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 40 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 NFzt[XNRem:uaX\ldoF1cW:wIHHzd4F6 NVvPWpoySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSCycn;zeIF1\SClZXzsJIxqdmVuIFnDOVA:OTNibl2= M4\Fc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyNEm4NlE3Lz5zMES5PFIyPjxxYU6=
human MCF-7 breast cell line NW\jR3BNWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRj23JIJz\WG|dDDj[YxtKGyrbnWsJGlEPTB;MD6zO{DPxE1? M3PRS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyNEm4NlE3Lz5zMES5PFIyPjxxYU6=
human SKOV-3 ovarian cell line MorBVJJwdGmoZYLheIlwdiCjc4PhfS=> MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[tN{BwfmG{aXHuJINmdGxibHnu[UwhUUN3ME2wMlczKM7:TR?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODR7OEKxOkc,OTB2OUiyNVY9N2F-
human breast cancer cell line (SK-BR-3) MkLZR5l1d3SxeHnjxsBie3OjeR?= NX;Z[4FwUW5iVnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4h[nKnYYP0JINidmOncjDj[YxtKGyrbnWgLHNMNUKULUOpMEBKSzVyPUSgcm0> M2fhOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzM{O0OVY6Lz5zMUOzOFU3QTxxYU6=
human lung cancer cell line (H128) MYDDfZRwfG:6aXRCpIF{e2G7 M1PYemlvKF[rdILvJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIx2dmdiY3HuZ4VzKGOnbHygcIlv\SBqSEGyPEktKEmFNUC9OkBvVQ>? M{DheVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzM{O0OVY6Lz5zMUOzOFU3QTxxYU6=
human stomach cancer cell line (MKN45) MYTDfZRwfG:6aXRCpIF{e2G7 MWLJckBXcXS{bzDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDzeI9u[WOqIHPhcoNmeiClZXzsJIxqdmViKF3LUlQ2MSxiSVO1NF05KG6P M2\VT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzM{O0OVY6Lz5zMUOzOFU3QTxxYU6=
human ovarian cancer cell line (SK-OV-3) NEj6NZhEgXSxdH;4bYPDqGG|c3H5 MVnJckBXcXS{bzDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDveoFzcWGwIHPhcoNmeiClZXzsJIxqdmViKGPLMW9XNTNrLDDJR|UxRTFzIH7N NFnCOI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUOzOFU3QSd-MUGzN|Q2Pjl:L3G+
human colon cancer cell line (WiDr) M3LTUWN6fG:2b4jpZ:Kh[XO|YYm= NGDWSW9KdiCYaYTyc{BkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBkd2yxbjDjZY5k\XJiY3XscEBtcW6nIDjXbWRzMSxiSVO1NF0yPCCwTR?= MoXwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF|M{S1OlkoRjFzM{O0OVY6RC:jPh?=
human lung cancer cell line (A549) MYHDfZRwfG:6aXRCpIF{e2G7 NHTTXohKdiCYaYTyc{BkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBtfW6pIHPhcoNmeiClZXzsJIxqdmViKFG1OFkq MmnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF|M{S1OlkoRjFzM{O0OVY6RC:jPh?=
NSCLC-H460 NHnmepFEgXSxdH;4bYPDqGG|c3H5 NIrsVJVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBvd25vc33hcIwu[2WubDDseY5oKGOjcnPpco9u[SClZXzsJIxqdmViSES2NEApVlOFTFOtTFQ3OCluIFnDOVA:QDBibl2= MoflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF3NkO5NlUoRjFzNU[zPVI2RC:jPh?=
PC-3 carcinoma cell line NIPLeHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MomxR49v[2WwdILheIlwdiC{ZYH1bZJm\CC2bzDpcohq[mm2IHfyc5d1cCCxZjDoeY1idiCycn;zeIF1\SCSQz2zJINiemOrbn;tZUBk\WyuIHzpcoUtKEmFNUC9N|UvPiCwTR?= NHLOTGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUS1OFI{OCd-MUW0OVQzOzB:L3G+
human HCT116 colon cancer cell line M1:0b2Z2dmO2aX;uJIF{e2G7 MV7Jcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBJS1RzMU[gZ49td25iY3HuZ4VzKGOnbHygcIlv\SxiSVO1NF04KG6P NWewTndYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4NFg1PTZpPkG1PFA5PDV4PD;hQi=>
human Bel-7402 liver cancer cell line NXHvV25uTnWwY4Tpc44h[XO|YYm= MmnrTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4hSmWuLUe0NFIhdGm4ZYKgZ4Fv[2W{IHPlcIwhdGmwZTygTWM2OD1|LkG5JO69VQ>? NVn1emN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4NFg1PTZpPkG1PFA5PDV4PD;hQi=>
human tumor HL60 cell-line MWnGeY5kfGmxbjDhd5NigQ>? NHryZnk{KGSjeYO= NFr3SlBKdi24aYTyc{BqdmirYnn0c5J6KGOxbnPlcpRz[XSrb36g[o9zKGi3bXHuJJR2dW:{IFjMOlAh[2WubD3sbY5mKHejczDk[ZRmem2rbnXkJJV{cW6pIGPSRkBie3OjeTDh[pRmeiB|IHThfZMhd2ZiaX7jeYJifGmxbjygTWM2OD1zOTDuUS=> M3LYcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OUGzPVk3Lz5zNUmxN|k6PjxxYU6=
human H460 cell NIfheFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYfPbGk{UW6qaXLpeIlwdiCxZjDoeY1idiCKNE[wJINmdGxiZ4Lve5RpNCCLQ{WwQVgxKG6P NH;hO2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkmxN|cxPid-MU[5NVM4ODZ:L3G+
MDA-MB-435 Mly4SpVv[3Srb36gZZN{[Xl? MXnJcohq[mm2aX;uJIFo[Wmwc4SgUWRCNU2ELUSzOUBUKGi3bXHuJIJz\WG|dDDjZY5k\XJiY3XscJMhcW5idHjlJIFje2WwY3Wgc4Yh[WykdX3pckwhUUN3MDC9JFAvODB3IN88UU4> MoX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTFyNUK4NFIoRjFzMEWyPFAzRC:jPh?=
MDA-MB-435 NGfsb3hHfW6ldHnvckBie3OjeR?= MlftTY5pcWKrdHnvckBi\2GrboP0JG1FSS2PQj20N|UhWyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIx{KGmwIITo[UBxemW|ZX7j[UBw\iB|MDDt[{9uVCCKU1GsJGlEPTBiPTCwMlA2KM7:TT6= NGLTXow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC1NlgxOid-MUGwOVI5ODJ:L3G+
PC-6/SN2-5H MWTGeY5kfGmxbjDhd5NigQ>? M1HrUHRRZ1SUQV7TVG9TXEWUOjD1dJRic2ViaX6gcYVu[nKjbnWgeoV{cWOuZTDmdo9uKFCFLU[vV24zNTWKIHPlcIx{NCCNbTC9JFQh|ryPLh?= NYnVT2xzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG2PFg6QDJpPkGxOlg5QTh{PD;hQi=>
HT-29 MVrGeY5kfGmxbjDhd5NigQ>? NXmzS4d4UW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJJJmeXWrcnXkJIFo[Wmwc4SgTHQuOjliaIXtZY4h[2:ub36gZ4Fv[2W{IHPlcIx{NCCLQ{WwJF0hOC5yMkezJO69VS5? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZzN{myO{c,OTJ4MUe5Nlc9N2F-
SaoS2 NEnYWmJHfW6ldHnvckBie3OjeR?= MYrUVH9VWkGQU2DPVnRGWjpiZIL1[{Bz\XOrc4ThcoNmMEmvYYTpcoljKG2nc4nsZZRmMSCrbjDCR3JRNWW6cILld5NqdmdiU3HvV|Ih[2WubIOsJGlEPTBiPTCwMlE4PiEQvF2u Mki3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVyNUm4PFEoRjF3MEW5PFgyRC:jPh?=
DU145 NF\OT41CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVPBdmFwQTZiaILz MmTMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBk\WyuczDh[pRmeiB7NjDodpMtKEmFNUCgQUAxNjByNDFOwG0v NUjtNopTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyO|YyPDFpPkG4Nlc3OTRzPD;hQi=>
MIA PaCa MXLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MmPSPVYhcHK| M3nQVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVnBJHBiS2FiY3XscJMh[W[2ZYKgPVYhcHK|LDDJR|UxKD1iMD6wNFYh|ryPLh?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ5NkG0NUc,OTh{N{[xOFE9N2F-
HT29 MoW3RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? Mn3yPVYhcHK| M1X6NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGSyPUBk\WyuczDh[pRmeiB7NjDodpMtKEmFNUCgQUAxNjBzMjFOwG0v MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ5NkG0NUc,OTh{N{[xOFE9N2F-
H460 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NHTLb4cyKGi{ MmC4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKNE[wJINmdGy|IHHmeIVzKDFiaIKgc4Yh\HK3ZzDlfJBwe3W{ZTDt[YF{fXKnZDDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjJ{IN88UU4> M4Hw[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEK0NVM{Lz5zOESyOFE{OzxxYU6=
HT29 M1noPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MYGxJIhz NEjDN4dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUNlkh[2WubIOgZYZ1\XJiMTDodkBw\iCmcoXnJIV5eG:|dYLlJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyxiSVO1NEA:KDBwNkeg{txONg>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR{NEGzN{c,OTh2MkSxN|M9N2F-
HT29 NXnjO5dUSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NV3vO5lrOSCqch?= NX7qWFhmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBDS1KSIH;2[ZJmgHC{ZYPzbY5oKG2rdH;4ZY51em:wZT3y[ZNqe3SjboSgbJVu[W5iSGSyPUBk\WyuczDh[pRmeiBzIHjyJI9nKGS{dXeg[Zhxd3O3cnWgcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{NCCLQ{WwJF0hOTFwNTFOwG0v MmnPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh2MkSxN|MoRjF6NEK0NVM{RC:jPh?=
