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 53 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 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTjTYF1UUN3ME21Mlc3OTF4IN88US=> MmLDV2FPT0WU
MRK-nu-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvRPHJKSzVyPUeuNVI6PjlizszN NYTIT3VQW0GQR1XS
NCCIT NXXpWIE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL1TWM2OD15LkW1OFgzKM7:TR?= M4ezXXNCVkeHUh?=
JiyoyeP-2003 MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDib3plUUN3ME24MlUxOjZ2IN88US=> M3n1cXNCVkeHUh?=
KS-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\yOWZVUUN3ME25MlQ2Pzh3IN88US=> NHLN[21USU6JRWK=
Becker Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PJW2lEPTB;OT60OlA5OiEQvF2= MYrTRW5ITVJ?
KARPAS-422 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTlwOU[zN|Yh|ryP M1rvNnNCVkeHUh?=
BB65-RCC NVX2cWZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTlwOUe0PVUh|ryP NILEVINUSU6JRWK=
SK-UT-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\KZ2lEPTB;MUCuN|Uh|ryP NWKyemV7W0GQR1XS
ST486 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTFyLkO1NUDPxE1? NUfoSWR[W0GQR1XS
LB831-BLC NYLNWXRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF74e3NKSzVyPUGxMlU3OjRizszN NWq0c3B1W0GQR1XS
COR-L279 MmH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjQVmlKSzVyPUGyMlI6ODdizszN MXjTRW5ITVJ?
NB1 NFfPUW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXR[HhHUUN3ME2xNk4{OzB6IN88US=> MoTXV2FPT0WU
D-247MG Mn;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7xXo1bUUN3ME2xNk4{PTF4IN88US=> NW\UR|V1W0GQR1XS
697 M4r6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zhV2lEPTB;MUKuOlAxPyEQvF2= MVXTRW5ITVJ?
GCIY NEe3PJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTiWmNHUUN3ME2xNk45PjF|IN88US=> MmXtV2FPT0WU
RPMI-8402 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rGPGlEPTB;MUOuOlI3OiEQvF2= NF3IWINUSU6JRWK=
Raji Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPWTWM2OD1zMz63PFk1KM7:TR?= MniwV2FPT0WU
MEG-01 M2HrfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TEU2lEPTB;MUOuPFM4QSEQvF2= MmHlV2FPT0WU
RPMI-6666 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33FbWlEPTB;MUOuPVEzOSEQvF2= NFX6dWxUSU6JRWK=
SCC-3 MmTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTxTWM2OD1zND6yPVU3KM7:TR?= NWf4SHBUW0GQR1XS
HCC1599 NX[zU|lUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nsOGlEPTB;MUSuOVk4PSEQvF2= NEjGZ|RUSU6JRWK=
OCI-AML2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTF3Lk[0PFIh|ryP MUHTRW5ITVJ?
OS-RC-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFu5cFZKSzVyPUG1Mlg{QDJizszN MV3TRW5ITVJ?
NCI-H1304 Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rvTGlEPTB;MU[uN|YxOSEQvF2= NEmwUmtUSU6JRWK=
HD-MY-Z NFWzVVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jEV2lEPTB;MU[uPFI1PiEQvF2= M3jUeXNCVkeHUh?=
JAR M3;YS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzOTWM2OD1zNz6wNVUzKM7:TR?= MnXNV2FPT0WU
TGW MmHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDNb3NrUUN3ME2xO{45OTJ2IN88US=> NGjWXohUSU6JRWK=
BC-3 Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYn1So5PUUN3ME2xPE4xOzB3IN88US=> M1SzOHNCVkeHUh?=
A101D NF7kVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\sOWlEPTB;MUiuN|IxQCEQvF2= NXnZVmxrW0GQR1XS
COLO-320-HSR MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\RTWM2OD1zOD63Olg5KM7:TR?= NEnIW4dUSU6JRWK=
LC4-1 NVv6UZZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDpTWM2OD1zOD64O|M1KM7:TR?= M1LZNXNCVkeHUh?=
BC-1 NEjzXZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zuXmlEPTB;MUmuNVE6QCEQvF2= NYDmbY1nW0GQR1XS
MHH-PREB-1 NWnQSGo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NImyO|ZKSzVyPUKwMlA{PTZizszN M4XibHNCVkeHUh?=
BL-70 NUi4[IluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzxdpdiUUN3ME2yNE4{Ojd2IN88US=> NGHKSZhUSU6JRWK=
CESS M3rmbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXlfpNKSzVyPUKwMlg2PDlizszN MY\TRW5ITVJ?
ES8 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3KXW1KSzVyPUKxMlA3KM7:TR?= NILVZVBUSU6JRWK=
NOMO-1 MlHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJzLkKwNFgh|ryP NUjnd3JQW0GQR1XS
ACN NVrOeJVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fGSWlEPTB;MkGuN|M5QSEQvF2= M3fwXXNCVkeHUh?=
EB-3 MnHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELuZnJKSzVyPUKzMlE5OzFizszN MmnkV2FPT0WU
LS-513 NFTsSmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJ|LkWxO|kh|ryP NHG2R3pUSU6JRWK=
HH MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorUTWM2OD1{ND6zPFE6KM7:TR?= NIDSbnpUSU6JRWK=
IST-SL2 NHfXeWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfCW|RKSzVyPUK0MlU{PDNizszN MkjrV2FPT0WU
HOP-62 NFr5OWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi0ZYd7UUN3ME2yOU41PDJ3IN88US=> NGnXSJJUSU6JRWK=
NCI-H2126 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfYV3NFUUN3ME2yOU43PTJ7IN88US=> NXTHR45jW0GQR1XS
BL-41 NHq5VZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfRe29KSzVyPUK1Mlk2QTdizszN NITw[VFUSU6JRWK=
KURAMOCHI NVXsd|VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLDRXZKSzVyPUK2MlgxQDJizszN NUHTTplKW0GQR1XS
KARPAS-299 NVviNXpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4n2[2lEPTB;Mk[uPFY1PiEQvF2= M{TyZnNCVkeHUh?=
QIMR-WIL M4[0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzzTWM2OD1{Nz65NVQ1KM7:TR?= NHrRUmZUSU6JRWK=
HL-60 NYDQTGcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H2ZmlEPTB;MkeuPVg3QSEQvF2= M1e2N3NCVkeHUh?=
TE-9 NIrzV2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjBTWM2OD1{OD63PVY6KM7:TR?= NH23dVFUSU6JRWK=
TE-8 MmLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXwTWM2OD1{OD65NFgh|ryP M4C3fHNCVkeHUh?=
NOS-1 M4HTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DZUWlEPTB;MkiuPVc{OyEQvF2= NULoW3FjW0GQR1XS
GI-1 NYjwVnl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDVR5BKSzVyPUK5MlAyOTNizszN MoDYV2FPT0WU
KM12 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ7Lk[yN|kh|ryP M3HFbHNCVkeHUh?=
BB30-HNC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfnRZRKSzVyPUK5Mlk1QDNizszN NW\nXJJ6W0GQR1XS
ES3 NWPFN4R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfITWM2OD1{OT65OVgzKM7:TR?= M{TVeHNCVkeHUh?=
NCI-H510A MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjXTWM2OD1|MD6wN|I6KM7:TR?= NX;4Xmc2W0GQR1XS
NCI-H82 MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHJe|RKSzVyPUOxMlAyOzVizszN NFTC[Y9USU6JRWK=
NCI-SNU-1 MnHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTCTWM2OD1|MT6xNFU6KM7:TR?= NHjzfFhUSU6JRWK=
NKM-1 NVrtUldPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXEWFBxUUN3ME2zNU4yOzl5IN88US=> M4TPNHNCVkeHUh?=
SIG-M5 M3X4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPKTWM2OD1|MT62PFM{KM7:TR?= NWO0co9UW0GQR1XS
SK-N-FI NWLafXhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLRUpNKSzVyPUOxMlc2OzVizszN MmrrV2FPT0WU
LOUCY NF\TTXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTE[JlKSzVyPUOyMlEzPTNizszN NILIZXpUSU6JRWK=
Calu-6 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzReoxjUUN3ME2zNk41PzR3IN88US=> Mn3QV2FPT0WU
GOTO NGrUdHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIH3VYNKSzVyPUOyMlkyOjlizszN NV;sN5VUW0GQR1XS
NCI-H526 NHfHOWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTN|LkS5N|Yh|ryP NX3rN5R[W0GQR1XS
RKO M13oTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUm0PW1jUUN3ME2zN{42QTZ7IN88US=> NGP0c|BUSU6JRWK=
NCI-H64 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TXUmlEPTB;M{OuPFU6PyEQvF2= NXnQOIl[W0GQR1XS
LP-1 NH7L[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3sUIFKSzVyPUOzMlg6ODhizszN MmDEV2FPT0WU
KGN NUS1dmtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnWd|dMUUN3ME2zOE4zPTJ2IN88US=> Ml3GV2FPT0WU
NCI-H2141 NIL2dm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Hq[mlEPTB;M{SuOlU{OyEQvF2= NVXiOHhXW0GQR1XS
TE-10 NXqyVHIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nKfGlEPTB;M{SuPVQzOiEQvF2= Mle1V2FPT0WU
K5 NWftPIJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M12xXmlEPTB;M{WuNFg3OSEQvF2= NX;Mc2ZlW0GQR1XS
IMR-5 M{X4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnu1TWM2OD1|NT6zNVM6KM7:TR?= MlX2V2FPT0WU
TE-441-T NWm1dpV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTN4LkGxOFgh|ryP NWXPVlJXW0GQR1XS
TE-6 NF;zNHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK2OZFYUUN3ME2zOk4{OjR4IN88US=> M1nwdXNCVkeHUh?=
MOLT-4 NEHndm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVm5dJk5UUN3ME2zOk4{Ojd4IN88US=> NHXmVnhUSU6JRWK=
COLO-684 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C2XWlEPTB;M{euNFEzKM7:TR?= MXLTRW5ITVJ?
LU-139 NVTlbmRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLMW25xUUN3ME2zO{4yQDV4IN88US=> MmjnV2FPT0WU
OPM-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTN5LkK5OFkh|ryP M1v6SXNCVkeHUh?=
ML-2 M4jUNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\sV4ZKSzVyPUO3MlY4OTJizszN NFXUcm9USU6JRWK=
RS4-11 NYL5WYhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\WO2lEPTB;M{euO|A3QSEQvF2= MXPTRW5ITVJ?
MONO-MAC-6 NEWyNXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vGOmlEPTB;M{iuNlQ4PyEQvF2= M1jQeHNCVkeHUh?=
NCI-H345 NXraNZFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXzfFd1UUN3ME2zPE46OTB4IN88US=> NXT3UWh6W0GQR1XS
NTERA-S-cl-D1 M1TyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fDR2lEPTB;M{muOVg1OiEQvF2= NXrUcmxuW0GQR1XS
NCI-H1882 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HFe2lEPTB;NECuOVk6QCEQvF2= MYrTRW5ITVJ?
LC-1F NULWSVhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnWTWM2OD12MT61O|A2KM7:TR?= MkTxV2FPT0WU
HT Mlf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGyTWM2OD12Mj6wNFI5KM7:TR?= M4DYdXNCVkeHUh?=
MLMA NHj4RXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\nSGlEPTB;NEKuNlc5PyEQvF2= M3zMW3NCVkeHUh?=
DG-75 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm5b5JYUUN3ME20Nk43PTR4IN88US=> NXXrXFBtW0GQR1XS
GI-ME-N NEnOcYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTR{Lk[2O|Eh|ryP M4nscnNCVkeHUh?=
MS-1 NHfpVHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTR{Lki5N{DPxE1? MV\TRW5ITVJ?
CGTH-W-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknLTWM2OD12ND65Olk4KM7:TR?= MVXTRW5ITVJ?
NCI-H209 NEjkdHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLrTWM2OD12Nj6wNVE2KM7:TR?= M2P1SnNCVkeHUh?=
LB2518-MEL Mn;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTR5LkC0OFgh|ryP Mm\GV2FPT0WU
DU-4475 NUKyb|RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTR6LkS5N|ch|ryP M{HzUXNCVkeHUh?=
LB2241-RCC NV3zPWNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X1[mlEPTB;NEiuOlIxOiEQvF2= Ml\nV2FPT0WU
LB771-HNC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPmSFRKSzVyPUS4MlkzOTJizszN NVHOVFVxW0GQR1XS

... 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