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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  • In vitro inhibition of mouse corticotroph tumor cells by R-roscovitine. (A) Treatment of ACTH-secreting AtT20 cells with R-roscovitine (1-2 × 10-5 μM) led to decreased number of viable cells at 24 and 48 h, as depicted by Wst-1 proliferation assay (mean ± SE; **P < 0.01). (B) Western blot of protein extracts derived from AtT20 cells treated with vehicle or R-roscovitine. (C) R-roscovitine treatment (10 μM) for 48 h induced senescence as indicated by increased β-gal expression. (D) ACTH concentration by radioimmunoassays of culture medium from AtT20 cells treated with vehicle or R-roscovitine (mean ±SE; **P < 0.01 and ***P < 0.001). (E) Western blot of protein extracts derived from AtT20 cells treated with R-roscovitine. Vehicle is 0.2% DMSO.

    PNAS 2011 108, 8417. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

    In vivo action of R-roscovitine inmouse corticotroph adenomas. Athymic nude mice were s.c. inoculated with corticotroph tumor AtT20 cells (1 × 105 cells). Three days after injection, mice were randomized to receive Rroscovitine (150 mg/kg) or vehicle by oral gavage twice daily, 5 d/wk. After 3 wk, tumor xenografts were dissected and (A) tumor volumes were decreased in R-roscovitine-treated animals. (B) Western blot of representative tumor specimens showed decreased ACTH and PCNA expression in R-roscovitine-treated tumors. (C) R-roscovitine-treated corticotroph tumors exhibited decreased PCNA and ACTH coexpressing cells. Fluorescence microscopy image of immunohistochemistry detecting PCNA (red) and ACTH (green) expression in control (a-c) and R-roscovitine-treated tumors (d-f). Cryosection slides were counterstained with DAPI (blue). (D) Blood was collected from each animal for measurement of plasma ACTH and serum corticosterone levels (mean ±SE; n = 13-14 mice for each group; **P < 0.01).

    PNAS 2011 108, 8417. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

  • (a-c) Relative viability of Cis-R cells and parental MDA-MB-231 (Cis-S) cells in the presence of cisplatin (10 μM) and the increasing concentrations of WEE1i (a), ATRi (b) and CHK1i (c). (d) Illustration of the experimental setup, with incorporation of IdU and CldU shown in red and green, respectively. (e) As shown in (d), MDA-MB-231 cells were incubated with IdU for 10 min as indicated, followed by cisplatin treatment for 3 hours, with or without indicated inhibitor(s) (top) for indicated total 40 min and CIdU was applied for 10 min. Cells were fixed and stained with IdU and CIdU antibodies. Nuclear DNA was counterstained by DAPI. (f) Quantification of indicated part of three separate experiments as in (e) represented as the mean ± SEM. CDKi:Roscovitine.

    Sci Rep, 2017, 7:43517. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

    Inhibition of CDK5 by roscovitine resulted in defective neuronal migration, which was rescued by expression of GFP-Ndel1 (S251E). a, Granular neurons were treated with roscovitine. Western blotting was performed 24 h after start of culture. Aurora-A and NDEL1 displayed similar expression levels with untreated neurons, whereas the levels of phosphorylated Aurora-A and NDEL1 proteins were decreased after treatment with roscovitine. Relative intensities of the bands of Western blotting are shown at the bottom.

    J Hematol Oncol 2012 7, 53. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

  •  

    Chronic treatment with roscovitine attenuates the development of atherosclerosis in ApoE-/- mice. Vehicle, roscovitine or resveratrol were daily administered to ApoE-/- mice under high fat high cholesterol diet, from the age of four weeks old. After 18 weeks of treatment, Oil-Red-O (A) and SA-β-gal (B) staining was performed using aortae collected from all groups of mice.Chronic treatment with roscovitine attenuates the development of atherosclerosis in ApoE-/- mice. Vehicle, roscovitine or resveratrol were daily administered to ApoE-/- mice under high fat high cholesterol diet, from the age of four weeks old. After 18 weeks of treatment, Oil-Red-O (A) and SA-β-gal (B) staining was performed using aortae collected from all groups of mice.

    University of Hong Kong. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

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 MmLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7ETWM2OD13Lke2NVE3KM7:TR?= NYLNUYV5W0GQR1XS
MRK-nu-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXaS|d5UUN3ME23MlEzQTZ7IN88US=> MV;TRW5ITVJ?
NCCIT NVfNToljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofvTWM2OD15LkW1OFgzKM7:TR?= Mm\NV2FPT0WU
JiyoyeP-2003 NH;LSGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfzOVlKSzVyPUiuOVAzPjRizszN MVzTRW5ITVJ?
KS-1 MnmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTlwNEW3PFUh|ryP M3jCWHNCVkeHUh?=
Becker NW\Qc2RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTlwNE[wPFIh|ryP NEnsTWxUSU6JRWK=
KARPAS-422 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPMTpRnUUN3ME25Mlk3OzN4IN88US=> NVHHXGFUW0GQR1XS
BB65-RCC NGjmOJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4G4cmlEPTB;OT65O|Q6PSEQvF2= NYLLUHNEW0GQR1XS
SK-UT-1 NV;ZZopKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTFyLkO1JO69VQ>? NFz3fXVUSU6JRWK=
ST486 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjPTWM2OD1zMD6zOVEh|ryP M{Hlc3NCVkeHUh?=
LB831-BLC NIrqZ2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF73U5VKSzVyPUGxMlU3OjRizszN MXjTRW5ITVJ?
COR-L279 NVf3bW02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHV[VRKSzVyPUGyMlI6ODdizszN NED0W2hUSU6JRWK=
NB1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33CVWlEPTB;MUKuN|MxQCEQvF2= NEHkXGRUSU6JRWK=
D-247MG M1flfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjw[WVEUUN3ME2xNk4{PTF4IN88US=> NUixUXF[W0GQR1XS
697 NYHNVJA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nnZmlEPTB;MUKuOlAxPyEQvF2= M2nyc3NCVkeHUh?=
GCIY NGG5b5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;NWGtKSzVyPUGyMlg3OTNizszN MUTTRW5ITVJ?
RPMI-8402 M4DsbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTF|Lk[yOlIh|ryP NGfxZ4VUSU6JRWK=
Raji NGLuc5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorqTWM2OD1zMz63PFk1KM7:TR?= MVnTRW5ITVJ?
MEG-01 NHXkdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTxTWM2OD1zMz64N|c6KM7:TR?= NGn2OpFUSU6JRWK=
RPMI-6666 MofHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3XW5hxUUN3ME2xN{46OTJzIN88US=> M3jQZXNCVkeHUh?=
SCC-3 NX;kT5FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrPUY9KSzVyPUG0MlI6PTZizszN MmX3V2FPT0WU
HCC1599 NH;HepRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEniZohKSzVyPUG0MlU6PzVizszN M{\DT3NCVkeHUh?=
OCI-AML2 NEeyfpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7nTWM2OD1zNT62OFgzKM7:TR?= NEizUHRUSU6JRWK=
OS-RC-2 NVu1OoxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVq1NGF2UUN3ME2xOU45Ozh{IN88US=> NX3RfnFlW0GQR1XS
NCI-H1304 NFLPSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPh[5N2UUN3ME2xOk4{PjBzIN88US=> Moq2V2FPT0WU
HD-MY-Z MkTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF4LkiyOFYh|ryP Ml;2V2FPT0WU
JAR NEDhS5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPXTGZFUUN3ME2xO{4xOTV{IN88US=> MnXPV2FPT0WU
TGW NHLYTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm0Z3ZKSzVyPUG3MlgyOjRizszN NX;VS5FuW0GQR1XS
BC-3 NEnS[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTF6LkCzNFUh|ryP MnvXV2FPT0WU
A101D Mn;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LSOWlEPTB;MUiuN|IxQCEQvF2= NILhZmhUSU6JRWK=
COLO-320-HSR Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DmWWlEPTB;MUiuO|Y5QCEQvF2= M1r0RXNCVkeHUh?=
LC4-1 M362[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF6Lki3N|Qh|ryP MVvTRW5ITVJ?
BC-1 NXHGe2FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjHfFFKSzVyPUG5MlEyQThizszN MVrTRW5ITVJ?
MHH-PREB-1 NFHuTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPCZ21NUUN3ME2yNE4xOzV4IN88US=> NEGwS4FUSU6JRWK=
BL-70 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGn3TYtKSzVyPUKwMlMzPzRizszN NXGyS|RbW0GQR1XS
CESS NVTUdItVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfGPXdKSzVyPUKwMlg2PDlizszN NVf3O|d6W0GQR1XS
ES8 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrBTWM2OD1{MT6wOkDPxE1? M3q0bHNCVkeHUh?=
NOMO-1 NWDSbolIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XqdmlEPTB;MkGuNlAxQCEQvF2= M170TnNCVkeHUh?=
ACN MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLkTWM2OD1{MT6zN|g6KM7:TR?= M{\EUnNCVkeHUh?=
EB-3 M2LoW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXRc4dKSzVyPUKzMlE5OzFizszN MlL4V2FPT0WU
LS-513 M2jhdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PFdWlEPTB;MkOuOVE4QSEQvF2= Mk\zV2FPT0WU
HH NX;Tdnc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;OTGlEPTB;MkSuN|gyQSEQvF2= M{n2PXNCVkeHUh?=
IST-SL2 MofXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnJ[5ZKSzVyPUK0MlU{PDNizszN NX7pZpRxW0GQR1XS
HOP-62 MmT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzxTWM2OD1{NT60OFI2KM7:TR?= MWPTRW5ITVJ?
NCI-H2126 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f3d2lEPTB;MkWuOlUzQSEQvF2= MX\TRW5ITVJ?
BL-41 NWi4dVNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;hNGpKSzVyPUK1Mlk2QTdizszN NGTVVYRUSU6JRWK=
KURAMOCHI NVy3XXlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJ4LkiwPFIh|ryP MVzTRW5ITVJ?
KARPAS-299 M{HtWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\iOYRJUUN3ME2yOk45PjR4IN88US=> MXTTRW5ITVJ?
QIMR-WIL MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTJ5LkmxOFQh|ryP NFWwNXNUSU6JRWK=
HL-60 NUXMZXh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7rTWM2OD1{Nz65PFY6KM7:TR?= NXPCbGNPW0GQR1XS
TE-9 NU\STVY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGiwOXpKSzVyPUK4Mlc6PjlizszN NWGyd2pJW0GQR1XS
TE-8 Mn;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXlO2dKSzVyPUK4MlkxQCEQvF2= NYXxN5ZnW0GQR1XS
NOS-1 M4T0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\jOmlEPTB;MkiuPVc{OyEQvF2= M3;SdHNCVkeHUh?=
GI-1 M2\QUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJ7LkCxNVMh|ryP MW\TRW5ITVJ?
KM12 NIL3R2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HLOWlEPTB;MkmuOlI{QSEQvF2= MoDhV2FPT0WU
BB30-HNC NYDHV4Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnP[mRxUUN3ME2yPU46PDh|IN88US=> Ml;FV2FPT0WU
ES3 NIHlNmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XKS2lEPTB;MkmuPVU5OiEQvF2= MlXwV2FPT0WU
NCI-H510A NU[zW2x6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTNyLkCzNlkh|ryP M4TwNnNCVkeHUh?=
NCI-H82 MkXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTNzLkCxN|Uh|ryP NHPJRndUSU6JRWK=
NCI-SNU-1 M1LkS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTNzLkGwOVkh|ryP NYfwc2xPW0GQR1XS
NKM-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTNzLkGzPVch|ryP NHywRZdUSU6JRWK=
SIG-M5 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknLTWM2OD1|MT62PFM{KM7:TR?= MYjTRW5ITVJ?
SK-N-FI NITzOFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLnTWM2OD1|MT63OVM2KM7:TR?= MoTRV2FPT0WU
LOUCY NELhWGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PsU2lEPTB;M{KuNVI2OyEQvF2= MX;TRW5ITVJ?
Calu-6 NGT3NpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{exUmlEPTB;M{KuOFc1PSEQvF2= MkHlV2FPT0WU
GOTO NWK2RZhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTySplEUUN3ME2zNk46OTJ7IN88US=> MmP3V2FPT0WU
NCI-H526 NY[5UndIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTN|LkS5N|Yh|ryP NV;x[3lkW0GQR1XS
RKO MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEL3cGFKSzVyPUOzMlU6PjlizszN NXLaN4dDW0GQR1XS
NCI-H64 NWDlPWxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3rZnhKSzVyPUOzMlg2QTdizszN NWW4b3JDW0GQR1XS
LP-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1q5bGlEPTB;M{OuPFkxQCEQvF2= M4nibHNCVkeHUh?=
KGN MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfmdpZKSzVyPUO0MlI2OjRizszN MVfTRW5ITVJ?
NCI-H2141 NV70e4ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHveVlKSzVyPUO0MlY2OzNizszN M3HQVHNCVkeHUh?=
TE-10 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jGdWlEPTB;M{SuPVQzOiEQvF2= NFXYNm1USU6JRWK=
K5 NYfzUFBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTN3LkC4OlEh|ryP MV\TRW5ITVJ?
IMR-5 NEDlZ2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTqTWM2OD1|NT6zNVM6KM7:TR?= MU\TRW5ITVJ?
TE-441-T M4DTN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHYTWM2OD1|Nj6xNVQ5KM7:TR?= M{DrNXNCVkeHUh?=
TE-6 NHvSeo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELrfmxKSzVyPUO2MlMzPDZizszN MUjTRW5ITVJ?
MOLT-4 Ml;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWq0[4dxUUN3ME2zOk4{Ojd4IN88US=> MorFV2FPT0WU
COLO-684 M1e1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTN5LkCxNkDPxE1? MoXiV2FPT0WU
LU-139 NHLleFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zq[mlEPTB;M{euNVg2PiEQvF2= NVjNelZXW0GQR1XS
OPM-2 Mle2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLCfFVzUUN3ME2zO{4zQTR7IN88US=> NV\oVZh4W0GQR1XS
ML-2 NVfEWYhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HFV2lEPTB;M{euOlcyOiEQvF2= M17Mb3NCVkeHUh?=
RS4-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTN5LkewOlkh|ryP MlTkV2FPT0WU
MONO-MAC-6 M4\icWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr3WIlKSzVyPUO4MlI1PzdizszN M4D2S3NCVkeHUh?=
NCI-H345 NVPmRVZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTN6LkmxNFYh|ryP M4X1NHNCVkeHUh?=
NTERA-S-cl-D1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILxZmZKSzVyPUO5MlU5PDJizszN NHGzT5FUSU6JRWK=
NCI-H1882 NVjrSVRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPDdIRkUUN3ME20NE42QTl6IN88US=> NEL3TmtUSU6JRWK=
LC-1F NILyWpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWD1W5hRUUN3ME20NU42PzB3IN88US=> M3zXOXNCVkeHUh?=
HT MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnSbmwyUUN3ME20Nk4xODJ6IN88US=> M2G3UHNCVkeHUh?=
MLMA Mmr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jvd2lEPTB;NEKuNlc5PyEQvF2= NXvuV4NEW0GQR1XS
DG-75 NYH1Tmh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLtdIs5UUN3ME20Nk43PTR4IN88US=> MVLTRW5ITVJ?
GI-ME-N MlfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTR{Lk[2O|Eh|ryP MYLTRW5ITVJ?
MS-1 NYDZfFJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX0OFFKSzVyPUSyMlg6OyEQvF2= MWnTRW5ITVJ?
CGTH-W-1 M1PacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jhfGlEPTB;NESuPVY6PyEQvF2= NU\qeGpVW0GQR1XS
NCI-H209 NUDaUllqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\1TWM2OD12Nj6wNVE2KM7:TR?= NWCyTY5DW0GQR1XS
LB2518-MEL MlXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\HTWM2OD12Nz6wOFQ5KM7:TR?= M4f4XHNCVkeHUh?=
DU-4475 MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTR6LkS5N|ch|ryP Ml25V2FPT0WU
LB2241-RCC M1v4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T3ZmlEPTB;NEiuOlIxOiEQvF2= NIf0R3lUSU6JRWK=
LB771-HNC MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITEWmFKSzVyPUS4MlkzOTJizszN M13qU3NCVkeHUh?=

... 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]
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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:
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
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)

  • Mass
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    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
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    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

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02649751 Recruiting Cystic Fibrosis University Hospital, Brest|ManRos Therapeutics|Cyclacel Pharmaceuticals, Inc. February 2016 Phase 2
NCT02160730 Recruiting Cushings Disease Shlomo Melmed, MD|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Cedars-Sinai Medical Center May 2014 Phase 2
NCT01333423 Withdrawn Breast Cancer M.D. Anderson Cancer Center|National Institutes of Health (NIH) September 2012 Phase 1
NCT00999401 Recruiting Advanced Solid Tumors Cyclacel Pharmaceuticals, Inc. April 2009 Phase 1
NCT00372073 Terminated Non-small Cell Lung Cancer Cyclacel Pharmaceuticals, Inc. July 2006 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.

Handling Instructions

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

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

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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