Roscovitine (Seliciclib,CYC202)

Catalog No.S1153

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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Cited by 41 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 NGnNU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTVwN{[xNVYh|ryP M4\CR3NCVkeHUh?=
MRK-nu-1 NIXnTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnMZlhCUUN3ME23MlEzQTZ7IN88US=> NWfqWWUyW0GQR1XS
NCCIT MnroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTKTWM2OD15LkW1OFgzKM7:TR?= M1:1S3NCVkeHUh?=
JiyoyeP-2003 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fkd2lEPTB;OD61NFI3PCEQvF2= MoD4V2FPT0WU
KS-1 MojZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fBVGlEPTB;OT60OVc5PSEQvF2= NFfOSZlUSU6JRWK=
Becker Mn3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTlwNE[wPFIh|ryP NIi2RlBUSU6JRWK=
KARPAS-422 NIe3eoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLZfoVjUUN3ME25Mlk3OzN4IN88US=> NYTDcXlJW0GQR1XS
BB65-RCC MnHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTlwOUe0PVUh|ryP NGnJTVFUSU6JRWK=
SK-UT-1 NY\QNIVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL2TWM2OD1zMD6zOUDPxE1? NWXVOXZVW0GQR1XS
ST486 NUP2fpBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHFTWM2OD1zMD6zOVEh|ryP Mn7YV2FPT0WU
LB831-BLC M2jOSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFzLkW2NlQh|ryP M1PVRnNCVkeHUh?=
COR-L279 MlvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jFSGlEPTB;MUKuNlkxPyEQvF2= MnL0V2FPT0WU
NB1 MkTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjyPWtVUUN3ME2xNk4{OzB6IN88US=> NXXsNINwW0GQR1XS
D-247MG M2fWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnOPJpKSzVyPUGyMlM2OTZizszN MlzsV2FPT0WU
697 NWC4bJpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fHfGlEPTB;MUKuOlAxPyEQvF2= NIXZSnFUSU6JRWK=
GCIY MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HWbGlEPTB;MUKuPFYyOyEQvF2= M1n0OHNCVkeHUh?=
RPMI-8402 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq1TWM2OD1zMz62NlYzKM7:TR?= NG\zVHpUSU6JRWK=
Raji NXrwT2JTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr2THRrUUN3ME2xN{44QDl2IN88US=> M{fRS3NCVkeHUh?=
MEG-01 NEXK[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HFcGlEPTB;MUOuPFM4QSEQvF2= MoPVV2FPT0WU
RPMI-6666 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTF|LkmxNlEh|ryP M1ux[3NCVkeHUh?=
SCC-3 NEjPOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF2LkK5OVYh|ryP NHzUSJRUSU6JRWK=
HCC1599 M3XyPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfVTWM2OD1zND61PVc2KM7:TR?= M4LC[HNCVkeHUh?=
OCI-AML2 NVzDW2o2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHMNlJKSzVyPUG1MlY1QDJizszN NIHVOJJUSU6JRWK=
OS-RC-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTF3LkizPFIh|ryP M{D2THNCVkeHUh?=
NCI-H1304 M2DpWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHzUJhDUUN3ME2xOk4{PjBzIN88US=> MonpV2FPT0WU
HD-MY-Z MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF4LkiyOFYh|ryP MkjCV2FPT0WU
JAR Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF5LkCxOVIh|ryP MnLWV2FPT0WU
TGW MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nUT2lEPTB;MUeuPFEzPCEQvF2= NVzLT4l5W0GQR1XS
BC-3 M3TW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF6LkCzNFUh|ryP NUL6dGRHW0GQR1XS
A101D NGTtS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjq[2RiUUN3ME2xPE4{OjB6IN88US=> M{fqTXNCVkeHUh?=
COLO-320-HSR NUPrUFR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITseVZKSzVyPUG4Mlc3QDhizszN NWLlfJREW0GQR1XS
LC4-1 M3e0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK3TWM2OD1zOD64O|M1KM7:TR?= M1PMUXNCVkeHUh?=
BC-1 NHvv[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXMTWM2OD1zOT6xNVk5KM7:TR?= Mmq5V2FPT0WU
MHH-PREB-1 NVK4PYs2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[3bWRZUUN3ME2yNE4xOzV4IN88US=> NV\JVm5qW0GQR1XS
BL-70 NXqzfGZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TzdGlEPTB;MkCuN|I4PCEQvF2= M1[yc3NCVkeHUh?=
CESS MoXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\UTWM2OD1{MD64OVQ6KM7:TR?= NHS0PJpUSU6JRWK=
ES8 Mmf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJzLkC2JO69VQ>? MoezV2FPT0WU
NOMO-1 MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDGb|BKSzVyPUKxMlIxODhizszN M1K1e3NCVkeHUh?=
ACN NX3XeXZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDpTWM2OD1{MT6zN|g6KM7:TR?= MUXTRW5ITVJ?
EB-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f0R2lEPTB;MkOuNVg{OSEQvF2= M3;uVXNCVkeHUh?=
LS-513 MlixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT6TWM2OD1{Mz61NVc6KM7:TR?= NHPDNXZUSU6JRWK=
HH NWHBb2NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJ2LkO4NVkh|ryP MoWyV2FPT0WU
IST-SL2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPTWJo{UUN3ME2yOE42OzR|IN88US=> MUPTRW5ITVJ?
HOP-62 M2TFWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfFPJRKUUN3ME2yOU41PDJ3IN88US=> NHW1UmRUSU6JRWK=
NCI-H2126 NYTucFJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJ3Lk[1Nlkh|ryP MVXTRW5ITVJ?
BL-41 MnXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXntOFdbUUN3ME2yOU46PTl5IN88US=> NYrVSWRUW0GQR1XS
KURAMOCHI MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTJ4LkiwPFIh|ryP NHixOVlUSU6JRWK=
KARPAS-299 NIq4VItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7xTWM2OD1{Nj64OlQ3KM7:TR?= MnH1V2FPT0WU
QIMR-WIL NIHaTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJ5LkmxOFQh|ryP NFLiXpdUSU6JRWK=
HL-60 NXX0dHMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknETWM2OD1{Nz65PFY6KM7:TR?= MnK2V2FPT0WU
TE-9 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJ6Lke5Olkh|ryP NGLpUoxUSU6JRWK=
TE-8 M1jYWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTCTWM2OD1{OD65NFgh|ryP M2XqO3NCVkeHUh?=
NOS-1 NUj3N3hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJ6Lkm3N|Mh|ryP NUPzbVdiW0GQR1XS
GI-1 Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDvNpZKSzVyPUK5MlAyOTNizszN MYLTRW5ITVJ?
KM12 M3HFU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJ7Lk[yN|kh|ryP NHG2R5ZUSU6JRWK=
BB30-HNC NUDXZXFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP6WnFKSzVyPUK5Mlk1QDNizszN NYHB[JRoW0GQR1XS
ES3 M1nodGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vlSGlEPTB;MkmuPVU5OiEQvF2= NFHQOXpUSU6JRWK=
NCI-H510A MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jYSGlEPTB;M{CuNFMzQSEQvF2= M2XPWHNCVkeHUh?=
NCI-H82 M36xc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HjeGlEPTB;M{GuNFE{PSEQvF2= MVvTRW5ITVJ?
NCI-SNU-1 M1m4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXac3FIUUN3ME2zNU4yODV7IN88US=> Mnr5V2FPT0WU
NKM-1 M1OwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;FTFBYUUN3ME2zNU4yOzl5IN88US=> M37PO3NCVkeHUh?=
SIG-M5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHpTHJEUUN3ME2zNU43QDN|IN88US=> NFHDZ2ZUSU6JRWK=
SK-N-FI NEfPfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLFWotRUUN3ME2zNU44PTN3IN88US=> NYrCT|FyW0GQR1XS
LOUCY MmP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jFRmlEPTB;M{KuNVI2OyEQvF2= NYHBSXZ1W0GQR1XS
Calu-6 NEjORZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LxVWlEPTB;M{KuOFc1PSEQvF2= MmOzV2FPT0WU
GOTO NFTaRZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTN{LkmxNlkh|ryP NIrmXoNUSU6JRWK=
NCI-H526 NYXqU3pzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzvenJKSzVyPUOzMlQ6OzZizszN MlXGV2FPT0WU
RKO M37RS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYr3VHFzUUN3ME2zN{42QTZ7IN88US=> NITjV|NUSU6JRWK=
NCI-H64 M3\TeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{eyNGlEPTB;M{OuPFU6PyEQvF2= MmHIV2FPT0WU
LP-1 NYmyfZlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnndmVDUUN3ME2zN{45QTB6IN88US=> NUjKclh{W0GQR1XS
KGN NXj3eINpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTN2LkK1NlQh|ryP M2S5[XNCVkeHUh?=
NCI-H2141 M4XLd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTN2Lk[1N|Mh|ryP Mo\nV2FPT0WU
TE-10 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vCUmlEPTB;M{SuPVQzOiEQvF2= MXXTRW5ITVJ?
K5 M4nRcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTuToljUUN3ME2zOU4xQDZzIN88US=> NFrZZ5pUSU6JRWK=
IMR-5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:1TWM2OD1|NT6zNVM6KM7:TR?= M1HtV3NCVkeHUh?=
TE-441-T NV\FT29jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HTR2lEPTB;M{[uNVE1QCEQvF2= M3HZ[nNCVkeHUh?=
TE-6 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTN4LkOyOFYh|ryP Mmq0V2FPT0WU
MOLT-4 NY[zSJFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jG[mlEPTB;M{[uN|I4PiEQvF2= MYnTRW5ITVJ?
COLO-684 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe2eFhmUUN3ME2zO{4xOTJizszN NWDFVnZ5W0GQR1XS
LU-139 M3K2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fFdWlEPTB;M{euNVg2PiEQvF2= NHv4OJdUSU6JRWK=
OPM-2 M4PPOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XuTGlEPTB;M{euNlk1QSEQvF2= NGruSIpUSU6JRWK=
ML-2 Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrxfVRCUUN3ME2zO{43PzF{IN88US=> MnHYV2FPT0WU
RS4-11 NEKxbHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUP5WYF5UUN3ME2zO{44ODZ7IN88US=> M4PqPXNCVkeHUh?=
MONO-MAC-6 Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTN6LkK0O|ch|ryP MVTTRW5ITVJ?
NCI-H345 NGHIU2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTN6LkmxNFYh|ryP NXfDXIF4W0GQR1XS
NTERA-S-cl-D1 MlvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fVXWlEPTB;M{muOVg1OiEQvF2= NVzEUGpUW0GQR1XS
NCI-H1882 MnS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjtTXVnUUN3ME20NE42QTl6IN88US=> NV:yW29TW0GQR1XS
LC-1F MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvrbVdFUUN3ME20NU42PzB3IN88US=> NVPhe|NTW0GQR1XS
HT MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTR{LkCwNlgh|ryP M3XXcHNCVkeHUh?=
MLMA M{nnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XCZmlEPTB;NEKuNlc5PyEQvF2= NXnMSnB{W0GQR1XS
DG-75 MnnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTR{Lk[1OFYh|ryP Mle4V2FPT0WU
GI-ME-N MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTR{Lk[2O|Eh|ryP M1ezRnNCVkeHUh?=
MS-1 NXPrXIZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnuTW1KSzVyPUSyMlg6OyEQvF2= NUTFcWFSW0GQR1XS
CGTH-W-1 MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfOR|JxUUN3ME20OE46Pjl5IN88US=> M4DITXNCVkeHUh?=
NCI-H209 M{K0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXL0XYJYUUN3ME20Ok4xOTF3IN88US=> NVfWPZJzW0GQR1XS
LB2518-MEL NWC4c3RRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTR5LkC0OFgh|ryP NUHZNnhDW0GQR1XS
DU-4475 NXXlRXd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTR6LkS5N|ch|ryP M3jMb3NCVkeHUh?=
LB2241-RCC M1nQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTITWM2OD12OD62NlAzKM7:TR?= MkO3V2FPT0WU
LB771-HNC NXPmNWZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHS[mwyUUN3ME20PE46OjF{IN88US=> NYGxSWhvW0GQR1XS

... 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.
  • Formulation: Roscovitine is dissolved in either absolute methanol or DMSO and then diluted in 10% Tween 80, 20% N-N-dimethylacetamide, and 70% polyethylene glycol 400.
  • 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

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Tech Support

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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID