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 DMSO USD 191 In stock
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4 Customer Reviews

  • 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.

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NHzCNppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X1UWlEPTB;NT63OlEyPiEQvF2= NVrXOpZrW0GQR1XS
MRK-nu-1 M4\mTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXl[oJ2UUN3ME23MlEzQTZ7IN88US=> MnzoV2FPT0WU
NCCIT M2LhTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTdwNUW0PFIh|ryP MnLSV2FPT0WU
JiyoyeP-2003 MnruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfQZVVKSzVyPUiuOVAzPjRizszN MXTTRW5ITVJ?
KS-1 M1nXTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrzNGJSUUN3ME25MlQ2Pzh3IN88US=> MWnTRW5ITVJ?
Becker Ml;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7tb4JuUUN3ME25MlQ3ODh{IN88US=> NWLSOI5YW0GQR1XS
KARPAS-422 MmTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjYT|VKSzVyPUmuPVY{OzZizszN M1nie3NCVkeHUh?=
BB65-RCC NV;GT5hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LxSmlEPTB;OT65O|Q6PSEQvF2= MofsV2FPT0WU
SK-UT-1 NFLnT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rGbWlEPTB;MUCuN|Uh|ryP NVj6ToJmW0GQR1XS
ST486 M3vKZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTFyLkO1NUDPxE1? NVzucYpxW0GQR1XS
LB831-BLC NGfifHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW0TWM2OD1zMT61OlI1KM7:TR?= Mmr3V2FPT0WU
COR-L279 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT5T5FKSzVyPUGyMlI6ODdizszN M{TLbXNCVkeHUh?=
NB1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTF{LkOzNFgh|ryP MWnTRW5ITVJ?
D-247MG NH3mW2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLzRldKSzVyPUGyMlM2OTZizszN MnnyV2FPT0WU
697 NE\oS2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S3PWlEPTB;MUKuOlAxPyEQvF2= NHn3cGhUSU6JRWK=
GCIY M3vVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jJbWlEPTB;MUKuPFYyOyEQvF2= NGL2eVJUSU6JRWK=
RPMI-8402 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPTZYlKSzVyPUGzMlYzPjJizszN Mn;VV2FPT0WU
Raji M3vId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\EUWlEPTB;MUOuO|g6PCEQvF2= MVjTRW5ITVJ?
MEG-01 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF|LkizO|kh|ryP M2D3VXNCVkeHUh?=
RPMI-6666 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTF|LkmxNlEh|ryP NEXCXo9USU6JRWK=
SCC-3 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfZNotCUUN3ME2xOE4zQTV4IN88US=> NVzi[3BYW0GQR1XS
HCC1599 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4K1cmlEPTB;MUSuOVk4PSEQvF2= MXPTRW5ITVJ?
OCI-AML2 M2TzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv0TWM2OD1zNT62OFgzKM7:TR?= NG[2N|hUSU6JRWK=
OS-RC-2 NHXoTWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLBTWM2OD1zNT64N|gzKM7:TR?= MV;TRW5ITVJ?
NCI-H1304 NUfWO5V6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\2TWM2OD1zNj6zOlAyKM7:TR?= NIXRNnBUSU6JRWK=
HD-MY-Z NGjQfXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTF4LkiyOFYh|ryP MVXTRW5ITVJ?
JAR NHywV4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGW2UZhKSzVyPUG3MlAyPTJizszN M2jNSXNCVkeHUh?=
TGW NYrQSVlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF5LkixNlQh|ryP M3PDNXNCVkeHUh?=
BC-3 M4[1W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[0SWtKSzVyPUG4MlA{ODVizszN M{W4Z3NCVkeHUh?=
A101D M{nydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXoTWM2OD1zOD6zNlA5KM7:TR?= MnHmV2FPT0WU
COLO-320-HSR NHjjb2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PrcmlEPTB;MUiuO|Y5QCEQvF2= MXzTRW5ITVJ?
LC4-1 NYjPepF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4qzTWlEPTB;MUiuPFc{PCEQvF2= NUjsbIRzW0GQR1XS
BC-1 NETjdIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;xTWM2OD1zOT6xNVk5KM7:TR?= NHvENFdUSU6JRWK=
MHH-PREB-1 NXfBc|JRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDjTWM2OD1{MD6wN|U3KM7:TR?= MljEV2FPT0WU
BL-70 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXKTWM2OD1{MD6zNlc1KM7:TR?= NEH4O4lUSU6JRWK=
CESS MkPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJyLki1OFkh|ryP M3zqWXNCVkeHUh?=
ES8 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTJzLkC2JO69VQ>? M4TQXHNCVkeHUh?=
NOMO-1 M4K5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjTTWM2OD1{MT6yNFA5KM7:TR?= Mlj4V2FPT0WU
ACN M{jRU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHBb5VKSzVyPUKxMlM{QDlizszN MlWwV2FPT0WU
EB-3 MmS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Hke2lEPTB;MkOuNVg{OSEQvF2= NXnKVGI2W0GQR1XS
LS-513 MmTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTJ|LkWxO|kh|ryP MUfTRW5ITVJ?
HH NGTFSXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLMR4lKSzVyPUK0MlM5OTlizszN MYHTRW5ITVJ?
IST-SL2 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnWWHp{UUN3ME2yOE42OzR|IN88US=> NGq0do1USU6JRWK=
HOP-62 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PhSWlEPTB;MkWuOFQzPSEQvF2= NUW5cnhLW0GQR1XS
NCI-H2126 NYXWOFVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJ3Lk[1Nlkh|ryP MkK0V2FPT0WU
BL-41 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDFRoY3UUN3ME2yOU46PTl5IN88US=> MmroV2FPT0WU
KURAMOCHI MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XPfWlEPTB;Mk[uPFA5OiEQvF2= M{HYbnNCVkeHUh?=
KARPAS-299 NVezb5BuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\sTWM2OD1{Nj64OlQ3KM7:TR?= M4XCNXNCVkeHUh?=
QIMR-WIL NHPib2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJ5LkmxOFQh|ryP NEX0cplUSU6JRWK=
HL-60 NHH5SpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W4NWlEPTB;MkeuPVg3QSEQvF2= NXToZ|d3W0GQR1XS
TE-9 M3;FXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLXTWM2OD1{OD63PVY6KM7:TR?= Mn\aV2FPT0WU
TE-8 NFX3[5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XwV2lEPTB;MkiuPVA5KM7:TR?= M3q3fHNCVkeHUh?=
NOS-1 MnLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDUTWM2OD1{OD65O|M{KM7:TR?= NWL0epl3W0GQR1XS
GI-1 M2fkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;MU49FUUN3ME2yPU4xOTF|IN88US=> MkG0V2FPT0WU
KM12 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvlTWM2OD1{OT62NlM6KM7:TR?= MlHMV2FPT0WU
BB30-HNC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3VTWM2OD1{OT65OFg{KM7:TR?= MlzDV2FPT0WU
ES3 M4DqSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD6OHRKSzVyPUK5Mlk2QDJizszN NIO0WVRUSU6JRWK=
NCI-H510A MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTNyLkCzNlkh|ryP NF[3To5USU6JRWK=
NCI-H82 NFzJR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXoTWM2OD1|MT6wNVM2KM7:TR?= M3fM[HNCVkeHUh?=
NCI-SNU-1 M4S4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LjSWlEPTB;M{GuNVA2QSEQvF2= NVL5UIVwW0GQR1XS
NKM-1 M4\pT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvhVI5KSzVyPUOxMlE{QTdizszN NWj4NIQzW0GQR1XS
SIG-M5 NY\OSGpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[xXWlEPTB;M{GuOlg{OyEQvF2= M171enNCVkeHUh?=
SK-N-FI NWLXfmxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTNzLke1N|Uh|ryP NFGwZpFUSU6JRWK=
LOUCY MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTN{LkGyOVMh|ryP NH3TcWJUSU6JRWK=
Calu-6 MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHnblAxUUN3ME2zNk41PzR3IN88US=> MVLTRW5ITVJ?
GOTO NUjHOmg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTN{LkmxNlkh|ryP MUHTRW5ITVJ?
NCI-H526 M2H4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP3TWM2OD1|Mz60PVM3KM7:TR?= NFTVUFBUSU6JRWK=
RKO MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj2dI1KUUN3ME2zN{42QTZ7IN88US=> MmPyV2FPT0WU
NCI-H64 NHzRN|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEKwe49KSzVyPUOzMlg2QTdizszN MXrTRW5ITVJ?
LP-1 MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETH[HVKSzVyPUOzMlg6ODhizszN NUm2S2kyW0GQR1XS
KGN MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1X5VWlEPTB;M{SuNlUzPCEQvF2= NF;KR4VUSU6JRWK=
NCI-H2141 NYTz[ldkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLicYlKSzVyPUO0MlY2OzNizszN MYHTRW5ITVJ?
TE-10 NWXl[JR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\Xd|JLUUN3ME2zOE46PDJ{IN88US=> M17HXXNCVkeHUh?=
K5 NIjEWoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF2wcY9KSzVyPUO1MlA5PjFizszN M1jP[3NCVkeHUh?=
IMR-5 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTN3LkOxN|kh|ryP MkjEV2FPT0WU
TE-441-T NIPqd|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS4TWM2OD1|Nj6xNVQ5KM7:TR?= MWHTRW5ITVJ?
TE-6 NXHQ[WdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;NNpg5UUN3ME2zOk4{OjR4IN88US=> MX3TRW5ITVJ?
MOLT-4 M2XtSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTN4LkOyO|Yh|ryP M3HCSnNCVkeHUh?=
COLO-684 M1jZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTN5LkCxNkDPxE1? MUDTRW5ITVJ?
LU-139 M36zfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{OzT2lEPTB;M{euNVg2PiEQvF2= NFP4U|hUSU6JRWK=
OPM-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojCTWM2OD1|Nz6yPVQ6KM7:TR?= NWLIeFlbW0GQR1XS
ML-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe4ZmgxUUN3ME2zO{43PzF{IN88US=> NH2z[5VUSU6JRWK=
RS4-11 NX:0ZoRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nMS2lEPTB;M{euO|A3QSEQvF2= NITvSFdUSU6JRWK=
MONO-MAC-6 Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPEfYdKSzVyPUO4MlI1PzdizszN NGXXNo9USU6JRWK=
NCI-H345 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XPXmlEPTB;M{iuPVExPiEQvF2= M4TVTnNCVkeHUh?=
NTERA-S-cl-D1 M4DkSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH1TWM2OD1|OT61PFQzKM7:TR?= M2ew[3NCVkeHUh?=
NCI-H1882 M{CyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnsWYY1UUN3ME20NE42QTl6IN88US=> NHWwR2hUSU6JRWK=
LC-1F NHXMR|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2qxcGlEPTB;NEGuOVcxPSEQvF2= NEK1R3pUSU6JRWK=
HT MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Xye2lEPTB;NEKuNFAzQCEQvF2= M4PtdHNCVkeHUh?=
MLMA M331N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTXTWM2OD12Mj6yO|g4KM7:TR?= M1zZSnNCVkeHUh?=
DG-75 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTR{Lk[1OFYh|ryP Ml71V2FPT0WU
GI-ME-N NVf5VJRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTR{Lk[2O|Eh|ryP MknBV2FPT0WU
MS-1 M1e1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTR{Lki5N{DPxE1? M1jqU3NCVkeHUh?=
CGTH-W-1 NFzYOYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLlTopKSzVyPUS0Mlk3QTdizszN MnftV2FPT0WU
NCI-H209 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTR4LkCxNVUh|ryP NF;FbYVUSU6JRWK=
LB2518-MEL NX2xU29QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnBXXlKSzVyPUS3MlA1PDhizszN NVewWmNCW0GQR1XS
DU-4475 M{DzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzDXnhKSzVyPUS4MlQ6OzdizszN NFHQeI5USU6JRWK=
LB2241-RCC MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTkTWM2OD12OD62NlAzKM7:TR?= MlL0V2FPT0WU
LB771-HNC Mk\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7yTWM2OD12OD65NlEzKM7:TR?= MYTTRW5ITVJ?

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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 <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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The Serial Dilution Calculator Equation

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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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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)
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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID