NXXneoxESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWFI6KGOnbHzzJIFnfGW{IEGgbJIhd2ZiZIL1[{BmgHCxc4Xy[UBu\WG|dYLl[EBi\nSncjC3NkBpenNuIFnDOVAhRSByLk[3JO69VS5? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR{NEGzN{c,OTh2MkSxN|M9N2F-
HT29 MkHlRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MXyxJIhz M4HlUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRmNTWCCxdnXy[ZhxemW|c3nu[{BucXSxeHHueJJwdmVvcnXzbZN1[W62IHj1cYFvKEiWMkmgZ4VtdHNiYX\0[ZIhOSCqcjDv[kBlenWpIHX4dI9{fXKnIH3lZZN2emWmIHHmeIVzKDd{IHjyd{whUUN3MDC9JFEyNjVizszNMi=> NX\3NIpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0NlQyOzNpPkG4OFI1OTN|PD;hQi=>
H460 NVezRpNqS3m2b4TvfIlkcXS7IHHzd4F6 M{L5dGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGg1PjBiY3XscJMtKEmFNUCgQUAxNjJ{IN88UU4> NX\xbWpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0N|QyPTNpPkG4OFM1OTV|PD;hQi=>
A549 Mlf3R5l1d3SxeHnjbZR6KGG|c3H5 M4\UWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[nliU2LCJI1mfGixZDygTWM2OCB;IECuNFgh|ryPLh?= M1yzbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUi2PFA4Lz5zOEm4OlgxPzxxYU6=
HT-29 MoKwR5l1d3SxeHnjbZR6KGG|c3H5 M2jDWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGK7IGPSRkBu\XSqb3SsJGlEPTBiPTCwMlEzKM7:TT6= M2TDTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUi2PFA4Lz5zOEm4OlgxPzxxYU6=
PC6 MoDuRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M{HWUlYh\GG7cx?= MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFNjDj[YxteyClYYLyfYlv\yCyUlOgZYZ1\XJiNjDkZZl{NCCLQ{WwJF0hOC5yMEC0N{DPxE1w MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ3NEi0N{c,OTl{NUS4OFM9N2F-
HCT116 Mn3GRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2naOFMh\GG7cx?= MnnRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiMzDkZZl{NCCLQ{WwJF0hOC5yMEC1OUDPxE1w NF\DTWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK1OFg1Oyd-MUmyOVQ5PDN:L3G+
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NCI-H460 M1\jSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NHzkRlI{KGSjeYO= NHK1fYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPDZyIHPlcIx{KGGodHXyJFMh\GG7czygTWM2OCB;IECuNFA{OyEQvF2u M1TXelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkW0PFQ{Lz5zOUK1OFg1OzxxYU6=
BCRP MmfzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3zrclYh\GG7cx?= MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFNjDlfJBz\XO|aX7nJGJEWlBiY3XscJMh[W[2ZYKgOkBl[Xm|LDDJR|UxKD1iMD6wNFUyKM7:TT6= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ3NEi0N{c,OTl{NUS4OFM9N2F-
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colon cancer cells MlrCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWTub|h{PzJiaILz MVjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDjc4xwdiClYX7j[ZIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUCgQUAxNjB4NjFOwG0v M2PEU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEi0NFg6Lz5{MEi4OFA5QTxxYU6=
HT-29 M1;qUmN6fG:2b4jpZ4l1gSCjc4PhfS=> NH;RN4ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyxiSVO1NEA:KDBwMEC1PUDPxE1w MlfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2N{C4OlQoRjJzNEewPFY1RC:jPh?=
A549 M1PtZ2N6fG:2b4jpZ4l1gSCjc4PhfS=> NVz4[4FHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyxiSVO1NEA:KDBwMES3JO69VS5? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR5MEi2OEc,OjF2N{C4OlQ9N2F-
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DU145 NUXyTVg{S3m2b4TvfIlkcXS7IHHzd4F6 NIPnT|NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyxiSVO1NEA:KDBwMEOg{txONg>? Mn3vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3N{i1OFUoRjJ|NUe4OVQ2RC:jPh?=
HT-29 NVvtUopwS3m2b4TvfIlkcXS7IHHzd4F6 NXj6[INHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRvMkmgZ4VtdHNuIFnDOVAhRSByLkCzJO69VS5? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV5OEW0OUc,OjN3N{i1OFU9N2F-
L1210 M2XjdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFTPd3JEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBNOTJzMDDj[YxteyxiSVO1NEA:KDBwMESg{txONg>? NInld5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W3PFU1PSd-MkO1O|g2PDV:L3G+
DU145 NVq0eHJjS3m2b4TvfIlkcXS7IHHzd4F6 MmfJO|IhcHK| MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkGxJO69VS5? NF23b3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[yNlk5OSd-MkO2NlI6QDF:L3G+
DU145 Mlq5SpVv[3Srb36gZZN{[Xl? NYHCemdtOC5zIITvJFAvPSC3TR?= Ml7qNlQhcHK| NXS2bFAzUW6qaXLpeIlwdiCxZjDISGFEKGmwIHj1cYFvKESXMUS1JINmdGy|IHHzd4V{e2WmIHHzJJVxemWpdXzheIlwdiCxZjDwNlF4[WZzIHX4dJJme3Orb36gZZQhOC5zIITvJFAvPSC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ{Mkm4NUc,OjN4MkK5PFE9N2F-
A549 MWDDfZRwfG:6aXPpeJkh[XO|YYm= NGnx[nk{KGSjeYO= MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFMh\GG7czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjByMkeyJO69VS5? NFvJcpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWyPVg4OCd-MkS1Nlk5PzB:L3G+
HCT116 MUfDfZRwfG:6aXPpeJkh[XO|YYm= M1PO[VMh\GG7cx?= NYjtN4pNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEOg[IF6eyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlA{OSEQvF2u NEfjb5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWyPVg4OCd-MkS1Nlk5PzB:L3G+
HT-29 NX[0fmJmS3m2b4TvfIlkcXS7IHHzd4F6 M3z3XVMh\GG7cx?= MnS0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhOyCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwMUC2Olch|ryPLh?= NHvFNW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWyPVg4OCd-MkS1Nlk5PzB:L3G+
HCT116 MX\DfZRwfG:6aXPpeJkh[XO|YYm= MlLJR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{NCCLQ{WwJF0hOC5zNk[g{txONg>? NWK3T2lmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1Nlk5PzBpPkK0OVI6QDdyPD;hQi=>
MDA-MB-231 M17lfGN6fG:2b4jpZ4l1gSCjc4PhfS=> MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|LDDJR|UxKD1iMD6xO|Yh|ryPLh?= NXnIbIljRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1Nlk5PzBpPkK0OVI6QDdyPD;hQi=>
A549 NV\3W|VJS3m2b4TvfIlkcXS7IHHzd4F6 NIP4bpFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{NCCLQ{WwJF0hOC5{NUmg{txONg>? NGLre5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWyPVg4OCd-MkS1Nlk5PzB:L3G+
HEK293 MlfqR5l1d3SxeHnjbZR6KGG|c3H5 M3PrZ|czKGi{cx?= MoTnTY51emmwc3njJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUd3MDC9JFAvODB3IN88UU4> M4ryVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkeyNFU2Lz5{NUK3NlA2PTxxYU6=
HCT116 NIDOdZdEgXSxdH;4bYNqfHliYYPzZZk> MmK0O|IhcHK| M4W4dWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OCB;IECuNFA1OjhizszNMi=> NV62PGp3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|U{PTlpPkK1PFM2OzV7PD;hQi=>
HT-29 MVHDfZRwfG:6aXPpeJkh[XO|YYm= M{nuUFczKGi{cx?= NE\odlhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OCB;IECuNFE5PTRizszNMi=> MofKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{WzOVkoRjJ3OEO1N|U6RC:jPh?=
HCT15 MXLDfZRwfG:6aXPpeJkh[XO|YYm= M1n1eVczKGi{cx?= NYLL[oxoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUWgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IECuNFA5KM7:TT6= NEO1flE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C2NFc3OCd-MkewOlA4PjB:L3G+
U251 MnywR5l1d3SxeHnjbZR6KGG|c3H5 M2LsclczKGi{cx?= MkjFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVI2OSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5yMkGg{txONg>? NE\3PW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C2NFc3OCd-MkewOlA4PjB:L3G+
U87MG MmLUR5l1d3SxeHnjbZR6KGG|c3H5 M3LldVczKGi{cx?= NVrwcmQ5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTh5TVegZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IECuNFMh|ryPLh?= M33WZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5ME[wO|YxLz5{N{C2NFc3ODxxYU6=
HT-29 Ml;WR5l1d3SxeHnjbZR6KGG|c3H5 NV3jRVQ1PzJiaILz MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5yNUSg{txONg>? NVPtO3dCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewOlA4PjBpPkK3NFYxPzZyPD;hQi=>
MCF7 NYP1UIdyS3m2b4TvfIlkcXS7IHHzd4F6 NIHkSWo4OiCqcoO= MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjVzNTFOwG0v MoPzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyNkC3OlAoRjJ5ME[wO|YxRC:jPh?=
MDA-MB-231 MXLDfZRwfG:6aXPpeJkh[XO|YYm= NXnoUmFqPzJiaILz NYXRdWx{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOS57NzFOwG0v NYOxNZFtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewOlA4PjBpPkK3NFYxPzZyPD;hQi=>
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HCT116 M4O0WWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NEPwVlI4OiCqcoO= NVXYS4RCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvODByN{ig{txONg>? NFTibZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEGxOVQ6Oid-M{CxNVU1QTJ:L3G+
A549 MWnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4HjWFczKGi{cx?= NIPBVlNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IECuNFAyPjJizszNMi=> NIjXNXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEGxOVQ6Oid-M{CxNVU1QTJ:L3G+
MCF7 M3HKVmN6fG:2b4jpZ4l1gSCjc4PhfS=> Mo\JO|IhcHK| NXX4ZpNVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OCB;IECuNFAxOSEQvF2u Ml\NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzNkmwN|goRjNyMU[5NFM5RC:jPh?=
A549 MXnDfZRwfG:6aXPpeJkh[XO|YYm= NXzndWF7PzJiaILz MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> NHXjbHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG2PVA{QCd-M{CxOlkxOzh:L3G+
Assay
Methods Test Index PMID
Western blot p-Chk1 / Chk1 / Topo I 18509065
Growth inhibition assay Cell viability 25759163
In vivo After oral dosing, peak SN-38 concentrations occurrs within 1 h, and the The percent unbound SN-38 lactone in murine plasma at 1000 ng/mL is 3.4 +/- 0.67%, whereas at 100 ng/mL the percent unbound is 1.18 +/- 0.14%. SN-38 lactone AUCs in micebearing human neuroblastoma xenografts are greater than in nontumor-bearing animals. [2]

Protocol (from reference)

Kinase Assay:[1]
  • Topoisomerase I Assay:

    One unit (the minimum amount for full relaxation of 0.5 μg SV40 DNA under the conditions of this study) of topoisomerase I, 0.5 μL of the test compounds, and 0.5μg SV40 DNA are added sequentially to the reaction buffer, which is composed of 25 mM Tris-HCl (pH 7.5), 50 mM KC1, 5 mM MgCl2, 0.25 mM EDTA disodium salt, 0.25 mM dithiothreitol, 15μg /mL bovine serum albumin, and 5% glycerol. Then, the reaction mixture (50 μL) is incubated for 10 min at 37 °C, and the reaction is terminated by treatment with 7.5 μL of a solution consisting of 1% sodium dodecyl sulfate, 20 mM EDTA disodium salt, and 0.5 mg/mL proteinase K for an additional 30 min at 37°C. The samples are mixed with 5 μL of the loading buffer containing 10 mM Na2HPO4, 31.3% sucrose, and 0.3% bromophenol blue. Relaxed (form Ir) DNA is separated from supercoiled (form I) and nicked (form II) DNA by electrophoresis on 0.8% agarose gel at 50 mA and 20 V for 17 h in the presence of 2 μg/mL chloroquine, 10 mM EDTA, 30 mM NaH2PO4, and 36 Mm Tris-HCl (pH 7.8). After electrophoresis, the gel is stained with 0.05% ethidium bromide and photographed with UV light (302 nm). The amount of DNA is quantified using a densitometer.

Cell Research:[3]
  • Cell lines: A-172, U-87, and LA-567
  • Concentrations: 0 -1000 nM
  • Incubation Time: 48 h
  • Method: MTT assay

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 392.4
Formula

C22H20N2O5

CAS No. 86639-52-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05101096 Recruiting Drug: Sacituzumab Govitecan-hziy Advanced Solid Tumors or Triple-negative Breast Cancer Gilead Sciences October 20 2021 Phase 1|Phase 2
NCT04866641 Recruiting Drug: T-1201 Injection 100 mg Kit Advanced Solid Tumor Taivex Therapeutics Corporation June 24 2021 Phase 1
NCT04617522 Recruiting Drug: Sacituzumab Govitecan-hziy Advanced or Metastatic Solid Tumor|Liver Failure Gilead Sciences April 6 2021 Phase 1
NCT03995706 Recruiting Drug: Sacituzumab Govitecan Glioblastoma The University of Texas Health Science Center at San Antonio|Gilead Sciences July 17 2019 Early Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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