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A549 MofIR5l1d3SxeHnjbZR6KGG|c3H5 MmHIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{BjgSCVUlKgcYV1cG:mLDDJR|UxKD1iMD6wPEDPxE1w Mor1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7OE[4NFcoRjF6OUi2PFA4RC:jPh?=
HT-29 MXLDfZRwfG:6aXPpeJkh[XO|YYm= NEfNSnBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCkeTDTVmIhdWW2aH;kMEBKSzVyIE2gNE4yOiEQvF2u M1q0RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUi2PFA4Lz5zOEm4OlgxPzxxYU6=
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HCT116 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGPGWWM{KGSjeYO= MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB|IHThfZMtKEmFNUCgQUAxNjByMEW1JO69VS5? M4TFT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkW0PFQ{Lz5zOUK1OFg1OzxxYU6=
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NCI-H460 NX20e45uSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MV[zJIRigXN? MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFYxKGOnbHzzJIFnfGW{IEOg[IF6eyxiSVO1NEA:KDBwMECzN{DPxE1w M{TxeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkW0PFQ{Lz5zOUK1OFg1OzxxYU6=
BCRP MYHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MWi2JIRigXN? MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFNjDlfJBz\XO|aX7nJGJEWlBiY3XscJMh[W[2ZYKgOkBl[Xm|LDDJR|UxKD1iMD6wNFUyKM7:TT6= NUnWOotURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOVQ5PDNpPkG5NlU1QDR|PD;hQi=>
KB3-1 NUPPXZBRS3m2b4TvfIlkcXS7IHHzd4F6 MUe0JIRigXN? M{T6SGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDOy1zIHPlcIx{KGGodHXyJFQh\GG7czDifUBOXFRibXX0bI9lNCCLQ{WwJF0hOC5yMESg{txONg>? MkfhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl|MEOzNFYoRjF7M{CzN|A3RC:jPh?=
KBV1 Mnn1R5l1d3SxeHnjbZR6KGG|c3H5 NWXEbXRPPCCmYYnz NXH6W4c1S3m2b4TvfIlkcXS7IHHnZYlve3RiTVTSNUBwfmW{ZYjwdoV{e2mwZzDoeY1idiCNQm[xJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCPVGSgcYV1cG:mLDDJR|UxKD1iMD6wOFYh|ryPLh?= NWW1RYtGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmzNFM{ODZpPkG5N|A{OzB4PD;hQi=>
KBH5.0 MlTaR5l1d3SxeHnjbZR6KGG|c3H5 MVW0JIRigXN? NXfDd3BrS3m2b4TvfIlkcXS7IHHnZYlve3RiQlPSVEBwfmW{ZYjwdoV{e2mwZzDoeY1idiCNQli1MlAh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IF3UWEBu\XSqb3SsJGlEPTBiPTCwMlMh|ryPLh?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTNyM{OwOkc,OTl|MEOzNFY9N2F-
NCI-H460 MkTwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUKxJIhz NF3JdZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPDZyIHPlcIx{KGGodHXyJJNpd3K2IITldo0h\Xiyb4P1doUh\m:{IEGgbJIhdWWjc4Xy[YQh[W[2ZYKgO|IhcHK|IHnuJIRzfWdvZoLl[UBu\WSrdX2sJGlEPTBiPTCwMlE{KM7:TT6= MlPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3M{C3NlAoRjF7NUOwO|IxRC:jPh?=
A549/ATCC MY\BcpRqfHWvb4KgZZN{[Xl? NV\FWWpSSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gRVU1QS:DVFPDJINmdGy|IHL5JHNTSiCvZYToc4QtKEmFNUCgQUAxNjB6ODFOwG0v NH3GU3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUW0NVQ5Oyd-MUm1OFE1QDN:L3G+
HT-29 NWTLeYZ3SW62aYT1cY9zKGG|c3H5 M4nNbWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIJ6KFOUQjDt[ZRpd2RuIFnDOVAhRSByLkG3JO69VS5? M{[1PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUSxOFg{Lz5zOUW0NVQ5OzxxYU6=
gastric cancer cells M2PBPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX:3NkBpenN? MYnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDnZZN1emmlIHPhcoNmeiClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NEA:KDBwME[2JO69VS5? MnGwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OESwPFkoRjJyOEi0NFg6RC:jPh?=
lung cancer cells M2LB[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUX5fJJTPzJiaILz MljkS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gcJVv\yClYX7j[ZIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUCgQUAxNjB4NjFOwG0v MnjRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OESwPFkoRjJyOEi0NFg6RC:jPh?=
colon cancer cells NGLIUXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVi3NkBpenN? NFPGZ3NIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBkd2yxbjDjZY5k\XJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVAhRSByLkC2OkDPxE1w M4PFclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEi0NFg6Lz5{MEi4OFA5QTxxYU6=
HT-29 M2PzR2N6fG:2b4jpZ4l1gSCjc4PhfS=> MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{whUUN3MDC9JFAvODB3OTFOwG0v MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR5MEi2OEc,OjF2N{C4OlQ9N2F-
A549 MnvGR5l1d3SxeHnjbZR6KGG|c3H5 NYjBVo9vS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyxiSVO1NEA:KDBwMES3JO69VS5? MmL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2N{C4OlQoRjJzNEewPFY1RC:jPh?=
PC3 MYDDfZRwfG:6aXPpeJkh[XO|YYm= NGTo[484OiCqcoO= NUX1em5OS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGW6cILld5NqdmdiYXzwbIE2[mW2YUOgbY51\We{aX6gZZN{\XO|ZXSgZZMh[2WubDDzeZJ3cX[jbDDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD6wNFI3KM7:TT6= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl3OUK0Okc,OjJ7NUmyOFY9N2F-
A2780 NXG5SJFNS3m2b4TvfIlkcXS7IHHzd4F6 M3roSVczKGi{cx?= MnfvR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMhd3[ncnX4dJJme3OrbnegZYxxcGF3YnX0ZVMhcW62ZXfybY4h[XO|ZYPz[YQh[XNiY3XscEB{fXK4aY\hcEBi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE4xODlizszNMi=> NUO4XZZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5OVkzPDZpPkKyPVU6OjR4PD;hQi=>
DU145 M1;yRWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{whUUN3MDC9JFAvODNizszNMi=> NX;iUWxnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1O|g2PDVpPkKzOVc5PTR3PD;hQi=>
HT-29 M1qy[2N6fG:2b4jpZ4l1gSCjc4PhfS=> NEHXboJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyxiSVO1NEA:KDBwMEOg{txONg>? NV;ZVmpuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1O|g2PDVpPkKzOVc5PTR3PD;hQi=>
L1210 M3zqRmN6fG:2b4jpZ4l1gSCjc4PhfS=> MnHKR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgUFEzOTBiY3XscJMtKEmFNUCgQUAxNjB2IN88UU4> M2fOblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUe4OVQ2Lz5{M{W3PFU1PTxxYU6=
DU145 NHzRSoxEgXSxdH;4bYNqfHliYYPzZZk> NHntdVM4OiCqcoO= M3HVO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNVEh|ryPLh?= MlvuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MkK5PFEoRjJ|NkKyPVgyRC:jPh?=
DU145 NWTQSIlpTnWwY4Tpc44h[XO|YYm= MmPVNE4yKHSxIECuOUB2VQ>? NXewXHpZOjRiaILz M17VUGlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBFXTF2NTDj[YxteyCjc4Pld5Nm\CCjczD1dJJm\3WuYYTpc44hd2ZicEKxe4FnOSCneIDy[ZN{cW:wIHH0JFAvOSC2bzCwMlUhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NHjOO|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[yNlk5OSd-MkO2NlI6QDF:L3G+
A549 MVzDfZRwfG:6aXPpeJkh[XO|YYm= MofSN{Bl[Xm| NVnoW4tjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB|IHThfZMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD6wNFI4OiEQvF2u MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV{OUi3NEc,OjR3Mkm4O|A9N2F-
HCT116 M{TMbmN6fG:2b4jpZ4l1gSCjc4PhfS=> MlHwN{Bl[Xm| M1X2cmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB|IHThfZMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD6wN|Eh|ryPLh?= NV\PSII1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1Nlk5PzBpPkK0OVI6QDdyPD;hQi=>
HT-29 MmLFR5l1d3SxeHnjbZR6KGG|c3H5 NU\GSHg5OyCmYYnz MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA{KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5zME[2O{DPxE1w MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV{OUi3NEc,OjR3Mkm4O|A9N2F-
HCT116 NF\2cI9EgXSxdH;4bYNqfHliYYPzZZk> NUTqfHRIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|LDDJR|UxKD1iMD6xOlYh|ryPLh?= M1vublxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUK5PFcxLz5{NEWyPVg4ODxxYU6=
MDA-MB-231 NF3xcphEgXSxdH;4bYNqfHliYYPzZZk> MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|LDDJR|UxKD1iMD6xO|Yh|ryPLh?= NFnFOpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWyPVg4OCd-MkS1Nlk5PzB:L3G+
A549 NV\oOnRFS3m2b4TvfIlkcXS7IHHzd4F6 M334TWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMtKEmFNUCgQUAxNjJ3OTFOwG0v MoPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3Mkm4O|AoRjJ2NUK5PFcxRC:jPh?=
HEK293 MUnDfZRwfG:6aXPpeJkh[XO|YYm= Mn;lO|IhcHK| M1uxZ2lvfHKrboPpZ{BkgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmJNUCgQUAxNjByNTFOwG0v MlnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{KwOVUoRjJ3MkeyNFU2RC:jPh?=
HCT116 Ml3yR5l1d3SxeHnjbZR6KGG|c3H5 M4W1elczKGi{cx?= MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFnDOVAhRSByLkCwOFI5KM7:TT6= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NUO1PUc,OjV6M{WzOVk9N2F-
HT-29 M4G2O2N6fG:2b4jpZ4l1gSCjc4PhfS=> NVm5UVBGPzJiaILz MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NEA:KDBwMEG4OVQh|ryPLh?= M{nJWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO1N|U6Lz5{NUizOVM2QTxxYU6=
HCT15 MXXDfZRwfG:6aXPpeJkh[XO|YYm= NVLG[pRWPzJiaILz NWXBUWlLS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUWgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IECuNFA5KM7:TT6= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB4MEe2NEc,OjdyNkC3OlA9N2F-
U251 M3TaNmN6fG:2b4jpZ4l1gSCjc4PhfS=> MUC3NkBpenN? NGLNSoFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWOjVzIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkCyNUDPxE1w MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB4MEe2NEc,OjdyNkC3OlA9N2F-
U87MG MojRR5l1d3SxeHnjbZR6KGG|c3H5 M4KyXlczKGi{cx?= NF\OOGpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWQDePRzDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD6wN{DPxE1w MlHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyNkC3OlAoRjJ5ME[wO|YxRC:jPh?=
HT-29 M2m1WGN6fG:2b4jpZ4l1gSCjc4PhfS=> MVS3NkBpenN? NIS5bpNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD6wOVQh|ryPLh?= M1Phe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5ME[wO|YxLz5{N{C2NFc3ODxxYU6=
MCF7 M4joPWN6fG:2b4jpZ4l1gSCjc4PhfS=> NE\CcVI4OiCqcoO= M4LueWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwNUG1JO69VS5? NXvPZpJJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewOlA4PjBpPkK3NFYxPzZyPD;hQi=>
MDA-MB-231 M3z5RWN6fG:2b4jpZ4l1gSCjc4PhfS=> MoHkO|IhcHK| NWD2cW04S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOS57NzFOwG0v M4LjVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5ME[wO|YxLz5{N{C2NFc3ODxxYU6=
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HCT116 NFu2fXVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NELNfoQ4OiCqcoO= MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD6wNFA4QCEQvF2u NVLRUotYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxNVU1QTJpPkOwNVE2PDl{PD;hQi=>
A549 MYPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{[zdVczKGi{cx?= Mn3TRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkCwNVYzKM7:TT6= MlO1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzMUW0PVIoRjNyMUG1OFkzRC:jPh?=
MCF7 MoTQR5l1d3SxeHnjbZR6KGG|c3H5 M1vUUlczKGi{cx?= NYPEbJk3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OCB;IECuNFAxOSEQvF2u NHfTZm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG2PVA{QCd-M{CxOlkxOzh:L3G+
A549 MV7DfZRwfG:6aXPpeJkh[XO|YYm= NEjoeHk4OiCqcoO= MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> NIGwbY49[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
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 21 mg/mL
(53.51 mM)
Water Insoluble
Ethanol Insoluble

* 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 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 2022-01-17)

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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