Roscovitine (Seliciclib,CYC202)

For research use only.

Catalog No.S1153

63 publications

Roscovitine (Seliciclib,CYC202) Chemical Structure

Molecular Weight(MW): 354.45

Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.

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Selleck's Roscovitine (Seliciclib,CYC202) has been cited by 63 publications

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.
Targets
CDK5/p35 [1]
(Cell-free assay)
Cdc2/CyclinB [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
ERK2 [1]
(Cell-free assay)
0.16 μM 0.65 μM 0.7 μM 0.7 μM 14 μM
In vitro

Roscovitine displays high efficiency and high selectivity towards some cyclin-dependent kinases with IC50 of 0.65, 0.7, 0.7 and 0.16 μM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E and cdk5/p53, respectively. [1] Roscovitine reversibly inhibits the prophaselmetaphase transition in the micromolar range of starfish oocytes and sea urchin embryos, inhibits in vitro M-phase-promoting factor activity and in vitro DNA synthesis in Xenopus egg extracts, and suppresses the proliferation of mammalian cell lines with an average IC50 of 16 μM. [1] In mesangial cells, Roscovitine results in a dose-dependent reduction of CDK2 activity that at concentrations of 7.5, 12.5 and 25 mM, Roscovitine causes a 25, 50% and 100% decrease in CDK2 activity, respectively. [2] A recent study shows that Roscovitine inhibits cdk5 kinase activity, cell proliferation, multicellular development, and cdk5 nuclear translocation in Dictyostelium discoideum, without affecting the expression of cdk5 protein during axenic growth. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A3-KAW M1PZbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X5NGlEPTB;NT63OlEyPiEQvF2= NXTZTGtkW0GQR1XS
MRK-nu-1 M1f6R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHXTohKSzVyPUeuNVI6PjlizszN NHywV5VUSU6JRWK=
NCCIT Mo\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTdwNUW0PFIh|ryP M2nsRXNCVkeHUh?=
JiyoyeP-2003 NYGxeHVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj6NGVyUUN3ME24MlUxOjZ2IN88US=> NYfjU|ZoW0GQR1XS
KS-1 M2\reWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\o[WVKSzVyPUmuOFU4QDVizszN NHjHfolUSU6JRWK=
Becker NWnDPVB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDaTWM2OD17LkS2NFgzKM7:TR?= M{PoOHNCVkeHUh?=
KARPAS-422 M3XlWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTlwOU[zN|Yh|ryP Mn74V2FPT0WU
BB65-RCC M1TsVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTlwOUe0PVUh|ryP MULTRW5ITVJ?
SK-UT-1 NInL[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\MTWM2OD1zMD6zOUDPxE1? MnmxV2FPT0WU
ST486 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTQTWM2OD1zMD6zOVEh|ryP NW\ibpJ4W0GQR1XS
LB831-BLC MnzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTFzLkW2NlQh|ryP M4HSVXNCVkeHUh?=
COR-L279 NXL4UlVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjVSWRKUUN3ME2xNk4zQTB5IN88US=> NEXZeHhUSU6JRWK=
NB1 NVvmUpJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ziOmlEPTB;MUKuN|MxQCEQvF2= MVvTRW5ITVJ?
D-247MG NYrBSoRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XNOWlEPTB;MUKuN|UyPiEQvF2= MYLTRW5ITVJ?
697 MmLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm0eI9YUUN3ME2xNk43ODB5IN88US=> M1rZcHNCVkeHUh?=
GCIY NIH0R49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfrZm1KSzVyPUGyMlg3OTNizszN MnztV2FPT0WU
RPMI-8402 NWP1NHhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLZd|VlUUN3ME2xN{43OjZ{IN88US=> NF:1S|ZUSU6JRWK=
Raji MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTF|Lke4PVQh|ryP NGnVTJZUSU6JRWK=
MEG-01 M3XjO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF|LkizO|kh|ryP MVPTRW5ITVJ?
RPMI-6666 NXewTpZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\D[3VIUUN3ME2xN{46OTJzIN88US=> M{XYXXNCVkeHUh?=
SCC-3 M{nGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnpdHpKSzVyPUG0MlI6PTZizszN M{jWS3NCVkeHUh?=
HCC1599 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fEfmlEPTB;MUSuOVk4PSEQvF2= NXK2Uo4xW0GQR1XS
OCI-AML2 M4[wd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\EcGlEPTB;MUWuOlQ5OiEQvF2= MYDTRW5ITVJ?
OS-RC-2 M1GwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHsTWM2OD1zNT64N|gzKM7:TR?= Ml;WV2FPT0WU
NCI-H1304 NUO5[WluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL2TWM2OD1zNj6zOlAyKM7:TR?= MW\TRW5ITVJ?
HD-MY-Z NHXJb4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnT[2lKSzVyPUG2MlgzPDZizszN NEP0RodUSU6JRWK=
JAR MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DYbGlEPTB;MUeuNFE2OiEQvF2= MnzMV2FPT0WU
TGW M4\Bc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXTTWM2OD1zNz64NVI1KM7:TR?= M170SHNCVkeHUh?=
BC-3 MkjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDOTWM2OD1zOD6wN|A2KM7:TR?= NVXLNm5zW0GQR1XS
A101D MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[4NXhKSzVyPUG4MlMzODhizszN MVzTRW5ITVJ?
COLO-320-HSR NIrPXGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm4[pBKSzVyPUG4Mlc3QDhizszN MnjnV2FPT0WU
LC4-1 NGLWe4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\iT5BbUUN3ME2xPE45PzN2IN88US=> NUHoTGpnW0GQR1XS
BC-1 NYnSepNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\sSos2UUN3ME2xPU4yOTl6IN88US=> NE\aOZJUSU6JRWK=
MHH-PREB-1 M3vPTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\DemlEPTB;MkCuNFM2PiEQvF2= MVfTRW5ITVJ?
BL-70 NEfmfmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJyLkOyO|Qh|ryP NHW5cJZUSU6JRWK=
CESS Mk\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTJyLki1OFkh|ryP M2nafnNCVkeHUh?=
ES8 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Xle2lEPTB;MkGuNFYh|ryP NYr6NYt2W0GQR1XS
NOMO-1 M4Ljc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJzLkKwNFgh|ryP MlTIV2FPT0WU
ACN NVvTVnhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorFTWM2OD1{MT6zN|g6KM7:TR?= NYXXe4F3W0GQR1XS
EB-3 MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TuVWlEPTB;MkOuNVg{OSEQvF2= MVLTRW5ITVJ?
LS-513 M2nYTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj4SnN5UUN3ME2yN{42OTd7IN88US=> NVLpSGNlW0GQR1XS
HH NIHlfmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHlTWM2OD1{ND6zPFE6KM7:TR?= MlvkV2FPT0WU
IST-SL2 NVrQNXR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjMTWM2OD1{ND61N|Q{KM7:TR?= MXzTRW5ITVJ?
HOP-62 NXT2c|FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHOTWM2OD1{NT60OFI2KM7:TR?= NX7C[W02W0GQR1XS
NCI-H2126 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTDTWM2OD1{NT62OVI6KM7:TR?= NET5RVNUSU6JRWK=
BL-41 MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljtTWM2OD1{NT65OVk4KM7:TR?= M1zqeXNCVkeHUh?=
KURAMOCHI MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHKRXJQUUN3ME2yOk45ODh{IN88US=> NYL3O2N6W0GQR1XS
KARPAS-299 NWfBUnJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfLTWM2OD1{Nj64OlQ3KM7:TR?= MlnPV2FPT0WU
QIMR-WIL NFH0W|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\IfmlEPTB;MkeuPVE1PCEQvF2= MnXnV2FPT0WU
HL-60 M2H1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHyUVJNUUN3ME2yO{46QDZ7IN88US=> NFv4PZlUSU6JRWK=
TE-9 NEjTRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\1TWM2OD1{OD63PVY6KM7:TR?= NUPucpNyW0GQR1XS
TE-8 NIDtUGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH1TWM2OD1{OD65NFgh|ryP M1;aeXNCVkeHUh?=
NOS-1 MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILBRnFKSzVyPUK4Mlk4OzNizszN M2PEXHNCVkeHUh?=
GI-1 Mlq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPQTWM2OD1{OT6wNVE{KM7:TR?= MmTVV2FPT0WU
KM12 NHLXenpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jtNmlEPTB;MkmuOlI{QSEQvF2= MnTiV2FPT0WU
BB30-HNC M4\5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYWwRYpEUUN3ME2yPU46PDh|IN88US=> MXPTRW5ITVJ?
ES3 M{nzU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDOfWxRUUN3ME2yPU46PTh{IN88US=> M33sTHNCVkeHUh?=
NCI-H510A NXvZXlVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TUZmlEPTB;M{CuNFMzQSEQvF2= M2O4dHNCVkeHUh?=
NCI-H82 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL5[FY1UUN3ME2zNU4xOTN3IN88US=> NUX4fVNJW0GQR1XS
NCI-SNU-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT6UXR1UUN3ME2zNU4yODV7IN88US=> M1XrNHNCVkeHUh?=
NKM-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jFTmlEPTB;M{GuNVM6PyEQvF2= M4H1T3NCVkeHUh?=
SIG-M5 MlfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D2NWlEPTB;M{GuOlg{OyEQvF2= M2rQdXNCVkeHUh?=
SK-N-FI MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnlTWM2OD1|MT63OVM2KM7:TR?= M1PjfHNCVkeHUh?=
LOUCY M{TuS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTN{LkGyOVMh|ryP NXfLUoNOW0GQR1XS
Calu-6 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPGVIJ2UUN3ME2zNk41PzR3IN88US=> NXvpVGJ4W0GQR1XS
GOTO MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN{LkmxNlkh|ryP Mn\SV2FPT0WU
NCI-H526 NHPYT49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTN|LkS5N|Yh|ryP NWnjeXY2W0GQR1XS
RKO NEnHdXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fEc2lEPTB;M{OuOVk3QSEQvF2= M4ezWHNCVkeHUh?=
NCI-H64 M2[3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHCTWM2OD1|Mz64OVk4KM7:TR?= Mm\1V2FPT0WU
LP-1 NYDURW03T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN|Lki5NFgh|ryP NH\weFZUSU6JRWK=
KGN M2XUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr3TWM2OD1|ND6yOVI1KM7:TR?= NGr4VpZUSU6JRWK=
NCI-H2141 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLFRmNFUUN3ME2zOE43PTN|IN88US=> M2\0NXNCVkeHUh?=
TE-10 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\XTWM2OD1|ND65OFIzKM7:TR?= NWXGZ4xWW0GQR1XS
K5 NIfnV5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Xq[GlEPTB;M{WuNFg3OSEQvF2= NUTEbHo3W0GQR1XS
IMR-5 NUPqdXptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\uTWM2OD1|NT6zNVM6KM7:TR?= MVrTRW5ITVJ?
TE-441-T NIDscVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIGzVXJKSzVyPUO2MlEyPDhizszN M{fCbHNCVkeHUh?=
TE-6 NGPqRoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXn1cmQxUUN3ME2zOk4{OjR4IN88US=> NYLNSolEW0GQR1XS
MOLT-4 NVTGRVlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYX5PHRkUUN3ME2zOk4{Ojd4IN88US=> M{n2T3NCVkeHUh?=
COLO-684 NXSyfW45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDLXplKSzVyPUO3MlAyOiEQvF2= M1XGSXNCVkeHUh?=
LU-139 M{js[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L3NGlEPTB;M{euNVg2PiEQvF2= Ml;0V2FPT0WU
OPM-2 MnXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjFZ|dKSzVyPUO3MlI6PDlizszN NYK0WlZ4W0GQR1XS
ML-2 NVPWc4VVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjT[IJzUUN3ME2zO{43PzF{IN88US=> MlGyV2FPT0WU
RS4-11 NV3FUJZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTqNHJKSzVyPUO3MlcxPjlizszN NGjIR5hUSU6JRWK=
MONO-MAC-6 NEXUN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3RdWtCUUN3ME2zPE4zPDd5IN88US=> MYjTRW5ITVJ?
NCI-H345 M3r2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHINlBKSzVyPUO4MlkyODZizszN MlHoV2FPT0WU
NTERA-S-cl-D1 MlzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfUUGFFUUN3ME2zPU42QDR{IN88US=> MXPTRW5ITVJ?
NCI-H1882 NEDKNINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTRyLkW5PVgh|ryP MnvGV2FPT0WU
LC-1F NIDTdYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf4OlJKSzVyPUSxMlU4ODVizszN NEnuUmFUSU6JRWK=
HT MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjLUZdKSzVyPUSyMlAxOjhizszN M3HQ[XNCVkeHUh?=
MLMA M{m4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTR{LkK3PFch|ryP M2PEZnNCVkeHUh?=
DG-75 MkPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PqWmlEPTB;NEKuOlU1PiEQvF2= Mo\5V2FPT0WU
GI-ME-N M1LObGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWKwUFUzUUN3ME20Nk43PjdzIN88US=> NEXx[4pUSU6JRWK=
MS-1 MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTR{Lki5N{DPxE1? M3LvbXNCVkeHUh?=
CGTH-W-1 M2nDZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTR2Lkm2PVch|ryP M3\jbHNCVkeHUh?=
NCI-H209 NGryO3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r3O2lEPTB;NE[uNFEyPSEQvF2= MljqV2FPT0WU
LB2518-MEL MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PNemlEPTB;NEeuNFQ1QCEQvF2= M3jqOXNCVkeHUh?=
DU-4475 MlK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrETWM2OD12OD60PVM4KM7:TR?= NGK3W5hUSU6JRWK=
LB2241-RCC Mon3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v3VmlEPTB;NEiuOlIxOiEQvF2= NXLXenpjW0GQR1XS
LB771-HNC NHTtNnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3WyfmlEPTB;NEiuPVIyOiEQvF2= M2rQVHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Rb / p-CDK2 / CDK2 / Cyclin D1 / Cyclin A2 / ERα / ERβ/ AIB1 / PELP1 ; 

PubMed: 21834972     


(a) The model cells MCF7, MCF7-TamR, MCF7-HER2, and MCF7-LTLTca were treated with roscovitine and the status of cell cycle regulators and the estrogen receptor (ERα) signaling proteins was analyzed by western blotting. 

pT231-tau / pS202-tau / tau; 

PubMed: 30915013     


SH-SY5Y-(P301L) cells were exposed for 6 h to a range of roscovitine concentrations. Cells were harvested and proteins were resolved by SDS-PAGE followed by western blotting.

21834972 30915013
Immunofluorescence
E2F1 / FASN / Bmi1 / Cyclin D2 / CDK2 / CDK4 ; 

PubMed: 20890301     


Immunofluorescence analysis of E2F1, FASN, E2F1/Shh target Bmi1, cyclin D2, cdk 2, and cdk 4 in Pzp53med cells treated with DMSO (control) or the cdk inhibitor roscovitine (10 nM) for 18 hours.

CDK1 / Smek2 / FUBP1 / Cdc20 ; 

PubMed: 24534090     


A-D Validation of changes in chromatin affinity following Cdk inhibition of indicated candidates (2 h, 50 μM roscovitine) using Triton extraction and immunofluorescence (IF) in HeLa cells. Quantification of IF data was performed by measuring changes in signal intensities in Image J.

20890301 24534090
Growth inhibition assay
Cell viability; 

PubMed: 29996940     


Cell viability assay on OVCAR5, OAW42, SKOV3 and NL3507 cells treated with roscovitine (2, 5, 10, 20, 40 μM) up to 96 h. Each point represents the mean of three replicates. Error bars, SD

29996940
In vivo Roscovitine, at a dose of 50 mg/kg, significantly inhibits growth of The Ewing's sarcoma family of tumors (ESFT) xenografts. [4] Roscovitine enhances the antitumor effect of doxorubicin without increased toxicity with a mechanism that involves cell cycle arrest rather than apoptosis in nude mice bearing established MCF7 xenografts. [5]

Protocol

Kinase Assay:[1]
- Collapse

Enzymes :

Kinases activities are assayed at 30 °C in buffer C. Blank values are subtracted from the data and activities calculated as molar amount of phosphate incorporated in protein acceptor during a 10-minute incubation. Controls are performed with appropriate dilutions of DMSO. In a few cases, phosphorylation of the substrate is assessed by autoradiography after SDS/PAGE. p34cdc2/cyclin B is purified from M-phase starfish (M. glacialis) oocytes by affinity chromatography. It is assayed with 1 mg histone Hl/mL, in the presence of 15 μM [γ-32P]ATP (3000 Ci/mmol; 1 mCi/mL) in a final volume of 30 μL. After a 10-minute incubation at 30 °C, 25-μL aliquots of supernatant are spotted onto pieces of Whatman P81 phosphocellulose paper, and, after 20 seconds, the filters are washed five times (for at least 5 minutes each time) in a solution of 10mL phosphoric acid/L water. The wet filters are transferred into 6-mL plastic scintillation vials, 5 mL ACS scintillation fluid is added and the radioactivity measured in a Packard counter. The kinase activity is expressed as molar amount of phosphate incorporated in histone H1 during a 10-minutes incubation or as a percentage of maximal activity. p33cdk2/cyclin A and p33cdk2/cyclinE are reconstituted from extracts of sf9 insect cells infected with various baculoviruses. Cyclins A and E are fusion proteins with glutathione S-transferase and the complexes are purified on glutathione-agarose beads. Kinase activities are assayed with 1 mg/mL histone H1, in the presence of 15 μM [γ-32P]ATP, during 10 minutes, in a final volume of 30 μL, as described for the p34cdc2/cyclin B kinase. p33cdk5/p35 is purified from bovine brain, excluding the Mono S-chromatographic step. The active fractions from the Superose 12 column are pooled and concentrated to a final concentration of approximately 25 μg enzyme/mL. The kinase is assayed with 1 mg/mL histone HI in the presence of 15 μM [γ-32P]ATP, during 10 minutes in a final volume of 30 μL, as described for the p34cdc2/cyclin B kinase. p33cdk5/cyclin D1 is obtained from insect cell lysates. Cdk4 is a fusion protein with glutathione-S-transferase and the active complex is purified on glutathione-agarose beads. Its kinase activity is assayed with purified retinoblastoma protein (complexed with glutathione-S-transferase) in the presence of 15 μM [γ-32P]ATP, in a final volume of 30 μL. After a 15-minute incubation, 30 μL Laemmli sample buffer is added. The phosphorylated substrate is resolved by 10 % SDS/PAGE and analysed by autoradiography by overnight exposure to Hyperfilm MP and densitometry. p33cdk4/cyclinD 2 is obtained from insect cell lysates. It is assayed with purified retinoblastoma protein (complexed with glutathione-S-transferase) in the presence of 15 μM [γ-32P]ATP in a final volume of 30 μL. After a 30-minute incubation, 30 μL Laemmli sample buffer is added. The phosphorylated substrate is resolved by 10% SDS/PAGE and analysed by autoradiography by overnight exposure to Hyperfilm MP and densitometry. MAP kinase erkl (tagged with glutathione-S-transferase), is expressed in bacteria, purified on glutathione-agarose beads and assayed with 1 mg myelin basic protein/ml in the presence of 15 μM [γ-32P]ATP as described above for the p34cdc2cyclin B kinase. His-tagged erkl and erk2 are activated in vitro by mitogen-activated protein kinase kinase, purified (Ni-affinity and Mono Q) and assayed as described