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 NETyTYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fsdWlEPTB;NT63OlEyPiEQvF2= NEO1XoJUSU6JRWK=
MRK-nu-1 NVPzW5ZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7KSIlmUUN3ME23MlEzQTZ7IN88US=> MV\TRW5ITVJ?
NCCIT M{X5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3nZlNKSzVyPUeuOVU1QDJizszN NXf6dooyW0GQR1XS
JiyoyeP-2003 NIjjVWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LmUmlEPTB;OD61NFI3PCEQvF2= NEW2V2lUSU6JRWK=
KS-1 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13pS2lEPTB;OT60OVc5PSEQvF2= NWHF[JVuW0GQR1XS
Becker M{OwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4juSmlEPTB;OT60OlA5OiEQvF2= MmjwV2FPT0WU
KARPAS-422 M{PtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD1XlZKSzVyPUmuPVY{OzZizszN NFvwUnpUSU6JRWK=
BB65-RCC MojaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXIPGZ{UUN3ME25Mlk4PDl3IN88US=> NEHHdmRUSU6JRWK=
SK-UT-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFyLkO1JO69VQ>? NEGxN3dUSU6JRWK=
ST486 M2XSPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHzNHZKSzVyPUGwMlM2OSEQvF2= NF\FTphUSU6JRWK=
LB831-BLC M2frVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFzLkW2NlQh|ryP MYXTRW5ITVJ?
COR-L279 NVP1ZYlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTF{LkK5NFch|ryP NFXJT2lUSU6JRWK=
NB1 NFn3VYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nDVmlEPTB;MUKuN|MxQCEQvF2= NX;VVlJzW0GQR1XS
D-247MG NVHyXIZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjMdINKSzVyPUGyMlM2OTZizszN NEP0NIlUSU6JRWK=
697 M4HEXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jPSWlEPTB;MUKuOlAxPyEQvF2= NFS2[WdUSU6JRWK=
GCIY M1LpdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrzOWVKSzVyPUGyMlg3OTNizszN NIGzeYJUSU6JRWK=
RPMI-8402 NFXte4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTF|Lk[yOlIh|ryP MYPTRW5ITVJ?
Raji NXHL[4s5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;UT4dwUUN3ME2xN{44QDl2IN88US=> M3fBRXNCVkeHUh?=
MEG-01 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;FTWM2OD1zMz64N|c6KM7:TR?= MWfTRW5ITVJ?
RPMI-6666 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGToTIxKSzVyPUGzMlkyOjFizszN Mn;qV2FPT0WU
SCC-3 NUHSTIJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\hUGYyUUN3ME2xOE4zQTV4IN88US=> MULTRW5ITVJ?
HCC1599 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTUTWM2OD1zND61PVc2KM7:TR?= NXnVWJFDW0GQR1XS
OCI-AML2 M{DnOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjzNHo3UUN3ME2xOU43PDh{IN88US=> M17pW3NCVkeHUh?=
OS-RC-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK0cYlKSzVyPUG1Mlg{QDJizszN MlXoV2FPT0WU
NCI-H1304 M3\UVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTF4LkO2NFEh|ryP MVTTRW5ITVJ?
HD-MY-Z NIPPcIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnkV|cyUUN3ME2xOk45OjR4IN88US=> MlrYV2FPT0WU
JAR MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlGzTWM2OD1zNz6wNVUzKM7:TR?= MkO3V2FPT0WU
TGW M4nMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfLcplKSzVyPUG3MlgyOjRizszN MVjTRW5ITVJ?
BC-3 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD1TWM2OD1zOD6wN|A2KM7:TR?= MWLTRW5ITVJ?
A101D NVGwNHVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DNSGlEPTB;MUiuN|IxQCEQvF2= M4XuV3NCVkeHUh?=
COLO-320-HSR NVXsTZJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF6Lke2PFgh|ryP NVvCWogxW0GQR1XS
LC4-1 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHDTWM2OD1zOD64O|M1KM7:TR?= MonZV2FPT0WU
BC-1 M{XmeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r1emlEPTB;MUmuNVE6QCEQvF2= M3[3e3NCVkeHUh?=
MHH-PREB-1 M{fLTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\YZmdJUUN3ME2yNE4xOzV4IN88US=> NEjUNndUSU6JRWK=
BL-70 NFvaV3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HEWGlEPTB;MkCuN|I4PCEQvF2= MYTTRW5ITVJ?
CESS MoPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnz5TWM2OD1{MD64OVQ6KM7:TR?= NFq3eJNUSU6JRWK=
ES8 Mk[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGH2d4dKSzVyPUKxMlA3KM7:TR?= Mk\kV2FPT0WU
NOMO-1 Mme4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJzLkKwNFgh|ryP MXTTRW5ITVJ?
ACN MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPQZnFKSzVyPUKxMlM{QDlizszN NXf1RZhOW0GQR1XS
EB-3 MkLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJ|LkG4N|Eh|ryP M{jhNXNCVkeHUh?=
LS-513 NWrtPXcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVezbmltUUN3ME2yN{42OTd7IN88US=> M17zNnNCVkeHUh?=
HH MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj0O|IxUUN3ME2yOE4{QDF7IN88US=> NHXLZnhUSU6JRWK=
IST-SL2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTJ2LkWzOFMh|ryP NHf3Xm9USU6JRWK=
HOP-62 NEfjUoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vQfGlEPTB;MkWuOFQzPSEQvF2= MWjTRW5ITVJ?
NCI-H2126 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LoRmlEPTB;MkWuOlUzQSEQvF2= MV7TRW5ITVJ?
BL-41 M1PQVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLtTWM2OD1{NT65OVk4KM7:TR?= NILrfG1USU6JRWK=
KURAMOCHI M4\aPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17rdmlEPTB;Mk[uPFA5OiEQvF2= NGrJe|ZUSU6JRWK=
KARPAS-299 NFn2e2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;XNZJKSzVyPUK2Mlg3PDZizszN MV7TRW5ITVJ?
QIMR-WIL NGi0eXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnVVJFZUUN3ME2yO{46OTR2IN88US=> MkXmV2FPT0WU
HL-60 M1;jWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u2fGlEPTB;MkeuPVg3QSEQvF2= MV3TRW5ITVJ?
TE-9 MmKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor4TWM2OD1{OD63PVY6KM7:TR?= NWXZ[G1WW0GQR1XS
TE-8 NU[4WJpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJ6LkmwPEDPxE1? NUP1[|M5W0GQR1XS
NOS-1 MkDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHkTWM2OD1{OD65O|M{KM7:TR?= NGOxS49USU6JRWK=
GI-1 MnS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TwPGlEPTB;MkmuNFEyOyEQvF2= M1z3VnNCVkeHUh?=
KM12 NHfGbINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nndGlEPTB;MkmuOlI{QSEQvF2= M{mxNHNCVkeHUh?=
BB30-HNC MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1m4cGlEPTB;MkmuPVQ5OyEQvF2= Mmn2V2FPT0WU
ES3 MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr5cpVSUUN3ME2yPU46PTh{IN88US=> MnvmV2FPT0WU
NCI-H510A NGD2[WpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3YOm5CUUN3ME2zNE4xOzJ7IN88US=> MnrMV2FPT0WU
NCI-H82 NVrPW|Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3y0cWlEPTB;M{GuNFE{PSEQvF2= MVnTRW5ITVJ?
NCI-SNU-1 NUjvXXM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTNzLkGwOVkh|ryP MoW4V2FPT0WU
NKM-1 MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIe2Xo5KSzVyPUOxMlE{QTdizszN NF7x[|BUSU6JRWK=
SIG-M5 MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHjTWM2OD1|MT62PFM{KM7:TR?= M{SxUHNCVkeHUh?=
SK-N-FI MlXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTNzLke1N|Uh|ryP NIradmRUSU6JRWK=
LOUCY NXfXS5lKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:5d5l{UUN3ME2zNk4yOjV|IN88US=> NHLnT|RUSU6JRWK=
Calu-6 NYHOfVNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7t[GlJUUN3ME2zNk41PzR3IN88US=> NWD2SYVYW0GQR1XS
GOTO NH;KeGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLNTZZJUUN3ME2zNk46OTJ7IN88US=> NXTUe2FZW0GQR1XS
NCI-H526 Ml7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjmc5pKSzVyPUOzMlQ6OzZizszN NFrM[3VUSU6JRWK=
RKO NY\oRpVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTN|LkW5Olkh|ryP MYXTRW5ITVJ?
NCI-H64 NHXhRYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;zTZNKSzVyPUOzMlg2QTdizszN MljHV2FPT0WU
LP-1 NWq0d4RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfSPYhKSzVyPUOzMlg6ODhizszN NWH6U5Q2W0GQR1XS
KGN M4nWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnPOFZIUUN3ME2zOE4zPTJ2IN88US=> M{\OUnNCVkeHUh?=
NCI-H2141 M1K3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLSTWM2OD1|ND62OVM{KM7:TR?= NUnyOXhxW0GQR1XS
TE-10 MlrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrwTWM2OD1|ND65OFIzKM7:TR?= MlH3V2FPT0WU
K5 NV3KfGxPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXQ[GlKSzVyPUO1MlA5PjFizszN NHW0cWdUSU6JRWK=
IMR-5 MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnVbGJTUUN3ME2zOU4{OTN7IN88US=> Mor0V2FPT0WU
TE-441-T Mn:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\ETWM2OD1|Nj6xNVQ5KM7:TR?= M2H4WXNCVkeHUh?=
TE-6 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrqTWM2OD1|Nj6zNlQ3KM7:TR?= Mlf3V2FPT0WU
MOLT-4 NUHH[YdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrvTWM2OD1|Nj6zNlc3KM7:TR?= MUjTRW5ITVJ?
COLO-684 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHqbXJKSzVyPUO3MlAyOiEQvF2= MUHTRW5ITVJ?
LU-139 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzUXIhKSzVyPUO3MlE5PTZizszN MXrTRW5ITVJ?
OPM-2 MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fHeWlEPTB;M{euNlk1QSEQvF2= NHHSO4VUSU6JRWK=
ML-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[2TWM2OD1|Nz62O|EzKM7:TR?= MU\TRW5ITVJ?
RS4-11 NUTWdIdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XDZmlEPTB;M{euO|A3QSEQvF2= Mn3qV2FPT0WU
MONO-MAC-6 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jVV2lEPTB;M{iuNlQ4PyEQvF2= Mn3BV2FPT0WU
NCI-H345 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\EV40zUUN3ME2zPE46OTB4IN88US=> NWfkfI9bW0GQR1XS
NTERA-S-cl-D1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTsZZpOUUN3ME2zPU42QDR{IN88US=> NYnnOmlMW0GQR1XS
NCI-H1882 M1vuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr4TWM2OD12MD61PVk5KM7:TR?= NE\KZYZUSU6JRWK=
LC-1F NF:wVZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTFeVVKSzVyPUSxMlU4ODVizszN MkL5V2FPT0WU
HT NX3BNnQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS4TWM2OD12Mj6wNFI5KM7:TR?= NVzhZoNFW0GQR1XS
MLMA NEHwfotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVWxfo04UUN3ME20Nk4zPzh5IN88US=> MX3TRW5ITVJ?
DG-75 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTR{Lk[1OFYh|ryP NX64epdwW0GQR1XS
GI-ME-N M3rTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XIUmlEPTB;NEKuOlY4OSEQvF2= NFz6UlJUSU6JRWK=
MS-1 NHvDVnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTR{Lki5N{DPxE1? M3vDU3NCVkeHUh?=
CGTH-W-1 MoPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrMTWM2OD12ND65Olk4KM7:TR?= M1TUb3NCVkeHUh?=
NCI-H209 M{nBcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTR4LkCxNVUh|ryP MUXTRW5ITVJ?
LB2518-MEL MmjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrTWlNKSzVyPUS3MlA1PDhizszN NFnQcnVUSU6JRWK=
DU-4475 NW\SUYFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC4TWM2OD12OD60PVM4KM7:TR?= MX3TRW5ITVJ?
LB2241-RCC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LFRWlEPTB;NEiuOlIxOiEQvF2= NFnk[21USU6JRWK=
LB771-HNC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfi[41KSzVyPUS4MlkzOTJizszN NWHNcXhlW0GQR1XS

... 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 individually and in order:
1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+69% PEG 400
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).

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 )

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* 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

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  • 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):
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    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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID