Roscovitine (Seliciclib,CYC202)

For research use only.

Catalog No.S1153

66 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 191 In stock
USD 147 In stock
USD 257 In stock
USD 470 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Roscovitine (Seliciclib,CYC202) has been cited by 66 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 NFS5WlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPDTWM2OD13Lke2NVE3KM7:TR?= NV;MfXZTW0GQR1XS
MRK-nu-1 NXvqdFNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHkd4I{UUN3ME23MlEzQTZ7IN88US=> M2DFXXNCVkeHUh?=
NCCIT M1uyOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfGTWM2OD15LkW1OFgzKM7:TR?= MojZV2FPT0WU
JiyoyeP-2003 Mn;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\WTWM2OD16LkWwNlY1KM7:TR?= Mlu0V2FPT0WU
KS-1 MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vHRmlEPTB;OT60OVc5PSEQvF2= M{DJb3NCVkeHUh?=
Becker MnXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrNTWM2OD17LkS2NFgzKM7:TR?= M33YZ3NCVkeHUh?=
KARPAS-422 MmTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTlwOU[zN|Yh|ryP M4PxenNCVkeHUh?=
BB65-RCC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v6b2lEPTB;OT65O|Q6PSEQvF2= M1LLXXNCVkeHUh?=
SK-UT-1 MkXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTFyLkO1JO69VQ>? MmD0V2FPT0WU
ST486 MoPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXWTFhVUUN3ME2xNE4{PTFizszN M1fGSnNCVkeHUh?=
LB831-BLC NG[1NpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;mTWM2OD1zMT61OlI1KM7:TR?= M37DXHNCVkeHUh?=
COR-L279 NEDabYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;MUmlEPTB;MUKuNlkxPyEQvF2= NFLoenNUSU6JRWK=
NB1 Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonhTWM2OD1zMj6zN|A5KM7:TR?= MmDNV2FPT0WU
D-247MG M1rsVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnMb5h[UUN3ME2xNk4{PTF4IN88US=> Mln0V2FPT0WU
697 M2HUbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWC1Vm9mUUN3ME2xNk43ODB5IN88US=> MoPDV2FPT0WU
GCIY NHzVT25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTF{Lki2NVMh|ryP MXLTRW5ITVJ?
RPMI-8402 NHfuVZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mly2TWM2OD1zMz62NlYzKM7:TR?= Mn[2V2FPT0WU
Raji MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[3TWM2OD1zMz63PFk1KM7:TR?= MVHTRW5ITVJ?
MEG-01 NVTrVolnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3WzTWlEPTB;MUOuPFM4QSEQvF2= M{TxN3NCVkeHUh?=
RPMI-6666 M3zNUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXmTWM2OD1zMz65NVIyKM7:TR?= M{fzfXNCVkeHUh?=
SCC-3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnQTWM2OD1zND6yPVU3KM7:TR?= M2DQR3NCVkeHUh?=
HCC1599 NVS5dIZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF2LkW5O|Uh|ryP MXrTRW5ITVJ?
OCI-AML2 M{X1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfkWW9KSzVyPUG1MlY1QDJizszN M4jiNXNCVkeHUh?=
OS-RC-2 NEntNW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NID5UZdKSzVyPUG1Mlg{QDJizszN MW\TRW5ITVJ?
NCI-H1304 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofMTWM2OD1zNj6zOlAyKM7:TR?= NGjyVGNUSU6JRWK=
HD-MY-Z MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XPTWlEPTB;MU[uPFI1PiEQvF2= MlzsV2FPT0WU
JAR MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;tSWlEPTB;MUeuNFE2OiEQvF2= NUjUbJBrW0GQR1XS
TGW MkjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXFTWM2OD1zNz64NVI1KM7:TR?= M2HU[3NCVkeHUh?=
BC-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7O[5hKSzVyPUG4MlA{ODVizszN NI\ibZNUSU6JRWK=
A101D NV;5bZA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnoVHNKSzVyPUG4MlMzODhizszN MlzsV2FPT0WU
COLO-320-HSR NXTPR4dUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnyxTWM2OD1zOD63Olg5KM7:TR?= M3vJd3NCVkeHUh?=
LC4-1 M3jPVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXpVXVRUUN3ME2xPE45PzN2IN88US=> M3zpUnNCVkeHUh?=
BC-1 NE\wfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF7LkGxPVgh|ryP MYXTRW5ITVJ?
MHH-PREB-1 M4fKNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTJyLkCzOVYh|ryP NXLXW4E4W0GQR1XS
BL-70 Mkj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XIWmlEPTB;MkCuN|I4PCEQvF2= NXHPZ3NyW0GQR1XS
CESS NX3a[pl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rDUWlEPTB;MkCuPFU1QSEQvF2= MmLTV2FPT0WU
ES8 NV;s[HRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDFRoVJUUN3ME2yNU4xPiEQvF2= MVPTRW5ITVJ?
NOMO-1 M1XJ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LzfmlEPTB;MkGuNlAxQCEQvF2= NHT4[YpUSU6JRWK=
ACN Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIS2O2ZKSzVyPUKxMlM{QDlizszN M3PGNnNCVkeHUh?=
EB-3 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjGbZRKSzVyPUKzMlE5OzFizszN NYraVnBRW0GQR1XS
LS-513 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPoTWM2OD1{Mz61NVc6KM7:TR?= NXiyS4JJW0GQR1XS
HH M17BPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJ2LkO4NVkh|ryP MkG2V2FPT0WU
IST-SL2 M2q4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLkTWM2OD1{ND61N|Q{KM7:TR?= NYL2S2h{W0GQR1XS
HOP-62 M4HNRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;C[mJKSzVyPUK1MlQ1OjVizszN MUnTRW5ITVJ?
NCI-H2126 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfLWnZYUUN3ME2yOU43PTJ7IN88US=> M4ewUHNCVkeHUh?=
BL-41 NX7We49bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL6VmFtUUN3ME2yOU46PTl5IN88US=> NUH3VY03W0GQR1XS
KURAMOCHI MmfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVi2e2x[UUN3ME2yOk45ODh{IN88US=> Ml;WV2FPT0WU
KARPAS-299 NVLxNIpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJ4Lki2OFYh|ryP NF;DO|ZUSU6JRWK=
QIMR-WIL M1HUSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX6zUI1zUUN3ME2yO{46OTR2IN88US=> NYjS[mdIW0GQR1XS
HL-60 M2nKR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJ5Lkm4Olkh|ryP MnP1V2FPT0WU
TE-9 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJ6Lke5Olkh|ryP NFfJeFFUSU6JRWK=
TE-8 NWjDRlJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr1TWM2OD1{OD65NFgh|ryP NVWwWmFzW0GQR1XS
NOS-1 NUS4TnJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3OPXJ1UUN3ME2yPE46PzN|IN88US=> NG\re4ZUSU6JRWK=
GI-1 NHzxWpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoroTWM2OD1{OT6wNVE{KM7:TR?= MU\TRW5ITVJ?
KM12 NF60XYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ7Lk[yN|kh|ryP M3rVWXNCVkeHUh?=
BB30-HNC M4HN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnQVllyUUN3ME2yPU46PDh|IN88US=> NYnIWIQ3W0GQR1XS
ES3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TBdGlEPTB;MkmuPVU5OiEQvF2= MXzTRW5ITVJ?
NCI-H510A M3r0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTp[plKSzVyPUOwMlA{OjlizszN NVfVVo5LW0GQR1XS
NCI-H82 NFnDXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVyxRZBIUUN3ME2zNU4xOTN3IN88US=> M2foW3NCVkeHUh?=
NCI-SNU-1 M2Hvc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoriTWM2OD1|MT6xNFU6KM7:TR?= NU\3cnhCW0GQR1XS
NKM-1 NYjte45IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LYWWlEPTB;M{GuNVM6PyEQvF2= M3TzbHNCVkeHUh?=
SIG-M5 NInRTYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7nTWM2OD1|MT62PFM{KM7:TR?= M4LLTXNCVkeHUh?=
SK-N-FI MonaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS3b5FKSzVyPUOxMlc2OzVizszN MVvTRW5ITVJ?
LOUCY Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjBTWM2OD1|Mj6xNlU{KM7:TR?= M{\SRnNCVkeHUh?=
Calu-6 NFfJcYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTN{LkS3OFUh|ryP M{\2T3NCVkeHUh?=
GOTO NV;XN4hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2THe2lEPTB;M{KuPVEzQSEQvF2= MVTTRW5ITVJ?
NCI-H526 M{\Td2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO3cXJOUUN3ME2zN{41QTN4IN88US=> MUjTRW5ITVJ?
RKO M3XhdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTN|LkW5Olkh|ryP MUHTRW5ITVJ?
NCI-H64 MljaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLa[lNKSzVyPUOzMlg2QTdizszN NFT6T5hUSU6JRWK=
LP-1 NGPab4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jW[WlEPTB;M{OuPFkxQCEQvF2= M3rmbHNCVkeHUh?=
KGN MkPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrXSlRKSzVyPUO0MlI2OjRizszN MXLTRW5ITVJ?
NCI-H2141 NVnQUZJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLEOZRnUUN3ME2zOE43PTN|IN88US=> MoroV2FPT0WU
TE-10 NUOwfphCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnq1TWM2OD1|ND65OFIzKM7:TR?= NYD4TpRtW0GQR1XS
K5 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ntNWlEPTB;M{WuNFg3OSEQvF2= NWe0NWhwW0GQR1XS
IMR-5 MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\K[GlEPTB;M{WuN|E{QSEQvF2= NX3vNolSW0GQR1XS
TE-441-T MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7rOYR2UUN3ME2zOk4yOTR6IN88US=> NXzGe2g2W0GQR1XS
TE-6 MlPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHRTWM2OD1|Nj6zNlQ3KM7:TR?= NHzBXmhUSU6JRWK=
MOLT-4 NXu3S2QzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnRd2Y5UUN3ME2zOk4{Ojd4IN88US=> M3TFPXNCVkeHUh?=
COLO-684 NV3zTYhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXsbFRKSzVyPUO3MlAyOiEQvF2= NGXF[4xUSU6JRWK=
LU-139 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTN5LkG4OVYh|ryP NIO1U4VUSU6JRWK=
OPM-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjJSVRKSzVyPUO3MlI6PDlizszN MUXTRW5ITVJ?
ML-2 NF\1Tm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTN5Lk[3NVIh|ryP M1jic3NCVkeHUh?=
RS4-11 NUW4Z2FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzne4w2UUN3ME2zO{44ODZ7IN88US=> NYDPcIFlW0GQR1XS
MONO-MAC-6 NVOzNoFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3OwTmlEPTB;M{iuNlQ4PyEQvF2= Mn3OV2FPT0WU
NCI-H345 NVLHcYdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33HSWlEPTB;M{iuPVExPiEQvF2= Mo\MV2FPT0WU
NTERA-S-cl-D1 NFvuXoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XaSGlEPTB;M{muOVg1OiEQvF2= NHTWW3VUSU6JRWK=
NCI-H1882 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTRyLkW5PVgh|ryP NVviXoZJW0GQR1XS
LC-1F MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTRzLkW3NFUh|ryP NGfycYdUSU6JRWK=
HT NF;jTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\GTWM2OD12Mj6wNFI5KM7:TR?= NG\pbVFUSU6JRWK=
MLMA M3HJOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDXTWM2OD12Mj6yO|g4KM7:TR?= NED6ToJUSU6JRWK=
DG-75 NH3wUndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzyTWM2OD12Mj62OVQ3KM7:TR?= NWL6eIo6W0GQR1XS
GI-ME-N NYHPbHYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnvVlZKSzVyPUSyMlY3PzFizszN MYPTRW5ITVJ?
MS-1 Mnv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHITWM2OD12Mj64PVMh|ryP MWrTRW5ITVJ?
CGTH-W-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm0NFZKSzVyPUS0Mlk3QTdizszN NGfrVopUSU6JRWK=
NCI-H209 MoH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHMVFFKSzVyPUS2MlAyOTVizszN NXzJVIdzW0GQR1XS
LB2518-MEL NFyzV|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTR5LkC0OFgh|ryP MYHTRW5ITVJ?
DU-4475 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTR6LkS5N|ch|ryP M2PxVnNCVkeHUh?=
LB2241-RCC MljhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYW2eYh[UUN3ME20PE43OjB{IN88US=> MlrZV2FPT0WU
LB771-HNC NWTVfXpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTR6LkmyNVIh|ryP M1Ljc3NCVkeHUh?=

... 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]
- Collapse
  • 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]
- Collapse
  • 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)
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

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
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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

CDK Inhibitors with Unique Features

Related CDK Products

Tags: buy Roscovitine|Roscovitine ic50|Roscovitine price|Roscovitine cost|Roscovitine solubility dmso|Roscovitine purchase|Roscovitine manufacturer|Roscovitine research buy|Roscovitine order|Roscovitine mouse|Roscovitine chemical structure|Roscovitine mw|Roscovitine molecular weight|Roscovitine datasheet|Roscovitine supplier|Roscovitine in vitro|Roscovitine cell line|Roscovitine concentration|Roscovitine nmr|Roscovitine in vivo|Roscovitine clinical trial|Roscovitine inhibitor|Roscovitine Cell Cycle inhibitor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID