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 MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17iUmlEPTB;NT63OlEyPiEQvF2= MYTTRW5ITVJ?
MRK-nu-1 NGC2XnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTdwMUK5Olkh|ryP MW\TRW5ITVJ?
NCCIT NYPXfXdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLnTWM2OD15LkW1OFgzKM7:TR?= NH74XWdUSU6JRWK=
JiyoyeP-2003 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXO3UHpxUUN3ME24MlUxOjZ2IN88US=> NXPBV4ZJW0GQR1XS
KS-1 Mn33S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTlwNEW3PFUh|ryP NIPCVJpUSU6JRWK=
Becker MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzGTWM2OD17LkS2NFgzKM7:TR?= MljPV2FPT0WU
KARPAS-422 NYHtWVRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGq0WZFKSzVyPUmuPVY{OzZizszN M3L5WHNCVkeHUh?=
BB65-RCC M1;XRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLJOnlOUUN3ME25Mlk4PDl3IN88US=> M3zvSXNCVkeHUh?=
SK-UT-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XpcGlEPTB;MUCuN|Uh|ryP MmDpV2FPT0WU
ST486 M3uybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPyb45KSzVyPUGwMlM2OSEQvF2= MUXTRW5ITVJ?
LB831-BLC NIjLb4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi0[pBKSzVyPUGxMlU3OjRizszN NVjMS|FnW0GQR1XS
COR-L279 Mn7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvHc3VKSzVyPUGyMlI6ODdizszN NHHmU5FUSU6JRWK=
NB1 MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PkO2lEPTB;MUKuN|MxQCEQvF2= NUfM[W5tW0GQR1XS
D-247MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIf4fmFKSzVyPUGyMlM2OTZizszN NUjHTI86W0GQR1XS
697 MlfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3Ve5hZUUN3ME2xNk43ODB5IN88US=> M4fPOnNCVkeHUh?=
GCIY MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXYbGZKSzVyPUGyMlg3OTNizszN NEDPVYNUSU6JRWK=
RPMI-8402 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\GXI9KSzVyPUGzMlYzPjJizszN NILrOoJUSU6JRWK=
Raji MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITweZlKSzVyPUGzMlc5QTRizszN NHjSbZlUSU6JRWK=
MEG-01 NWXKTWd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly4TWM2OD1zMz64N|c6KM7:TR?= Ml\ZV2FPT0WU
RPMI-6666 NYHrW4VsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLPOppuUUN3ME2xN{46OTJzIN88US=> MmrnV2FPT0WU
SCC-3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlK0TWM2OD1zND6yPVU3KM7:TR?= MXrTRW5ITVJ?
HCC1599 Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TMR2lEPTB;MUSuOVk4PSEQvF2= MY\TRW5ITVJ?
OCI-AML2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTRUXhJUUN3ME2xOU43PDh{IN88US=> M2L3enNCVkeHUh?=
OS-RC-2 NEDHbXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nCUmlEPTB;MUWuPFM5OiEQvF2= NFX5PGJUSU6JRWK=
NCI-H1304 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHITWM2OD1zNj6zOlAyKM7:TR?= M3v2enNCVkeHUh?=
HD-MY-Z M2\GZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvmTWM2OD1zNj64NlQ3KM7:TR?= MUnTRW5ITVJ?
JAR NV:0ZW9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7QTWM2OD1zNz6wNVUzKM7:TR?= MoXWV2FPT0WU
TGW Ml\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF5LkixNlQh|ryP Mo\XV2FPT0WU
BC-3 NInTV4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DHb2lEPTB;MUiuNFMxPSEQvF2= NYq5UFRUW0GQR1XS
A101D NW\PfIhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTF6LkOyNFgh|ryP NIP0Zo1USU6JRWK=
COLO-320-HSR NXnrO2N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrnV2U1UUN3ME2xPE44Pjh6IN88US=> NE\nb3hUSU6JRWK=
LC4-1 NX\qSlhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTF6Lki3N|Qh|ryP MVnTRW5ITVJ?
BC-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjzOXBoUUN3ME2xPU4yOTl6IN88US=> NH;veItUSU6JRWK=
MHH-PREB-1 NV;abohXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mor0TWM2OD1{MD6wN|U3KM7:TR?= M3fSfnNCVkeHUh?=
BL-70 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LmSmlEPTB;MkCuN|I4PCEQvF2= Mnq0V2FPT0WU
CESS NHzYbWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXG2TIVYUUN3ME2yNE45PTR7IN88US=> M4DtenNCVkeHUh?=
ES8 M1j4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJzLkC2JO69VQ>? MV7TRW5ITVJ?
NOMO-1 M{jpbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXqblh5UUN3ME2yNU4zODB6IN88US=> NULEcWdoW0GQR1XS
ACN NXO4XohnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJzLkOzPFkh|ryP NFPNdIdUSU6JRWK=
EB-3 NV;2UXJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEmxSHpKSzVyPUKzMlE5OzFizszN NF\3XWRUSU6JRWK=
LS-513 MkCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUH3Z2FNUUN3ME2yN{42OTd7IN88US=> M3u5PHNCVkeHUh?=
HH M1fuVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ2LkO4NVkh|ryP MoXWV2FPT0WU
IST-SL2 Ml\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrzS4VyUUN3ME2yOE42OzR|IN88US=> M1\NSHNCVkeHUh?=
HOP-62 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP0TWM2OD1{NT60OFI2KM7:TR?= MlfNV2FPT0WU
NCI-H2126 NXiyW|Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVyxZYpSUUN3ME2yOU43PTJ7IN88US=> NWnNPVVzW0GQR1XS
BL-41 NHHDZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3STWM2OD1{NT65OVk4KM7:TR?= MYPTRW5ITVJ?
KURAMOCHI MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX2[293UUN3ME2yOk45ODh{IN88US=> NYn4cGhWW0GQR1XS
KARPAS-299 NYm0RYJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3BO4NKSzVyPUK2Mlg3PDZizszN MYfTRW5ITVJ?
QIMR-WIL MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:xTWM2OD1{Nz65NVQ1KM7:TR?= MWHTRW5ITVJ?
HL-60 NEXN[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e0U2lEPTB;MkeuPVg3QSEQvF2= NUDsR5BFW0GQR1XS
TE-9 M1L4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmW1TWM2OD1{OD63PVY6KM7:TR?= NHO1d2xUSU6JRWK=
TE-8 NGXUeJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHf1SnhKSzVyPUK4MlkxQCEQvF2= NWCzeHdmW0GQR1XS
NOS-1 NGf4WVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2G4T2lEPTB;MkiuPVc{OyEQvF2= MkfVV2FPT0WU
GI-1 MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjjWJBKSzVyPUK5MlAyOTNizszN MknXV2FPT0WU
KM12 M1rn[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJ7Lk[yN|kh|ryP MUDTRW5ITVJ?
BB30-HNC MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTSTWM2OD1{OT65OFg{KM7:TR?= Ml;iV2FPT0WU
ES3 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlK0TWM2OD1{OT65OVgzKM7:TR?= MkjpV2FPT0WU
NCI-H510A NFLpVFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHMUHQ{UUN3ME2zNE4xOzJ7IN88US=> NIjMU5VUSU6JRWK=
NCI-H82 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTNzLkCxN|Uh|ryP NHPGfJVUSU6JRWK=
NCI-SNU-1 NEWzW5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTNzLkGwOVkh|ryP NYTMbmFJW0GQR1XS
NKM-1 M2HYSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnqTWM2OD1|MT6xN|k4KM7:TR?= NYXCdYNQW0GQR1XS
SIG-M5 NXvqV4ZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIOwT21KSzVyPUOxMlY5OzNizszN M3HreHNCVkeHUh?=
SK-N-FI NXv6e41kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTNzLke1N|Uh|ryP MWrTRW5ITVJ?
LOUCY NV25fmFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml20TWM2OD1|Mj6xNlU{KM7:TR?= NH;S[4FUSU6JRWK=
Calu-6 M{PKfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7jTWdKSzVyPUOyMlQ4PDVizszN M{\WbXNCVkeHUh?=
GOTO MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrQepN2UUN3ME2zNk46OTJ7IN88US=> MkDuV2FPT0WU
NCI-H526 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\YXWZKSzVyPUOzMlQ6OzZizszN M3n4NXNCVkeHUh?=
RKO NFv0NXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmK4TWM2OD1|Mz61PVY6KM7:TR?= NILyV4FUSU6JRWK=
NCI-H64 MoLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLP[ZVRUUN3ME2zN{45PTl5IN88US=> MmXWV2FPT0WU
LP-1 NYfiZWhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;4W2lEPTB;M{OuPFkxQCEQvF2= MVLTRW5ITVJ?
KGN M1H0b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTN2LkK1NlQh|ryP MXvTRW5ITVJ?
NCI-H2141 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[0VpR5UUN3ME2zOE43PTN|IN88US=> MlnQV2FPT0WU
TE-10 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTN2Lkm0NlIh|ryP MoLNV2FPT0WU
K5 M17aT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zlUWlEPTB;M{WuNFg3OSEQvF2= NY\5RWNiW0GQR1XS
IMR-5 M4P1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTN3LkOxN|kh|ryP NUjSfXBWW0GQR1XS
TE-441-T NHXCcYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonyTWM2OD1|Nj6xNVQ5KM7:TR?= MnfuV2FPT0WU
TE-6 NHrQSYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED5dYRKSzVyPUO2MlMzPDZizszN NWjW[Wo4W0GQR1XS
MOLT-4 M1LXcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTN4LkOyO|Yh|ryP NGq2d|ZUSU6JRWK=
COLO-684 NILON|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13KZ2lEPTB;M{euNFEzKM7:TR?= MnvBV2FPT0WU
LU-139 NUPVO4RJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDyWFlKSzVyPUO3MlE5PTZizszN MVXTRW5ITVJ?
OPM-2 MkD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTN5LkK5OFkh|ryP NXH4dHVoW0GQR1XS
ML-2 NU\IWJM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTN5Lk[3NVIh|ryP NVz2SJVpW0GQR1XS
RS4-11 NGHVfY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HxSGlEPTB;M{euO|A3QSEQvF2= MXXTRW5ITVJ?
MONO-MAC-6 NILDSWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHNTWM2OD1|OD6yOFc4KM7:TR?= M4HjUnNCVkeHUh?=
NCI-H345 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELCU2dKSzVyPUO4MlkyODZizszN NI\lWIVUSU6JRWK=
NTERA-S-cl-D1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLyPJRKSzVyPUO5MlU5PDJizszN NEi0eXRUSU6JRWK=
NCI-H1882 NF[yW2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPzS5BbUUN3ME20NE42QTl6IN88US=> MnfoV2FPT0WU
LC-1F NFvNW2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4O5eWlEPTB;NEGuOVcxPSEQvF2= MWnTRW5ITVJ?
HT MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTR{LkCwNlgh|ryP MWjTRW5ITVJ?
MLMA NGX1[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTR{LkK3PFch|ryP NW\QWHp7W0GQR1XS
DG-75 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTUOHdUUUN3ME20Nk43PTR4IN88US=> MV7TRW5ITVJ?
GI-ME-N NFnvbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDJTWM2OD12Mj62OlcyKM7:TR?= M3;VUHNCVkeHUh?=
MS-1 NEDtNYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTR{Lki5N{DPxE1? NXTaUGtZW0GQR1XS
CGTH-W-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTR2Lkm2PVch|ryP MVjTRW5ITVJ?
NCI-H209 MmDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz6TWM2OD12Nj6wNVE2KM7:TR?= NWn2[2lxW0GQR1XS
LB2518-MEL MoT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnH[ZBMUUN3ME20O{4xPDR6IN88US=> M3;PV3NCVkeHUh?=
DU-4475 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHC[2JuUUN3ME20PE41QTN5IN88US=> M1u4NXNCVkeHUh?=
LB2241-RCC NFrUPIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\pTWM2OD12OD62NlAzKM7:TR?= MXLTRW5ITVJ?
LB771-HNC NVP2bWVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR6LkmyNVIh|ryP M2[5d3NCVkeHUh?=

... 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