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 NIeyUItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\hTWM2OD13Lke2NVE3KM7:TR?= M3mycnNCVkeHUh?=
MRK-nu-1 NIrzcnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTdwMUK5Olkh|ryP NEn3eJpUSU6JRWK=
NCCIT MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT4[IJKSzVyPUeuOVU1QDJizszN M4SxcHNCVkeHUh?=
JiyoyeP-2003 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInvbnhKSzVyPUiuOVAzPjRizszN MojWV2FPT0WU
KS-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzsToJKSzVyPUmuOFU4QDVizszN NYq3NlYxW0GQR1XS
Becker NXrzXY1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTLZ5ViUUN3ME25MlQ3ODh{IN88US=> M3fGb3NCVkeHUh?=
KARPAS-422 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDpTWM2OD17Lkm2N|M3KM7:TR?= M4\EfnNCVkeHUh?=
BB65-RCC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;XRWlEPTB;OT65O|Q6PSEQvF2= M3fE[HNCVkeHUh?=
SK-UT-1 NVf1c3FvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTFyLkO1JO69VQ>? MXvTRW5ITVJ?
ST486 MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXuXVFKSzVyPUGwMlM2OSEQvF2= MlHuV2FPT0WU
LB831-BLC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnBUmlKSzVyPUGxMlU3OjRizszN NHrEfI1USU6JRWK=
COR-L279 NYrQbpVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF{LkK5NFch|ryP NHXXdYRUSU6JRWK=
NB1 NF\4UJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XUe2lEPTB;MUKuN|MxQCEQvF2= MYrTRW5ITVJ?
D-247MG NWLQbZNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH6TWM2OD1zMj6zOVE3KM7:TR?= NVPLTVNlW0GQR1XS
697 NVjrblA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X2RmlEPTB;MUKuOlAxPyEQvF2= NYGwWGFPW0GQR1XS
GCIY Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofnTWM2OD1zMj64OlE{KM7:TR?= M1LtWHNCVkeHUh?=
RPMI-8402 MmjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fVOmlEPTB;MUOuOlI3OiEQvF2= MlnoV2FPT0WU
Raji NGLyc|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTF|Lke4PVQh|ryP MUPTRW5ITVJ?
MEG-01 MnfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nUbGlEPTB;MUOuPFM4QSEQvF2= M3vvWHNCVkeHUh?=
RPMI-6666 M3XDXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTF|LkmxNlEh|ryP MWPTRW5ITVJ?
SCC-3 M4LwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTF2LkK5OVYh|ryP MWXTRW5ITVJ?
HCC1599 M4nvOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu3TWM2OD1zND61PVc2KM7:TR?= NVP2W5NRW0GQR1XS
OCI-AML2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G0PGlEPTB;MUWuOlQ5OiEQvF2= NVS3PGtIW0GQR1XS
OS-RC-2 M2PyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfDUZNKSzVyPUG1Mlg{QDJizszN NF3ZPIpUSU6JRWK=
NCI-H1304 MnizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFm4UodKSzVyPUG2MlM3ODFizszN MYPTRW5ITVJ?
HD-MY-Z NWnuVnI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TpPWlEPTB;MU[uPFI1PiEQvF2= NUPEflYyW0GQR1XS
JAR NXTke4M4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF5LkCxOVIh|ryP MX3TRW5ITVJ?
TGW M{jmVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXONnVEUUN3ME2xO{45OTJ2IN88US=> NYrVUINTW0GQR1XS
BC-3 M1q0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H3UGlEPTB;MUiuNFMxPSEQvF2= MWHTRW5ITVJ?
A101D Mn7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7KOmJuUUN3ME2xPE4{OjB6IN88US=> MV;TRW5ITVJ?
COLO-320-HSR MkS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF6Lke2PFgh|ryP M33rb3NCVkeHUh?=
LC4-1 M1\wNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX1c41mUUN3ME2xPE45PzN2IN88US=> M{nG[3NCVkeHUh?=
BC-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS4[5d[UUN3ME2xPU4yOTl6IN88US=> MXXTRW5ITVJ?
MHH-PREB-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJyLkCzOVYh|ryP M4XofHNCVkeHUh?=
BL-70 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYi0VmM1UUN3ME2yNE4{Ojd2IN88US=> MmflV2FPT0WU
CESS MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HZWGlEPTB;MkCuPFU1QSEQvF2= MoG3V2FPT0WU
ES8 M33ObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfs[oNLUUN3ME2yNU4xPiEQvF2= MWTTRW5ITVJ?
NOMO-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XsbWlEPTB;MkGuNlAxQCEQvF2= M2D5NXNCVkeHUh?=
ACN NXjJS2xHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXVTWM2OD1{MT6zN|g6KM7:TR?= M{XOZnNCVkeHUh?=
EB-3 MkTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDRTWM2OD1{Mz6xPFMyKM7:TR?= Mn:2V2FPT0WU
LS-513 Ml3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTGTWM2OD1{Mz61NVc6KM7:TR?= NHfCeWVUSU6JRWK=
HH M1vsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEWyV2VKSzVyPUK0MlM5OTlizszN NILxZmhUSU6JRWK=
IST-SL2 NV;OXnA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LZOWlEPTB;MkSuOVM1OyEQvF2= MWPTRW5ITVJ?
HOP-62 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGWwS4NKSzVyPUK1MlQ1OjVizszN M4G1W3NCVkeHUh?=
NCI-H2126 M{nvdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Hae2lEPTB;MkWuOlUzQSEQvF2= M{\Bb3NCVkeHUh?=
BL-41 NYHWUVR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJ3Lkm1PVch|ryP NVPkc4s5W0GQR1XS
KURAMOCHI MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fpWGlEPTB;Mk[uPFA5OiEQvF2= M1LSR3NCVkeHUh?=
KARPAS-299 Ml\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XiUWlEPTB;Mk[uPFY1PiEQvF2= MoPlV2FPT0WU
QIMR-WIL MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfuRXJ1UUN3ME2yO{46OTR2IN88US=> NEn2So5USU6JRWK=
HL-60 M13nVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWe0TpJ5UUN3ME2yO{46QDZ7IN88US=> NFnSSVlUSU6JRWK=
TE-9 MofPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPkcpNKSzVyPUK4Mlc6PjlizszN MXnTRW5ITVJ?
TE-8 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXy0RmtUUUN3ME2yPE46ODhizszN M{ezd3NCVkeHUh?=
NOS-1 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJ6Lkm3N|Mh|ryP NX36cGtQW0GQR1XS
GI-1 MlfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\M[HQ2UUN3ME2yPU4xOTF|IN88US=> M{fU[3NCVkeHUh?=
KM12 NUnNOIYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPMTWM2OD1{OT62NlM6KM7:TR?= MnO5V2FPT0WU
BB30-HNC M4\4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUC2UJFjUUN3ME2yPU46PDh|IN88US=> M3vn[nNCVkeHUh?=
ES3 NYDqT5RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\QNGlEPTB;MkmuPVU5OiEQvF2= M37pfXNCVkeHUh?=
NCI-H510A MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HsfGlEPTB;M{CuNFMzQSEQvF2= M3zkUnNCVkeHUh?=
NCI-H82 MknzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;zNXNKSzVyPUOxMlAyOzVizszN Mn3EV2FPT0WU
NCI-SNU-1 M1\1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTNzLkGwOVkh|ryP MV3TRW5ITVJ?
NKM-1 MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTNzLkGzPVch|ryP MXLTRW5ITVJ?
SIG-M5 NHzseGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPvOVhKSzVyPUOxMlY5OzNizszN MnG5V2FPT0WU
SK-N-FI NXzmc413T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LucGlEPTB;M{GuO|U{PSEQvF2= M3v4NHNCVkeHUh?=
LOUCY NXTPfmhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXOTHBMUUN3ME2zNk4yOjV|IN88US=> NWXhSXhOW0GQR1XS
Calu-6 Mk\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7kclhtUUN3ME2zNk41PzR3IN88US=> M4DKdnNCVkeHUh?=
GOTO MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTtTWM2OD1|Mj65NVI6KM7:TR?= MnXGV2FPT0WU
NCI-H526 NF7rZWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN|LkS5N|Yh|ryP M3[xZnNCVkeHUh?=
RKO NX[3NlJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTN|LkW5Olkh|ryP NWDsTIN6W0GQR1XS
NCI-H64 M4\SWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXQfndqUUN3ME2zN{45PTl5IN88US=> MXnTRW5ITVJ?
LP-1 NEXm[|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTN|Lki5NFgh|ryP MWfTRW5ITVJ?
KGN NIHpd5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS4TWM2OD1|ND6yOVI1KM7:TR?= NVXJfnNrW0GQR1XS
NCI-H2141 MofwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWD2bW1mUUN3ME2zOE43PTN|IN88US=> MW\TRW5ITVJ?
TE-10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTN2Lkm0NlIh|ryP M4rCfHNCVkeHUh?=
K5 M1XSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTIWJc1UUN3ME2zOU4xQDZzIN88US=> M{K1c3NCVkeHUh?=
IMR-5 M3TNNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MneyTWM2OD1|NT6zNVM6KM7:TR?= MlPBV2FPT0WU
TE-441-T M4LuNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnCeYFKSzVyPUO2MlEyPDhizszN NYj1WWY1W0GQR1XS
TE-6 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPvZpNKSzVyPUO2MlMzPDZizszN MmDQV2FPT0WU
MOLT-4 M3znNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi5ZVdbUUN3ME2zOk4{Ojd4IN88US=> NVHv[mFGW0GQR1XS
COLO-684 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\SOGlEPTB;M{euNFEzKM7:TR?= MlGzV2FPT0WU
LU-139 M2TwWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHBc3ZGUUN3ME2zO{4yQDV4IN88US=> M3SyNnNCVkeHUh?=
OPM-2 NYiwOlBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm4[FlUUUN3ME2zO{4zQTR7IN88US=> Mmm4V2FPT0WU
ML-2 NIjUTXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfVZ2tKSzVyPUO3MlY4OTJizszN MnjFV2FPT0WU
RS4-11 M3P3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX3S2ZKSzVyPUO3MlcxPjlizszN NICxc3FUSU6JRWK=
MONO-MAC-6 MmXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PnT2lEPTB;M{iuNlQ4PyEQvF2= NF7YSHZUSU6JRWK=
NCI-H345 MnniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTN6LkmxNFYh|ryP NUTCV3BxW0GQR1XS
NTERA-S-cl-D1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\HTWM2OD1|OT61PFQzKM7:TR?= NWDrO214W0GQR1XS
NCI-H1882 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rEOGlEPTB;NECuOVk6QCEQvF2= M{HTNHNCVkeHUh?=
LC-1F NWLwVYx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLQTWM2OD12MT61O|A2KM7:TR?= MVLTRW5ITVJ?
HT MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXYTWM2OD12Mj6wNFI5KM7:TR?= NVm4[2xrW0GQR1XS
MLMA NE\3WWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkS4TWM2OD12Mj6yO|g4KM7:TR?= Ml\iV2FPT0WU
DG-75 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PhdmlEPTB;NEKuOlU1PiEQvF2= MoXBV2FPT0WU
GI-ME-N Mni0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTR{Lk[2O|Eh|ryP Ml;uV2FPT0WU
MS-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTR{Lki5N{DPxE1? MlHxV2FPT0WU
CGTH-W-1 NXXYcWoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTR2Lkm2PVch|ryP NX7ZZYUzW0GQR1XS
NCI-H209 NYewZXdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTR4LkCxNVUh|ryP NYDtcWRpW0GQR1XS
LB2518-MEL M4fUdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HjVWlEPTB;NEeuNFQ1QCEQvF2= MVPTRW5ITVJ?
DU-4475 NWeySHp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHRfotKSzVyPUS4MlQ6OzdizszN Ml:0V2FPT0WU
LB2241-RCC M{fQfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVn3[ZBSUUN3ME20PE43OjB{IN88US=> M2PlfXNCVkeHUh?=
LB771-HNC NGC5flFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjwbpVRUUN3ME20PE46OjF{IN88US=> NELVfohUSU6JRWK=

... 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 <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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* 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID