Roscovitine (Seliciclib,CYC202)

For research use only. Not for use in humans.

Catalog No.S1153

53 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 53 publications

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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 M3rDNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrtUFVKSzVyPUWuO|YyOTZizszN NEfsPIpUSU6JRWK=
MRK-nu-1 NYrH[2ZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfiWZVmUUN3ME23MlEzQTZ7IN88US=> M2TUcHNCVkeHUh?=
NCCIT NV3rS4hoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHBcY9KSzVyPUeuOVU1QDJizszN MUfTRW5ITVJ?
JiyoyeP-2003 NVPIWFFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHpTm5KSzVyPUiuOVAzPjRizszN MXnTRW5ITVJ?
KS-1 MlLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLQRZlYUUN3ME25MlQ2Pzh3IN88US=> MVvTRW5ITVJ?
Becker M4m0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTlwNE[wPFIh|ryP MnXLV2FPT0WU
KARPAS-422 NGXCeWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHBW3BKSzVyPUmuPVY{OzZizszN MkLFV2FPT0WU
BB65-RCC NYj3eYY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDTSXJKSzVyPUmuPVc1QTVizszN MYLTRW5ITVJ?
SK-UT-1 NVWzVpJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFyLkO1JO69VQ>? NHTvS3hUSU6JRWK=
ST486 M2L0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TlU2lEPTB;MUCuN|UyKM7:TR?= M2rSVnNCVkeHUh?=
LB831-BLC Mo\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\UOohPUUN3ME2xNU42PjJ2IN88US=> MUfTRW5ITVJ?
COR-L279 MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LVfGlEPTB;MUKuNlkxPyEQvF2= M1O4TnNCVkeHUh?=
NB1 NX71bZZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4WydWlEPTB;MUKuN|MxQCEQvF2= M2GweXNCVkeHUh?=
D-247MG NYj2Nlh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnTPW1{UUN3ME2xNk4{PTF4IN88US=> M1LhfXNCVkeHUh?=
697 NYrjRYFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HSbmlEPTB;MUKuOlAxPyEQvF2= MV3TRW5ITVJ?
GCIY NV;CS4wxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPzTWM2OD1zMj64OlE{KM7:TR?= NVXafJgyW0GQR1XS
RPMI-8402 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF|Lk[yOlIh|ryP M{XMdXNCVkeHUh?=
Raji M{DSbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfybpVlUUN3ME2xN{44QDl2IN88US=> MWPTRW5ITVJ?
MEG-01 M1y5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX4dXBSUUN3ME2xN{45Ozd7IN88US=> M{XzUXNCVkeHUh?=
RPMI-6666 NH:1UWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF|LkmxNlEh|ryP NX\GfHp7W0GQR1XS
SCC-3 M2Pq[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTF2LkK5OVYh|ryP NWe0ZnRrW0GQR1XS
HCC1599 NYn1c2dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fSeGlEPTB;MUSuOVk4PSEQvF2= M{HjZnNCVkeHUh?=
OCI-AML2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTF3Lk[0PFIh|ryP NFm4RWFUSU6JRWK=
OS-RC-2 NVjV[2tkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWiwTlRYUUN3ME2xOU45Ozh{IN88US=> NYfkTGVjW0GQR1XS
NCI-H1304 NUewdnNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rFc2lEPTB;MU[uN|YxOSEQvF2= NXLL[2hWW0GQR1XS
HD-MY-Z MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonsTWM2OD1zNj64NlQ3KM7:TR?= NEH6OZFUSU6JRWK=
JAR M3Pocmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HEb2lEPTB;MUeuNFE2OiEQvF2= NYfweYR6W0GQR1XS
TGW M1vkXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\obWZPUUN3ME2xO{45OTJ2IN88US=> NHWwZ2lUSU6JRWK=
BC-3 MoHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzBUGtKSzVyPUG4MlA{ODVizszN NIezeXVUSU6JRWK=
A101D MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXOTWM2OD1zOD6zNlA5KM7:TR?= NH70VGxUSU6JRWK=
COLO-320-HSR MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLNTWM2OD1zOD63Olg5KM7:TR?= M1yzNHNCVkeHUh?=
LC4-1 NInCeoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LGemlEPTB;MUiuPFc{PCEQvF2= NYjQfG5sW0GQR1XS
BC-1 NI\EempIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7wTWM2OD1zOT6xNVk5KM7:TR?= MlXGV2FPT0WU
MHH-PREB-1 NELEfIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTJyLkCzOVYh|ryP MkLtV2FPT0WU
BL-70 NVvFPYpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\lTWM2OD1{MD6zNlc1KM7:TR?= MmXaV2FPT0WU
CESS NYnwcWE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJyLki1OFkh|ryP NUHFOmhnW0GQR1XS
ES8 NHT5XGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJzLkC2JO69VQ>? NUnNSmQyW0GQR1XS
NOMO-1 NGe1O3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPmTWM2OD1{MT6yNFA5KM7:TR?= Mo[wV2FPT0WU
ACN MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojITWM2OD1{MT6zN|g6KM7:TR?= Mn3JV2FPT0WU
EB-3 MlfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJ|LkG4N|Eh|ryP NUfsUpE{W0GQR1XS
LS-513 NF:2UGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XaXGlEPTB;MkOuOVE4QSEQvF2= MVjTRW5ITVJ?
HH NWD3[ItZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPWTWM2OD1{ND6zPFE6KM7:TR?= MlXkV2FPT0WU
IST-SL2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrvcHhKSzVyPUK0MlU{PDNizszN NF61NmlUSU6JRWK=
HOP-62 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XhbGlEPTB;MkWuOFQzPSEQvF2= M3XTOnNCVkeHUh?=
NCI-H2126 MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;YTWM2OD1{NT62OVI6KM7:TR?= MWnTRW5ITVJ?
BL-41 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzqTWM2OD1{NT65OVk4KM7:TR?= NFnyfmhUSU6JRWK=
KURAMOCHI NETzT2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TlTGlEPTB;Mk[uPFA5OiEQvF2= Mk\MV2FPT0WU
KARPAS-299 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETsd3BKSzVyPUK2Mlg3PDZizszN MmnVV2FPT0WU
QIMR-WIL NVjKTGlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O5WGlEPTB;MkeuPVE1PCEQvF2= NGG4So9USU6JRWK=
HL-60 M{jLPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTJ5Lkm4Olkh|ryP NFvJZ4VUSU6JRWK=
TE-9 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP5fpFKSzVyPUK4Mlc6PjlizszN NXzCUpFxW0GQR1XS
TE-8 NX72T5RFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X2bWlEPTB;MkiuPVA5KM7:TR?= MVvTRW5ITVJ?
NOS-1 NUT2XIJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTFUGVKSzVyPUK4Mlk4OzNizszN NHGz[3JUSU6JRWK=
GI-1 Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LEZWlEPTB;MkmuNFEyOyEQvF2= NY\6fmlYW0GQR1XS
KM12 NYnDd4dwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLiTWM2OD1{OT62NlM6KM7:TR?= MWHTRW5ITVJ?
BB30-HNC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJ7Lkm0PFMh|ryP MknTV2FPT0WU
ES3 M1S2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELae3BKSzVyPUK5Mlk2QDJizszN NVL2S4l4W0GQR1XS
NCI-H510A NFe2PJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rrWGlEPTB;M{CuNFMzQSEQvF2= MV\TRW5ITVJ?
NCI-H82 NG\mVlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTNzLkCxN|Uh|ryP MnrWV2FPT0WU
NCI-SNU-1 NVrtTG9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHIc4MxUUN3ME2zNU4yODV7IN88US=> MVfTRW5ITVJ?
NKM-1 M3m1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW0TWM2OD1|MT6xN|k4KM7:TR?= MlTHV2FPT0WU
SIG-M5 NEfsOIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4foUWlEPTB;M{GuOlg{OyEQvF2= MYjTRW5ITVJ?
SK-N-FI M3HhVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTNzLke1N|Uh|ryP Moj6V2FPT0WU
LOUCY MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPKZWR7UUN3ME2zNk4yOjV|IN88US=> NFLmTZFUSU6JRWK=
Calu-6 NYPwdlZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr3eFduUUN3ME2zNk41PzR3IN88US=> NX3EepZ2W0GQR1XS
GOTO NWnWcnY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3YTWM2OD1|Mj65NVI6KM7:TR?= M3OyS3NCVkeHUh?=
NCI-H526 NWXaZXVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTN|LkS5N|Yh|ryP NFT2[GJUSU6JRWK=
RKO M2P5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[zTWM2OD1|Mz61PVY6KM7:TR?= MYXTRW5ITVJ?
NCI-H64 M3S1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDGb4xKSzVyPUOzMlg2QTdizszN MXnTRW5ITVJ?
LP-1 M2fse2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWniNnF{UUN3ME2zN{45QTB6IN88US=> MUnTRW5ITVJ?
KGN MkPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHqVVNKSzVyPUO0MlI2OjRizszN M3rT[XNCVkeHUh?=
NCI-H2141 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTN2Lk[1N|Mh|ryP M1frNXNCVkeHUh?=
TE-10 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLLTWM2OD1|ND65OFIzKM7:TR?= NVXvdpBZW0GQR1XS
K5 NULIdnZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HYfWlEPTB;M{WuNFg3OSEQvF2= NEOwTpRUSU6JRWK=
IMR-5 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTN3LkOxN|kh|ryP NHHVSpZUSU6JRWK=
TE-441-T MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGT0[nZKSzVyPUO2MlEyPDhizszN MUTTRW5ITVJ?
TE-6 MkjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PHcGlEPTB;M{[uN|I1PiEQvF2= Ml\uV2FPT0WU
MOLT-4 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C2RmlEPTB;M{[uN|I4PiEQvF2= M3zIVnNCVkeHUh?=
COLO-684 NFS3PI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\EfJNKSzVyPUO3MlAyOiEQvF2= MXLTRW5ITVJ?
LU-139 NFT6TW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN5LkG4OVYh|ryP NWLHfnJsW0GQR1XS
OPM-2 M3vkXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfwbHlKSzVyPUO3MlI6PDlizszN MkXTV2FPT0WU
ML-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTN5Lk[3NVIh|ryP M4foeXNCVkeHUh?=
RS4-11 NXq0Zo9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{H0U2lEPTB;M{euO|A3QSEQvF2= MnnrV2FPT0WU
MONO-MAC-6 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TWNWlEPTB;M{iuNlQ4PyEQvF2= NHnyeppUSU6JRWK=
NCI-H345 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\hO|ZLUUN3ME2zPE46OTB4IN88US=> NY\OT|VYW0GQR1XS
NTERA-S-cl-D1 NY\mOpl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:3[JdKSzVyPUO5MlU5PDJizszN Mmq1V2FPT0WU
NCI-H1882 MnLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3jTWM2OD12MD61PVk5KM7:TR?= MYLTRW5ITVJ?
LC-1F NGjCN3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfVWlcxUUN3ME20NU42PzB3IN88US=> NXqzSmpJW0GQR1XS
HT MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDzUWpPUUN3ME20Nk4xODJ6IN88US=> MYTTRW5ITVJ?
MLMA MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q4cGlEPTB;NEKuNlc5PyEQvF2= MULTRW5ITVJ?
DG-75 M4nkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17aTWlEPTB;NEKuOlU1PiEQvF2= NXq4UnNDW0GQR1XS
GI-ME-N NHHxbXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjsfmRTUUN3ME20Nk43PjdzIN88US=> MWrTRW5ITVJ?
MS-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljETWM2OD12Mj64PVMh|ryP MUTTRW5ITVJ?
CGTH-W-1 NIe5dpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rFS2lEPTB;NESuPVY6PyEQvF2= NHjScmZUSU6JRWK=
NCI-H209 M2XG[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD4TWM2OD12Nj6wNVE2KM7:TR?= M{\XUXNCVkeHUh?=
LB2518-MEL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvsTWM2OD12Nz6wOFQ5KM7:TR?= NVK2[Y91W0GQR1XS
DU-4475 M1jDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXWxdIpYUUN3ME20PE41QTN5IN88US=> M17veHNCVkeHUh?=
LB2241-RCC NGXiTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfUTWM2OD12OD62NlAzKM7:TR?= M2T4U3NCVkeHUh?=
LB771-HNC NV64SWY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP5VWZQUUN3ME20PE46OjF{IN88US=> NHS2ZWJUSU6JRWK=

... 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
Smiles CCC(CO)NC1=NC(=C2N=C[N](C(C)C)C2=N1)NCC3=CC=CC=C3

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID