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 29 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 NX;3NZhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\0bHFKSzVyPUWuO|YyOTZizszN M1rFOnNCVkeHUh?=
MRK-nu-1 M2rqOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTdwMUK5Olkh|ryP MVPTRW5ITVJ?
NCCIT MmLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f1[WlEPTB;Nz61OVQ5OiEQvF2= Mlq4V2FPT0WU
JiyoyeP-2003 NULSRoJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHNTWM2OD16LkWwNlY1KM7:TR?= NHTyemJUSU6JRWK=
KS-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\hWGlEPTB;OT60OVc5PSEQvF2= Ml\UV2FPT0WU
Becker NInn[Y9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfzZmFKUUN3ME25MlQ3ODh{IN88US=> MX;TRW5ITVJ?
KARPAS-422 NXjtN2dqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHGTWM2OD17Lkm2N|M3KM7:TR?= MXvTRW5ITVJ?
BB65-RCC MlXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HPN2lEPTB;OT65O|Q6PSEQvF2= MYPTRW5ITVJ?
SK-UT-1 NHfLU2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTWTWM2OD1zMD6zOUDPxE1? M3viZnNCVkeHUh?=
ST486 MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLTW5FKSzVyPUGwMlM2OSEQvF2= NIXufXVUSU6JRWK=
LB831-BLC MnLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoSwTWM2OD1zMT61OlI1KM7:TR?= NHW4SpJUSU6JRWK=
COR-L279 MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF{LkK5NFch|ryP MWPTRW5ITVJ?
NB1 NIjaSG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkm1TWM2OD1zMj6zN|A5KM7:TR?= M1\6c3NCVkeHUh?=
D-247MG NYO5XmtMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHuxd5hKSzVyPUGyMlM2OTZizszN MkKxV2FPT0WU
697 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHDOY9KSzVyPUGyMlYxODdizszN MlvZV2FPT0WU
GCIY NEHtfJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLhNHNKSzVyPUGyMlg3OTNizszN M33Od3NCVkeHUh?=
RPMI-8402 NWTnZ|VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LO[WlEPTB;MUOuOlI3OiEQvF2= MX3TRW5ITVJ?
Raji NGDZeJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzCTWM2OD1zMz63PFk1KM7:TR?= M2TSTnNCVkeHUh?=
MEG-01 NFXo[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF|LkizO|kh|ryP M1X0bXNCVkeHUh?=
RPMI-6666 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfaRZhIUUN3ME2xN{46OTJzIN88US=> MkPyV2FPT0WU
SCC-3 NGnaZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi5fZBiUUN3ME2xOE4zQTV4IN88US=> MlrJV2FPT0WU
HCC1599 NXXCU2wzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLRTWM2OD1zND61PVc2KM7:TR?= M2XKPXNCVkeHUh?=
OCI-AML2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTF3Lk[0PFIh|ryP NV7R[YpkW0GQR1XS
OS-RC-2 M1vhN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LQOWlEPTB;MUWuPFM5OiEQvF2= MYLTRW5ITVJ?
NCI-H1304 NWPxbGp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrqdXVKSzVyPUG2MlM3ODFizszN NIrCSHJUSU6JRWK=
HD-MY-Z Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O5emlEPTB;MU[uPFI1PiEQvF2= M4C1OnNCVkeHUh?=
JAR NEm5T3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnGyTWM2OD1zNz6wNVUzKM7:TR?= NYjDWlVCW0GQR1XS
TGW NYPTbmdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHT5fIpKSzVyPUG3MlgyOjRizszN Mo\YV2FPT0WU
BC-3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT0UlJKSzVyPUG4MlA{ODVizszN NI\oRWtUSU6JRWK=
A101D MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHqcGIxUUN3ME2xPE4{OjB6IN88US=> M3PSZnNCVkeHUh?=
COLO-320-HSR NUDCfmNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTtTWM2OD1zOD63Olg5KM7:TR?= M3f0d3NCVkeHUh?=
LC4-1 M4PmT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLKZoQ{UUN3ME2xPE45PzN2IN88US=> NXG4O3R7W0GQR1XS
BC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLPTWM2OD1zOT6xNVk5KM7:TR?= M3K4fHNCVkeHUh?=
MHH-PREB-1 NYnLWIxsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJyLkCzOVYh|ryP M1TqbHNCVkeHUh?=
BL-70 NWKwdJI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m0TmlEPTB;MkCuN|I4PCEQvF2= MXTTRW5ITVJ?
CESS NV3md5BNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3Tcm11UUN3ME2yNE45PTR7IN88US=> NFXH[lJUSU6JRWK=
ES8 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LucGlEPTB;MkGuNFYh|ryP MXrTRW5ITVJ?
NOMO-1 MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7KTWM2OD1{MT6yNFA5KM7:TR?= MmXDV2FPT0WU
ACN NXjsdm5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXvTWM2OD1{MT6zN|g6KM7:TR?= NXGzbFdyW0GQR1XS
EB-3 NXLNOlZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q3dGlEPTB;MkOuNVg{OSEQvF2= NHTCR5NUSU6JRWK=
LS-513 MnT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rXdmlEPTB;MkOuOVE4QSEQvF2= MofqV2FPT0WU
HH M3fVRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJ2LkO4NVkh|ryP MoSxV2FPT0WU
IST-SL2 MlTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzsbVJKSzVyPUK0MlU{PDNizszN NVvVU|JtW0GQR1XS
HOP-62 NUPVcoc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfITWM2OD1{NT60OFI2KM7:TR?= NYjPOFJSW0GQR1XS
NCI-H2126 NV;KV4tZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LOSWlEPTB;MkWuOlUzQSEQvF2= MXHTRW5ITVJ?
BL-41 MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfIV|ZKSzVyPUK1Mlk2QTdizszN MlHPV2FPT0WU
KURAMOCHI M1PWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHS0c|VKSzVyPUK2MlgxQDJizszN MVfTRW5ITVJ?
KARPAS-299 NILuT4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r5VmlEPTB;Mk[uPFY1PiEQvF2= MUXTRW5ITVJ?
QIMR-WIL MoniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnrNZdKSzVyPUK3MlkyPDRizszN MmjLV2FPT0WU
HL-60 M3zxcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\kWnRKSzVyPUK3Mlk5PjlizszN M1[yd3NCVkeHUh?=
TE-9 NHfEcY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3u2VGlEPTB;MkiuO|k3QSEQvF2= M3XrfnNCVkeHUh?=
TE-8 M1jLd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJ6LkmwPEDPxE1? NFnrb4RUSU6JRWK=
NOS-1 MlXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7GTWM2OD1{OD65O|M{KM7:TR?= NFf0bGpUSU6JRWK=
GI-1 M2Gwb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Xkb2lEPTB;MkmuNFEyOyEQvF2= NGrqXlZUSU6JRWK=
KM12 MmL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\Gb5oyUUN3ME2yPU43OjN7IN88US=> M2jsbnNCVkeHUh?=
BB30-HNC NWTEOIp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILXVXhKSzVyPUK5Mlk1QDNizszN M3LRZ3NCVkeHUh?=
ES3 NUfvOmV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjLbnI5UUN3ME2yPU46PTh{IN88US=> NVG0Z2k5W0GQR1XS
NCI-H510A MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTNyLkCzNlkh|ryP NGS4bpFUSU6JRWK=
NCI-H82 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3viPGlEPTB;M{GuNFE{PSEQvF2= NH;XfJVUSU6JRWK=
NCI-SNU-1 MlzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojaTWM2OD1|MT6xNFU6KM7:TR?= M{fDW3NCVkeHUh?=
NKM-1 M17mZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HSXmlEPTB;M{GuNVM6PyEQvF2= M3rFO3NCVkeHUh?=
SIG-M5 NHL6OmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PqO2lEPTB;M{GuOlg{OyEQvF2= NXT5Nm5JW0GQR1XS
SK-N-FI M{HmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXWV|ZOUUN3ME2zNU44PTN3IN88US=> NGLLUoJUSU6JRWK=
LOUCY MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDldY5KSzVyPUOyMlEzPTNizszN NFK3RnlUSU6JRWK=
Calu-6 M4HJSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTJVm8yUUN3ME2zNk41PzR3IN88US=> NF;GOmlUSU6JRWK=
GOTO M4S4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[yWWlEPTB;M{KuPVEzQSEQvF2= M{DNeHNCVkeHUh?=
NCI-H526 NIG4NWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjETWM2OD1|Mz60PVM3KM7:TR?= NYK1c3kxW0GQR1XS
RKO MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TSNmlEPTB;M{OuOVk3QSEQvF2= Ml;nV2FPT0WU
NCI-H64 MofXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTN|Lki1PVch|ryP MWfTRW5ITVJ?
LP-1 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTnTWM2OD1|Mz64PVA5KM7:TR?= M13ZdnNCVkeHUh?=
KGN MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\3eGlEPTB;M{SuNlUzPCEQvF2= M4PRUnNCVkeHUh?=
NCI-H2141 NGfHOm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nUbmlEPTB;M{SuOlU{OyEQvF2= M3XsNHNCVkeHUh?=
TE-10 MnTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TKWWlEPTB;M{SuPVQzOiEQvF2= MnyyV2FPT0WU
K5 NG\0XZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTjTWM2OD1|NT6wPFYyKM7:TR?= NV\aRWE1W0GQR1XS
IMR-5 M1\6cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTN3LkOxN|kh|ryP NEC2Um5USU6JRWK=
TE-441-T NHvXUnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[xTWM2OD1|Nj6xNVQ5KM7:TR?= NUizV2t[W0GQR1XS
TE-6 NGDocmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\pbG5ZUUN3ME2zOk4{OjR4IN88US=> M4PjNHNCVkeHUh?=
MOLT-4 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjKdY5KSzVyPUO2MlMzPzZizszN MWrTRW5ITVJ?
COLO-684 M1\kRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXCZ5VKSzVyPUO3MlAyOiEQvF2= NG\xO2FUSU6JRWK=
LU-139 M{jYUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\GemlEPTB;M{euNVg2PiEQvF2= M3vUW3NCVkeHUh?=
OPM-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;FTWM2OD1|Nz6yPVQ6KM7:TR?= MVrTRW5ITVJ?
ML-2 M2nNfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmn6TWM2OD1|Nz62O|EzKM7:TR?= NHnodHRUSU6JRWK=
RS4-11 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTN5LkewOlkh|ryP NITFXmJUSU6JRWK=
MONO-MAC-6 NEfQWG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG2Um9KSzVyPUO4MlI1PzdizszN M2W3V3NCVkeHUh?=
NCI-H345 NIPSZ4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe2O3FKSzVyPUO4MlkyODZizszN NX;WepVNW0GQR1XS
NTERA-S-cl-D1 MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3BTWM2OD1|OT61PFQzKM7:TR?= M2faRXNCVkeHUh?=
NCI-H1882 NF36WWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XESGlEPTB;NECuOVk6QCEQvF2= NUXwbYwyW0GQR1XS
LC-1F MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:5VGlEPTB;NEGuOVcxPSEQvF2= Ml3FV2FPT0WU
HT NFjyUItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2f0VmlEPTB;NEKuNFAzQCEQvF2= NYnaNHpoW0GQR1XS
MLMA NX7ZT|hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\vNIx7UUN3ME20Nk4zPzh5IN88US=> MXXTRW5ITVJ?
DG-75 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC3OnB7UUN3ME20Nk43PTR4IN88US=> MlXsV2FPT0WU
GI-ME-N NE\HfGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTR{Lk[2O|Eh|ryP NIPl[YRUSU6JRWK=
MS-1 MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXZdo5KSzVyPUSyMlg6OyEQvF2= NUjHTI1XW0GQR1XS
CGTH-W-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vYVmlEPTB;NESuPVY6PyEQvF2= MXrTRW5ITVJ?
NCI-H209 MljMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL6TWM2OD12Nj6wNVE2KM7:TR?= MXrTRW5ITVJ?
LB2518-MEL MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3OU2pKSzVyPUS3MlA1PDhizszN Mom0V2FPT0WU
DU-4475 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTR6LkS5N|ch|ryP M3XxOHNCVkeHUh?=
LB2241-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGP5d2ZKSzVyPUS4MlYzODJizszN NHq2dolUSU6JRWK=
LB771-HNC NWTOO5NCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK3TWM2OD12OD65NlEzKM7:TR?= MXXTRW5ITVJ?

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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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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