above during 10 minutes in a final volume of 30 μL. Protein kinase C isoforms are purified from baculovirus infected sf9 insect cells and assayed with 1 mg/mL protamine sulfate in the presence of 15 μM [γ-32P]ATP, during 10 minutes at 30 °C, in a final volume of 30 μL. Phosphorylated protamine sulfate is recovered on Whatman P81 phosphocellulose paper as described for the cdc2 kinase. The catalytic subunit of cAMP-dependent protein kinase, purified from bovine heart, is assayed with 1 mg histone Hl/ml, in the presence of 15 μM [γ-32P]ATP as described for the p34cdc2/cyclin B kinase. cGMP-dependent protein kinase, purified to homogeneity from bovine tracheal smooth muscle, is assayed with 1 mg histone Hl/mL, in the presence of 15 μM [γ-32P]ATP as described for the p34cdc2/cyclin B kinase. Casein kinase 2 is isolated from rat liver cytosol and assayed with 1 mg casein/mL and 15 μM [γ-32P]ATP. The substrate is spotted on Whatmann 3MM filters and washed with 10% (mass/vol.) trichloroacetic acid. Myosin light chain kinase, purified from chicken gizzard is assayed in the presence of 100 nM calmodulin, 100 μM CaCl2, 50 mM Hepes, 5 mM MgCI,, 1 mM dithiothreitol and 0.1 mg BSA/ml at pH 7.5 using a synthetic peptide based on the smooth-muscle myosin light-chain phosphorylation site and in the presence of 15 μM [γ-32P]ATP, in a final volume of 50 μL. Incorporation of radioactive phosphate is monitored on phosphocellulose filters as described above. ASK-γ, a plant homologue of GSK-3, is expressed as a glutathione-S-transferase fusion protein in Escherichia coli and purified on glutathione-agarose. ASK-γ kinase is assayed, for 10 minutes at 30 °C, with 5 μg myelin basic protein, in the presence of 15 μM [γ-32P]ATP in a final volume of 30 μL. The phosphorylated myelin basic protein is recovered on Whatman P81 phosphocellulose paper as described for the p34cdc2/cyclin B kinase. Insulin receptor tyrosine kinase domain (CIRK-41) is overexpressed in a baculovirus system and purified to homogeneity. Its kinase activity is assayed, for 10 minutes at 30 °C, with 5 μg Raytide, in the presence of 15 μM [γ-32P]ATP, in a final volume of 30 μL. The phosphorylated Raytide is recovered on Whatman P81 phosphocellulose paper as described for the p34cdc2/cyclin B kinase. c-src kinase is purified from infected Sf9 cells. The v-abl kinase is expressed in E. coli and affinity purified on IgG Affigel 10. Both kinases are assayed for 10 minutes at 30 °C, with 5 μg Raytide, in the presence of 15 μM [γ-32P]ATP, in a final volume of 30 μL. The phosphorylated Raytide is recovered on Whatman P81 phosphocellulose paper as described for the p34cdc2/cyclin B kinase.
Cell Research:[1]
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  • Cell lines: Leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, breast cancer
  • Concentrations: 0.01 - 100 μM
  • Incubation Time: 48 hours
  • Method: 60 human tumour cell lines comprising nine tumor types are cultured for 24 hours prior to a 48-hour continuous exposure to 0.01-100 μM roscovitine. A sulforhodaminine B protein assay is used to estimate the cytotoxicity.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: A4573 cells are injected s.c. into the right posterior flank of CD1 nu/nu mice.
  • Dosages: ≤50 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (200.31 mM)
Ethanol 6 mg/mL (16.92 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+69% PEG 400
For best results, use promptly after mixing.
5mg/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 354.45
Formula

C19H26N6O

CAS No. 186692-46-6
Storage powder
in solvent
Synonyms N/A
Smiles CCC(CO)NC1=NC(=C2N=C[N](C(C)C)C2=N1)NCC3=CC=CC=C3

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    How can I reconstitute the drug for in vivo studies?

  • Answer:

    S1153 in 1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+PEG 400 is a clear solution which is okay for injection. And S1153 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30mg/ml is a suspension, which is fine for oral gavage.

CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID