SN-38

For research use only.

Catalog No.S4908 Synonyms: NK012

35 publications

SN-38 Chemical Structure

CAS No. 86639-52-3

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.

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Selleck's SN-38 has been cited by 35 publications

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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 MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 NX\IS2JxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSCycn;zeIF1\SClZXzsJIxqdmVuIFnDOVA:OTNibl2= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODR7OEKxOkc,OTB2OUiyNVY9N2F-
human MCF-7 breast cell line NIHCRmhRem:uaX\ldoF1cW:wIHHzd4F6 M1nrUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGMVch[nKnYYP0JINmdGxibHnu[UwhUUN3ME2wMlM4KM7:TR?= MkHjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB2OUiyNVYoRjFyNEm4NlE3RC:jPh?=
human SKOV-3 ovarian cell line MoHmVJJwdGmoZYLheIlwdiCjc4PhfS=> NGHqd2lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLU3YuOyCxdnHybYFvKGOnbHygcIlv\SxiSVO1NF0xNjd{IN88US=> MkS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB2OUiyNVYoRjFyNEm4NlE3RC:jPh?=
human breast cancer cell line (SK-BR-3) Mn\zR5l1d3SxeHnjxsBie3OjeR?= NYC1fIp4UW5iVnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4h[nKnYYP0JINidmOncjDj[YxtKGyrbnWgLHNMNUKULUOpMEBKSzVyPUSgcm0> M3;6cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzM{O0OVY6Lz5zMUOzOFU3QTxxYU6=
human lung cancer cell line (H128) NXzOOmxnS3m2b4TvfIlkyqCjc4PhfS=> MXjJckBXcXS{bzDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDseY5oKGOjbnPldkBk\WyuIHzpcoUhMEhzMkipMEBKSzVyPU[gcm0> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTN|NEW2PUc,OTF|M{S1Olk9N2F-
human stomach cancer cell line (MKN45) NF\KNY9EgXSxdH;4bYPDqGG|c3H5 NXnTXFdxUW5iVnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4he3SxbXHjbEBk[W6lZYKgZ4VtdCCuaX7lJEhOU052NTmsJGlEPTB;ODDuUS=> NHq0[lQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUOzOFU3QSd-MUGzN|Q2Pjl:L3G+
human ovarian cancer cell line (SK-OV-3) M1nTdWN6fG:2b4jpZ:Kh[XO|YYm= M1T2XmlvKF[rdILvJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI93[XKrYX6gZ4Fv[2W{IHPlcIwhdGmwZTCoV2suV1ZvMzmsJGlEPTB;MUGgcm0> MlezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF|M{S1OlkoRjFzM{O0OVY6RC:jPh?=
human colon cancer cell line (WiDr) Mm\IR5l1d3SxeHnjxsBie3OjeR?= NWPqd493UW5iVnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4h[2:ub36gZ4Fv[2W{IHPlcIwhdGmwZTCoW4lFeiluIFnDOVA:OTRibl2= NFPpPWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUOzOFU3QSd-MUGzN|Q2Pjl:L3G+
human lung cancer cell line (A549) M1PNbGN6fG:2b4jpZ:Kh[XO|YYm= MWDJckBXcXS{bzDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDseY5oKGOjbnPldkBk\WyuIHzpcoUhMEF3NEmp NVfIR|NmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUGzN|Q2PjlpPkGxN|M1PTZ7PD;hQi=>
NSCLC-H460 MXPDfZRwfG:6aXRCpIF{e2G7 NUDTfFBHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdm:wLYPtZYxtNWOnbHygcJVv\yClYYLjbY5wdWFiY3XscEBtcW6nIFi0OlAhME6VQ1zDMWg1PjBrLDDJR|UxRThyIH7N NGjvSlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUW2N|kzPSd-MUG1OlM6OjV:L3G+
PC-3 carcinoma cell line NV7nPIZUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPnR49v[2WwdILheIlwdiC{ZYH1bZJm\CC2bzDpcohq[mm2IHfyc5d1cCCxZjDoeY1idiCycn;zeIF1\SCSQz2zJINiemOrbn;tZUBk\WyuIHzpcoUtKEmFNUC9N|UvPiCwTR?= NYr5OWwxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW0OVQzOzBpPkG1OFU1OjNyPD;hQi=>
human HCT116 colon cancer cell line MWDGeY5kfGmxbjDhd5NigQ>? NXHQWJdTUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOxbH;uJINidmOncjDj[YxtKGyrbnWsJGlEPTB;NzDuUS=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPThyOES1Okc,OTV6MEi0OVY9N2F-
human Bel-7402 liver cancer cell line MXLGeY5kfGmxbjDhd5NigQ>? M2HafWlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKEKnbD23OFAzKGyrdnXyJINidmOncjDj[YxtKGyrbnWsJGlEPTB;Mz6xPUDPxE1? NVjifVV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4NFg1PTZpPkG1PFA5PDV4PD;hQi=>
human tumor HL60 cell-line M{PjOWZ2dmO2aX;uJIF{e2G7 MUOzJIRigXN? NVn6d2tlUW5vdnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIZweiCqdX3hckB1fW2xcjDIUFYxKGOnbHytcIlv\SC5YYOg[IV1\XKvaX7l[EB2e2mwZzDTVmIh[XO|YYmgZYZ1\XJiMzDkZZl{KG:oIHnuZ5Vj[XSrb36sJGlEPTB;MUmgcm0> M{nYT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OUGzPVk3Lz5zNUmxN|k6PjxxYU6=
human H460 cell M4fEPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVO5[4tqUW6qaXLpeIlwdiCxZjDoeY1idiCKNE[wJINmdGxiZ4Lve5RpNCCLQ{WwQVgxKG6P Mm\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ7MUO3NFYoRjF4OUGzO|A3RC:jPh?=
MDA-MB-435 M{TGdWZ2dmO2aX;uJIF{e2G7 NFvwPVdKdmirYnn0bY9vKGGpYXnud5QhVUSDLV3CMVQ{PSCVIHj1cYFvKGK{ZXHzeEBk[W6lZYKgZ4VtdHNiaX6geIhmKGGkc3XuZ4Uhd2ZiYXzieY1qdixiSVO1NEA:KDBwMEC1JO69VS5? NIf4Oo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC1NlgxOid-MUGwOVI5ODJ:L3G+
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A549 M3K3cmN6fG:2b4jpZ4l1gSCjc4PhfS=> NV7ZeGd{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCkeTDTVmIhdWW2aH;kMEBKSzVyIE2gNE4xQCEQvF2u MnXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7OE[4NFcoRjF6OUi2PFA4RC:jPh?=
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A549 M{jr[mN6fG:2b4jpZ4l1gSCjc4PhfS=> MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzMEBKSzVyIE2gNE4xPDdizszNMi=> Ml3qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2N{C4OlQoRjJzNEewPFY1RC:jPh?=
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DU145 M331eWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3rtUmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{NCCLQ{WwJF0hOC5yMzFOwG0v MlTTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3N{i1OFUoRjJ|NUe4OVQ2RC:jPh?=
HT-29 M2\MTGN6fG:2b4jpZ4l1gSCjc4PhfS=> M4HsU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{NCCLQ{WwJF0hOC5yMzFOwG0v MkXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3N{i1OFUoRjJ|NUe4OVQ2RC:jPh?=
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DU145 MnnZR5l1d3SxeHnjbZR6KGG|c3H5 NUXKZmVJPzJiaILz MkTHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR|UxKD1iMD6xNUDPxE1w NILJV5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[yNlk5OSd-MkO2NlI6QDF:L3G+
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A549 NF70WXVEgXSxdH;4bYNqfHliYYPzZZk> NVj1RolHOyCmYYnz MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFMh\GG7czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjByMkeyJO69VS5? NU\nV4RTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1Nlk5PzBpPkK0OVI6QDdyPD;hQi=>
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HT-29 M1r4TGN6fG:2b4jpZ4l1gSCjc4PhfS=> MnOzN{Bl[Xm| M2fXcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDNiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkGwOlY4KM7:TT6= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV{OUi3NEc,OjR3Mkm4O|A9N2F-
HCT116 MlLhR5l1d3SxeHnjbZR6KGG|c3H5 NHmxZYREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNuIFnDOVAhRSByLkG2OkDPxE1w NFm5W4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWyPVg4OCd-MkS1Nlk5PzB:L3G+
MDA-MB-231 MojBR5l1d3SxeHnjbZR6KGG|c3H5 NXW4UXd3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{whUUN3MDC9JFAvOTd4IN88UU4> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV{OUi3NEc,OjR3Mkm4O|A9N2F-
A549 MYjDfZRwfG:6aXPpeJkh[XO|YYm= MlvKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{whUUN3MDC9JFAvOjV7IN88UU4> Mn3QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3Mkm4O|AoRjJ2NUK5PFcxRC:jPh?=
HEK293 MYrDfZRwfG:6aXPpeJkh[XO|YYm= MV63NkBpenN? MkDJTY51emmwc3njJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUd3MDC9JFAvODB3IN88UU4> M1;xOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkeyNFU2Lz5{NUK3NlA2PTxxYU6=
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HT-29 M3TUSWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1rxNVczKGi{cx?= MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NEA:KDBwMEG4OVQh|ryPLh?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NUO1PUc,OjV6M{WzOVk9N2F-
HCT15 MnHuR5l1d3SxeHnjbZR6KGG|c3H5 MY[3NkBpenN? NWfHR3FlS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUWgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IECuNFA5KM7:TT6= M2HpNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5ME[wO|YxLz5{N{C2NFc3ODxxYU6=
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HT-29 M2f5UmN6fG:2b4jpZ4l1gSCjc4PhfS=> MlnhO|IhcHK| MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5yNUSg{txONg>? NX\lZmdmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewOlA4PjBpPkK3NFYxPzZyPD;hQi=>
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LAN-5 MkHVdWhVWyCjc4PhfS=> NHXKc4ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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HCT116 MYnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MYO3NkBpenN? NF31XHJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE4xODB5ODFOwG0v NEe1VWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEGxOVQ6Oid-M{CxNVU1QTJ:L3G+
A549 M1jtZmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mmm5O|IhcHK| NV7KS4c4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlAxOTZ{IN88UU4> NWjK[JdMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxNVU1QTJpPkOwNVE2PDl{PD;hQi=>
MCF7 M4W1[WN6fG:2b4jpZ4l1gSCjc4PhfS=> NE\iemY4OiCqcoO= M1\xVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFnDOVAhRSByLkCwNFEh|ryPLh?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF4OUCzPEc,OzBzNkmwN|g9N2F-
A549 MWfDfZRwfG:6aXPpeJkh[XO|YYm= NU\1eXllPzJiaILz MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> NUDUN2lHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxOlkxOzhpPkOwNVY6ODN6PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Chk1 / Chk1 / Topo I ; 

PubMed: 18509065     


Log-phase Ovcar-5 cells were treated for 24 h with diluent (0.1% DMSO, lanes 1 and 6), gemcitabine at 12.5, 25, 50 or 100 nM (lanes 2-5, respectively), or SN-38 at 2.5, 5, 10, 20 and 40 nM in the absence (lanes 7-11) or presence (lanes 12-17) of 50 nM gemcitabine. At the end of the incubation, whole cell lysates were prepared, subjected to SDS-PAGE, transferred to nitrocellulose, and probed with reagents that recognize phospho-Ser345-Chk1, total Chk1, topo I or, as control, β-actin. Because of the limited number of lanes on our electrophoresis apparatus, lanes 1-5 and 6-17 represent two different membranes from the same experiment that were probed simultaneously.

18509065
Growth inhibition assay
Cell viability; 

PubMed: 25759163     


(A) Drug sensitivity towards SN‐38 and oxaliplatin for the parental and drug resistant cell lines. Cells were exposed to a range of drug concentrations for 48 h and cell viability was assessed by an endpoint MTT assay. Results of representative experiments are shown. Green (triangle) is the parental cell line, blue (diamond) the SN‐38 resistant cell line, and red (square) the oxaliplatin resistant cell line.

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

Kinase Assay:[1]
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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]
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  • 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 powder
in solvent
Synonyms NK012
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

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

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03245450 Recruiting Drug: Eribulin mesilate|Drug: Irinotecan hydrochloride Refractory or Recurrent Solid Tumors|Rhabdomyosarcoma|Non-Rhabdomyosarcoma Soft Tissue Sarcoma|Ewing Sarcoma Eisai Inc. February 22 2018 Phase 1|Phase 2
NCT03295084 Completed Drug: Irinotecan|Drug: Capecitabine Metastatic Colorectal Cancer Dorte Nielsen|Herlev Hospital July 15 2015 Phase 1
NCT01963182 Completed Drug: Irinotecan First Line Metastatic Colorectal Cancer Centre Jean Perrin October 2013 Phase 2
NCT01859858 Completed Dietary Supplement: curcumin|Drug: Irinotecan Advanced Colorectal Cancer UNC Lineberger Comprehensive Cancer Center June 2013 Phase 1
NCT02481960 Terminated Procedure: CM-BC2 Irinotecan drug-eluting bead Glioma Boston Scientific Corporation February 21 2012 Phase 1|Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID