Roscovitine (Seliciclib)

For research use only.

Catalog No.S1153 Synonyms: CYC202

71 publications

Roscovitine (Seliciclib) Chemical Structure

CAS No. 186692-46-6

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) has been cited by 71 publications

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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 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NECyWYxKSzVyPUWuO|YyOTZizszN MnP4V2FPT0WU
MRK-nu-1 NH[2PHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXGwW3JxUUN3ME23MlEzQTZ7IN88US=> NF\DTZZUSU6JRWK=
NCCIT MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO0[FZDUUN3ME23MlU2PDh{IN88US=> M2nHb3NCVkeHUh?=
JiyoyeP-2003 M1XiV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi0NVVKSzVyPUiuOVAzPjRizszN NHL6VVVUSU6JRWK=
KS-1 NXW4ZXRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHIUlF5UUN3ME25MlQ2Pzh3IN88US=> Mn7VV2FPT0WU
Becker MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e2[mlEPTB;OT60OlA5OiEQvF2= M1L0OnNCVkeHUh?=
KARPAS-422 NILtTYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LDXWlEPTB;OT65OlM{PiEQvF2= MVjTRW5ITVJ?
BB65-RCC NV\CU|ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIqzWYpKSzVyPUmuPVc1QTVizszN MWnTRW5ITVJ?
SK-UT-1 NYm0NlVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfWV3NDUUN3ME2xNE4{PSEQvF2= Mn;1V2FPT0WU
ST486 NVKyTINvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLZTWM2OD1zMD6zOVEh|ryP M{LPW3NCVkeHUh?=
LB831-BLC NVTve2dRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFzLkW2NlQh|ryP MYjTRW5ITVJ?
COR-L279 MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTF{LkK5NFch|ryP NHrEU4hUSU6JRWK=
NB1 M3:zb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzETWM2OD1zMj6zN|A5KM7:TR?= NVfxWnpwW0GQR1XS
D-247MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF{LkO1NVYh|ryP NIfXWXlUSU6JRWK=
697 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1juV2lEPTB;MUKuOlAxPyEQvF2= MnfoV2FPT0WU
GCIY MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnnTWM2OD1zMj64OlE{KM7:TR?= MYHTRW5ITVJ?
RPMI-8402 MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTF|Lk[yOlIh|ryP MoHsV2FPT0WU
Raji NVradG1oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnTTWM2OD1zMz63PFk1KM7:TR?= MW\TRW5ITVJ?
MEG-01 NXnv[W1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4f6dGlEPTB;MUOuPFM4QSEQvF2= MXnTRW5ITVJ?
RPMI-6666 NUnWcJd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofvTWM2OD1zMz65NVIyKM7:TR?= MoDnV2FPT0WU
SCC-3 M2DYR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjCRnNKSzVyPUG0MlI6PTZizszN M3mzfnNCVkeHUh?=
HCC1599 NETxN4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVG2SFA5UUN3ME2xOE42QTd3IN88US=> NH6wOIpUSU6JRWK=
OCI-AML2 M3j5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PabWlEPTB;MUWuOlQ5OiEQvF2= MXvTRW5ITVJ?
OS-RC-2 NUHDXlUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq0fpNKUUN3ME2xOU45Ozh{IN88US=> MofUV2FPT0WU
NCI-H1304 NWPyWFc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTF4LkO2NFEh|ryP MoDEV2FPT0WU
HD-MY-Z NGfSSY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPtPIlGUUN3ME2xOk45OjR4IN88US=> NX[5SnN7W0GQR1XS
JAR MlrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;3TWM2OD1zNz6wNVUzKM7:TR?= NIXtSmlUSU6JRWK=
TGW M4HX[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XXbWlEPTB;MUeuPFEzPCEQvF2= M4DMWnNCVkeHUh?=
BC-3 NWmwNWFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvadFVKSzVyPUG4MlA{ODVizszN MmiwV2FPT0WU
A101D NF3Oco5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTyWJFKSzVyPUG4MlMzODhizszN NYC0VmlWW0GQR1XS
COLO-320-HSR NUjjZmRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTF6Lke2PFgh|ryP NF\VOVlUSU6JRWK=
LC4-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor1TWM2OD1zOD64O|M1KM7:TR?= MmHSV2FPT0WU
BC-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fBXGlEPTB;MUmuNVE6QCEQvF2= Mn3uV2FPT0WU
MHH-PREB-1 M2i4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXftT4o1UUN3ME2yNE4xOzV4IN88US=> M3m0fXNCVkeHUh?=
BL-70 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfWdpRKSzVyPUKwMlMzPzRizszN MX;TRW5ITVJ?
CESS M3LjVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzWN2pbUUN3ME2yNE45PTR7IN88US=> NIPwUHNUSU6JRWK=
ES8 MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\3XIZKSzVyPUKxMlA3KM7:TR?= M3X3SXNCVkeHUh?=
NOMO-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;I[3pKSzVyPUKxMlIxODhizszN NV\xVohuW0GQR1XS
ACN MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF61[XpKSzVyPUKxMlM{QDlizszN NY\BcIRXW0GQR1XS
EB-3 NU\0WlF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\VOlNKUUN3ME2yN{4yQDNzIN88US=> NHrZfJdUSU6JRWK=
LS-513 Mk\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJ|LkWxO|kh|ryP NGLIdndUSU6JRWK=
HH NWrkWnZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fWW2lEPTB;MkSuN|gyQSEQvF2= NYTYWIxQW0GQR1XS
IST-SL2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnBdVFVUUN3ME2yOE42OzR|IN88US=> NXLLe4hQW0GQR1XS
HOP-62 NWrDXIJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJ3LkS0NlUh|ryP NYL2XW57W0GQR1XS
NCI-H2126 NUizbppxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPPTWM2OD1{NT62OVI6KM7:TR?= NHnCNZVUSU6JRWK=
BL-41 NWDUUXN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljCTWM2OD1{NT65OVk4KM7:TR?= NGfPSHJUSU6JRWK=
KURAMOCHI M1y4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIewSo5KSzVyPUK2MlgxQDJizszN NVvlR2xVW0GQR1XS
KARPAS-299 MnPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITybmFKSzVyPUK2Mlg3PDZizszN MXfTRW5ITVJ?
QIMR-WIL NGi2WIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmOyTWM2OD1{Nz65NVQ1KM7:TR?= Mli0V2FPT0WU
HL-60 NUfIWHRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7zcJVyUUN3ME2yO{46QDZ7IN88US=> NF;B[4NUSU6JRWK=
TE-9 NFj0fWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ6Lke5Olkh|ryP MWTTRW5ITVJ?
TE-8 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TtPGlEPTB;MkiuPVA5KM7:TR?= MkLRV2FPT0WU
NOS-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHhemlKSzVyPUK4Mlk4OzNizszN NFHMUHJUSU6JRWK=
GI-1 NV7U[lZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fnNmlEPTB;MkmuNFEyOyEQvF2= Mmj0V2FPT0WU
KM12 NHz5VnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHwVYVKSzVyPUK5MlYzOzlizszN NWfqXmpiW0GQR1XS
BB30-HNC M3T0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7oTWM2OD1{OT65OFg{KM7:TR?= NXO2U2Z3W0GQR1XS
ES3 M1;jUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJ7Lkm1PFIh|ryP M1rlWHNCVkeHUh?=
NCI-H510A NUXrXogzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEiwN4hKSzVyPUOwMlA{OjlizszN MYXTRW5ITVJ?
NCI-H82 M1ywbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj5TWM2OD1|MT6wNVM2KM7:TR?= NFLqcG9USU6JRWK=
NCI-SNU-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TvdmlEPTB;M{GuNVA2QSEQvF2= MV7TRW5ITVJ?
NKM-1 MlHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTNzLkGzPVch|ryP MWHTRW5ITVJ?
SIG-M5 Mkj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTrWGdqUUN3ME2zNU43QDN|IN88US=> M1WwVHNCVkeHUh?=
SK-N-FI M2XvXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLhOZJUUUN3ME2zNU44PTN3IN88US=> MknHV2FPT0WU
LOUCY NWLmcnlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTN{LkGyOVMh|ryP NFy1OFVUSU6JRWK=
Calu-6 MkPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvjSHdKSzVyPUOyMlQ4PDVizszN M4G4THNCVkeHUh?=
GOTO MljkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXQbpBHUUN3ME2zNk46OTJ7IN88US=> NGO4eWxUSU6JRWK=
NCI-H526 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;1TWM2OD1|Mz60PVM3KM7:TR?= NGLwOXJUSU6JRWK=
RKO MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzaNG9KSzVyPUOzMlU6PjlizszN Mli1V2FPT0WU
NCI-H64 NV\KXoFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Ly[WlEPTB;M{OuPFU6PyEQvF2= M4\zZ3NCVkeHUh?=
LP-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7JN2xMUUN3ME2zN{45QTB6IN88US=> MmrtV2FPT0WU
KGN Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj6V3p7UUN3ME2zOE4zPTJ2IN88US=> Ml62V2FPT0WU
NCI-H2141 NGrwSWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDCcJJKSzVyPUO0MlY2OzNizszN MVzTRW5ITVJ?
TE-10 M1m0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPyT5VKSzVyPUO0Mlk1OjJizszN MXrTRW5ITVJ?
K5 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1m2O2lEPTB;M{WuNFg3OSEQvF2= MlvJV2FPT0WU
IMR-5 MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTN3LkOxN|kh|ryP MWHTRW5ITVJ?
TE-441-T Ml3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\2UGlEPTB;M{[uNVE1QCEQvF2= NVTldlZjW0GQR1XS
TE-6 NYnxW2tET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXETWM2OD1|Nj6zNlQ3KM7:TR?= M123NnNCVkeHUh?=
MOLT-4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPSPJFKSzVyPUO2MlMzPzZizszN MmryV2FPT0WU
COLO-684 NVzBbYpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfpZWZKSzVyPUO3MlAyOiEQvF2= NF7zOJVUSU6JRWK=
LU-139 NXr1c3B4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPPWFRNUUN3ME2zO{4yQDV4IN88US=> NVXIZVNnW0GQR1XS
OPM-2 NGq1R|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTN5LkK5OFkh|ryP NUnXO3hqW0GQR1XS
ML-2 Mk\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTN5Lk[3NVIh|ryP NFnaWW5USU6JRWK=
RS4-11 NWiyUYJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTN5LkewOlkh|ryP M{PRS3NCVkeHUh?=
MONO-MAC-6 NFrPeXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTN6LkK0O|ch|ryP NGrSWVBUSU6JRWK=
NCI-H345 Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jiZmlEPTB;M{iuPVExPiEQvF2= NFj3eGFUSU6JRWK=
NTERA-S-cl-D1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlyyTWM2OD1|OT61PFQzKM7:TR?= MlnKV2FPT0WU
NCI-H1882 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTRyLkW5PVgh|ryP M2jpcnNCVkeHUh?=
LC-1F MnjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPU[nZKSzVyPUSxMlU4ODVizszN NWDseFVsW0GQR1XS
HT M2j1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPDWZpKSzVyPUSyMlAxOjhizszN NXzROYJ3W0GQR1XS
MLMA NGP0ZVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTR{LkK3PFch|ryP M4PoWHNCVkeHUh?=
DG-75 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLNWnlzUUN3ME20Nk43PTR4IN88US=> MYrTRW5ITVJ?
GI-ME-N NYrRXVNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF70bGtKSzVyPUSyMlY3PzFizszN NXvVc|dXW0GQR1XS
MS-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rjdGlEPTB;NEKuPFk{KM7:TR?= MYDTRW5ITVJ?
CGTH-W-1 M4fn[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTGN2d[UUN3ME20OE46Pjl5IN88US=> MlzMV2FPT0WU
NCI-H209 M3jyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjwNmZzUUN3ME20Ok4xOTF3IN88US=> MYrTRW5ITVJ?
LB2518-MEL NEO2T|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvrUFNKSzVyPUS3MlA1PDhizszN M{jWfnNCVkeHUh?=
DU-4475 NX:zXoIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTR6LkS5N|ch|ryP MmrMV2FPT0WU
LB2241-RCC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHqWIFKSzVyPUS4MlYzODJizszN NWe0NmtlW0GQR1XS
LB771-HNC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnTTWM2OD12OD65NlEzKM7:TR?= NXXLPI1IW0GQR1XS

... 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)
Water Insoluble
Ethanol '6 mg/mL
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 CYC202
Smiles CCC(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)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 ()
% 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID