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 20 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 MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:ycplKSzVyPUWuO|YyOTZizszN M4XYT3NCVkeHUh?=
MRK-nu-1 M2HD[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrkTWM2OD15LkGyPVY6KM7:TR?= NXyzN|dZW0GQR1XS
NCCIT NUniXmQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTdwNUW0PFIh|ryP NES0blNUSU6JRWK=
JiyoyeP-2003 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRThwNUCyOlQh|ryP NV\0OXgyW0GQR1XS
KS-1 M1W4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTlwNEW3PFUh|ryP NFW0d5BUSU6JRWK=
Becker M3i3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXETWM2OD17LkS2NFgzKM7:TR?= M2fPSHNCVkeHUh?=
KARPAS-422 NE[ydWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HicGlEPTB;OT65OlM{PiEQvF2= MUHTRW5ITVJ?
BB65-RCC NWXzc5RTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fvUGlEPTB;OT65O|Q6PSEQvF2= Ml\6V2FPT0WU
SK-UT-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HXdGlEPTB;MUCuN|Uh|ryP NX7IVlA1W0GQR1XS
ST486 MkjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\VR2lEPTB;MUCuN|UyKM7:TR?= NV\ndGtiW0GQR1XS
LB831-BLC NImzVFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTFzLkW2NlQh|ryP NYexW4hTW0GQR1XS
COR-L279 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkX5TWM2OD1zMj6yPVA4KM7:TR?= MYHTRW5ITVJ?
NB1 Mn\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmmzTWM2OD1zMj6zN|A5KM7:TR?= MWfTRW5ITVJ?
D-247MG NGjiNY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TYUWlEPTB;MUKuN|UyPiEQvF2= M{LUeXNCVkeHUh?=
697 NGThdG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLSTFNKSzVyPUGyMlYxODdizszN MYjTRW5ITVJ?
GCIY NV[zSHBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n3RWlEPTB;MUKuPFYyOyEQvF2= NHvabplUSU6JRWK=
RPMI-8402 MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PNUWlEPTB;MUOuOlI3OiEQvF2= MVXTRW5ITVJ?
Raji NUKxWmZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHYNYRKSzVyPUGzMlc5QTRizszN M4PjR3NCVkeHUh?=
MEG-01 M3rDVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF|LkizO|kh|ryP Mm[zV2FPT0WU
RPMI-6666 M33Sd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF|LkmxNlEh|ryP MYXTRW5ITVJ?
SCC-3 M1PHbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF2LkK5OVYh|ryP MYHTRW5ITVJ?
HCC1599 NUXJUlRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrwTWM2OD1zND61PVc2KM7:TR?= Ml;EV2FPT0WU
OCI-AML2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH63WpZKSzVyPUG1MlY1QDJizszN MYLTRW5ITVJ?
OS-RC-2 NGK4N|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi1e|d{UUN3ME2xOU45Ozh{IN88US=> NX3IVHg2W0GQR1XS
NCI-H1304 NVLTOlN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjsTWM2OD1zNj6zOlAyKM7:TR?= Mn;LV2FPT0WU
HD-MY-Z MoHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF4LkiyOFYh|ryP MkfmV2FPT0WU
JAR MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGwZ3NjUUN3ME2xO{4xOTV{IN88US=> MVPTRW5ITVJ?
TGW MnXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF5LkixNlQh|ryP MoDRV2FPT0WU
BC-3 M4\XXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF6LkCzNFUh|ryP MnnJV2FPT0WU
A101D MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXPZlRXUUN3ME2xPE4{OjB6IN88US=> MVnTRW5ITVJ?
COLO-320-HSR NFTLXHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nvXmlEPTB;MUiuO|Y5QCEQvF2= M3P1U3NCVkeHUh?=
LC4-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTDTWM2OD1zOD64O|M1KM7:TR?= NY\pW3JzW0GQR1XS
BC-1 MkfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLibYVVUUN3ME2xPU4yOTl6IN88US=> NYj0dnhyW0GQR1XS
MHH-PREB-1 NGO1d|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJyLkCzOVYh|ryP M4\BVnNCVkeHUh?=
BL-70 NEH6fVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDGZVJFUUN3ME2yNE4{Ojd2IN88US=> NXWxNm1EW0GQR1XS
CESS MlGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe3OHh5UUN3ME2yNE45PTR7IN88US=> M162e3NCVkeHUh?=
ES8 MkjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJzLkC2JO69VQ>? M3;tPHNCVkeHUh?=
NOMO-1 MomwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJzLkKwNFgh|ryP NIXHUohUSU6JRWK=
ACN NYXnTldXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEexNXBKSzVyPUKxMlM{QDlizszN NX3mNXNUW0GQR1XS
EB-3 MkTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfITWM2OD1{Mz6xPFMyKM7:TR?= M2jOV3NCVkeHUh?=
LS-513 NXPCc491T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfTTWM2OD1{Mz61NVc6KM7:TR?= NUX3eVVZW0GQR1XS
HH NXH6bY9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v2dWlEPTB;MkSuN|gyQSEQvF2= M2K3XnNCVkeHUh?=
IST-SL2 MlXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ2LkWzOFMh|ryP MmXuV2FPT0WU
HOP-62 MlLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjxV|NKSzVyPUK1MlQ1OjVizszN NHfkXXVUSU6JRWK=
NCI-H2126 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC1ZoVKSzVyPUK1MlY2OjlizszN NXrsSHg4W0GQR1XS
BL-41 MlfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfaZZdkUUN3ME2yOU46PTl5IN88US=> NE\ZfJFUSU6JRWK=
KURAMOCHI NFm1N2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDGfXRKSzVyPUK2MlgxQDJizszN M3zuSHNCVkeHUh?=
KARPAS-299 MmXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4The2lEPTB;Mk[uPFY1PiEQvF2= MYPTRW5ITVJ?
QIMR-WIL M{S5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M32wRWlEPTB;MkeuPVE1PCEQvF2= MWnTRW5ITVJ?
HL-60 NH\Le5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;vbWlEPTB;MkeuPVg3QSEQvF2= Ml3BV2FPT0WU
TE-9 MlfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDkVnNKSzVyPUK4Mlc6PjlizszN NVX0eo1UW0GQR1XS
TE-8 MmrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJ6LkmwPEDPxE1? NIm4cm9USU6JRWK=
NOS-1 M2mzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PZTmlEPTB;MkiuPVc{OyEQvF2= MomyV2FPT0WU
GI-1 NHTFN|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWThVVQ4UUN3ME2yPU4xOTF|IN88US=> MVXTRW5ITVJ?
KM12 NHvzdlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LmeWlEPTB;MkmuOlI{QSEQvF2= M2fzOXNCVkeHUh?=
BB30-HNC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVy0Ro97UUN3ME2yPU46PDh|IN88US=> NX7DTGFxW0GQR1XS
ES3 NWjMcIFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzMTWM2OD1{OT65OVgzKM7:TR?= MXTTRW5ITVJ?
NCI-H510A M4PNfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jwOGlEPTB;M{CuNFMzQSEQvF2= NYPNOmtYW0GQR1XS
NCI-H82 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkn3TWM2OD1|MT6wNVM2KM7:TR?= NVTl[WdYW0GQR1XS
NCI-SNU-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\nOXpkUUN3ME2zNU4yODV7IN88US=> NYLHNlRFW0GQR1XS
NKM-1 M4OyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTNzLkGzPVch|ryP MnzmV2FPT0WU
SIG-M5 MlfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfvTWM2OD1|MT62PFM{KM7:TR?= NWTPSItOW0GQR1XS
SK-N-FI M{HUe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXCTWM2OD1|MT63OVM2KM7:TR?= NIHsSFJUSU6JRWK=
LOUCY MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnTfZlCUUN3ME2zNk4yOjV|IN88US=> MnnaV2FPT0WU
Calu-6 NWDlbHd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;BWHI2UUN3ME2zNk41PzR3IN88US=> MnLCV2FPT0WU
GOTO M3nVNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTldGxKSzVyPUOyMlkyOjlizszN M4rMb3NCVkeHUh?=
NCI-H526 MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7IWWtKSzVyPUOzMlQ6OzZizszN MWnTRW5ITVJ?
RKO M3nTZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfCOmNKSzVyPUOzMlU6PjlizszN MlvWV2FPT0WU
NCI-H64 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTLTWM2OD1|Mz64OVk4KM7:TR?= M3LoT3NCVkeHUh?=
LP-1 M3LVOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTN|Lki5NFgh|ryP NE\J[HFUSU6JRWK=
KGN NHvQT4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTN2LkK1NlQh|ryP Mm\QV2FPT0WU
NCI-H2141 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfSZ4ZKSzVyPUO0MlY2OzNizszN NGTYOHhUSU6JRWK=
TE-10 MkXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHSO3NKSzVyPUO0Mlk1OjJizszN MXLTRW5ITVJ?
K5 M2G4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TZXmlEPTB;M{WuNFg3OSEQvF2= MmrKV2FPT0WU
IMR-5 MnnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X5[GlEPTB;M{WuN|E{QSEQvF2= M{fs[3NCVkeHUh?=
TE-441-T M1jnOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHGVnJKSzVyPUO2MlEyPDhizszN NF\XcoFUSU6JRWK=
TE-6 M2jOWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrZ[pVKSzVyPUO2MlMzPDZizszN NVzJ[I1QW0GQR1XS
MOLT-4 NUPHfJg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTN4LkOyO|Yh|ryP M{LoXHNCVkeHUh?=
COLO-684 NUWwdpNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\pUZVKSzVyPUO3MlAyOiEQvF2= MYXTRW5ITVJ?
LU-139 M1\KUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLxcW5KSzVyPUO3MlE5PTZizszN NGC2[pFUSU6JRWK=
OPM-2 NIHHNnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvoR4NSUUN3ME2zO{4zQTR7IN88US=> NYjBeZNwW0GQR1XS
ML-2 M3\2TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKzTWM2OD1|Nz62O|EzKM7:TR?= Mn[4V2FPT0WU
RS4-11 MkjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jkWmlEPTB;M{euO|A3QSEQvF2= M{HSTnNCVkeHUh?=
MONO-MAC-6 NF:3VHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\4TWM2OD1|OD6yOFc4KM7:TR?= NVfyR2xvW0GQR1XS
NCI-H345 NIqySHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\5XmlEPTB;M{iuPVExPiEQvF2= NWrwcHJWW0GQR1XS
NTERA-S-cl-D1 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXBTWM2OD1|OT61PFQzKM7:TR?= NV6xZ|hYW0GQR1XS
NCI-H1882 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTRyLkW5PVgh|ryP MV\TRW5ITVJ?
LC-1F NWHD[|ZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXiWmtKSzVyPUSxMlU4ODVizszN Mo\wV2FPT0WU
HT MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTR{LkCwNlgh|ryP NIfMdHVUSU6JRWK=
MLMA MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\UOJNKSzVyPUSyMlI4QDdizszN MVPTRW5ITVJ?
DG-75 M1;5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjofpdKUUN3ME20Nk43PTR4IN88US=> Mn:yV2FPT0WU
GI-ME-N M{LBW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLoWXNKSzVyPUSyMlY3PzFizszN MWHTRW5ITVJ?
MS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TBdGlEPTB;NEKuPFk{KM7:TR?= NIriN2lUSU6JRWK=
CGTH-W-1 NVTufJk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjnNowzUUN3ME20OE46Pjl5IN88US=> MkPIV2FPT0WU
NCI-H209 NWTEOG9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTrNHNtUUN3ME20Ok4xOTF3IN88US=> NYjCcGxrW0GQR1XS
LB2518-MEL NUi3fnlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rGcWlEPTB;NEeuNFQ1QCEQvF2= NEfkSJpUSU6JRWK=
DU-4475 NWfS[WM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTR6LkS5N|ch|ryP M{LrSnNCVkeHUh?=
LB2241-RCC MlnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPTTWM2OD12OD62NlAzKM7:TR?= NULObnBPW0GQR1XS
LB771-HNC MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDSTWM2OD12OD65NlEzKM7:TR?= MWnTRW5ITVJ?

... Click to View More Cell Line Experimental Data

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]
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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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03774446 Recruiting Cushing Disease Cedars-Sinai Medical Center November 2 2018 Phase 2
NCT03774446 Recruiting Cushing Disease Cedars-Sinai Medical Center November 2 2018 Phase 2
NCT02649751 Terminated Cystic Fibrosis University Hospital Brest|ManRos Therapeutics|Cyclacel Pharmaceuticals Inc. February 22 2016 Phase 2
NCT02649751 Terminated Cystic Fibrosis University Hospital Brest|ManRos Therapeutics|Cyclacel Pharmaceuticals Inc. February 22 2016 Phase 2
NCT02160730 Terminated Cushings Disease Shlomo Melmed MD|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Cedars-Sinai Medical Center May 2014 Phase 2
NCT02160730 Terminated Cushings Disease Shlomo Melmed MD|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Cedars-Sinai Medical Center May 2014 Phase 2

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.

CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID