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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5 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.

  • (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 NILUfIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\pTWM2OD13Lke2NVE3KM7:TR?= NVjZd5RGW0GQR1XS
MRK-nu-1 NX7SOIRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoO3TWM2OD15LkGyPVY6KM7:TR?= NVzwXZFpW0GQR1XS
NCCIT M1e2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIraVHZKSzVyPUeuOVU1QDJizszN Mk\RV2FPT0WU
JiyoyeP-2003 NHPCN5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRThwNUCyOlQh|ryP MkHJV2FPT0WU
KS-1 NXTNUJh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTyTWM2OD17LkS1O|g2KM7:TR?= NFTSTFNUSU6JRWK=
Becker NFjndYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnNWFRKSzVyPUmuOFYxQDJizszN MWLTRW5ITVJ?
KARPAS-422 M3\oV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXftOHRVUUN3ME25Mlk3OzN4IN88US=> Mnf2V2FPT0WU
BB65-RCC M1T4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1n6VmlEPTB;OT65O|Q6PSEQvF2= NXnpR3VDW0GQR1XS
SK-UT-1 NXmzTHo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPRTWM2OD1zMD6zOUDPxE1? NUT4dYlRW0GQR1XS
ST486 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSxbYJUUUN3ME2xNE4{PTFizszN NIDtfJVUSU6JRWK=
LB831-BLC NE\kNmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjHTWM2OD1zMT61OlI1KM7:TR?= M1HPVHNCVkeHUh?=
COR-L279 NFLreJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLzbIZsUUN3ME2xNk4zQTB5IN88US=> MYTTRW5ITVJ?
NB1 NVzXe2VGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvUUI4zUUN3ME2xNk4{OzB6IN88US=> Mn3mV2FPT0WU
D-247MG Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTF{LkO1NVYh|ryP NF\FXVdUSU6JRWK=
697 M{nSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr3T3VKSzVyPUGyMlYxODdizszN NF[zZmlUSU6JRWK=
GCIY NIj3XXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTF{Lki2NVMh|ryP NHPmSYdUSU6JRWK=
RPMI-8402 NW\uSmpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTF|Lk[yOlIh|ryP NWjtXY1bW0GQR1XS
Raji NHXQfnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPXTWM2OD1zMz63PFk1KM7:TR?= NEPneIxUSU6JRWK=
MEG-01 NV7YVINYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDFelRKSzVyPUGzMlg{PzlizszN M3XUVXNCVkeHUh?=
RPMI-6666 MnHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[wdXNKSzVyPUGzMlkyOjFizszN M{W3RnNCVkeHUh?=
SCC-3 M4TlVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LsUmlEPTB;MUSuNlk2PiEQvF2= NXK0clNUW0GQR1XS
HCC1599 NVLrdXRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PlSmlEPTB;MUSuOVk4PSEQvF2= NWLRV|d6W0GQR1XS
OCI-AML2 NXvROYtbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm2TYpDUUN3ME2xOU43PDh{IN88US=> M4LPPHNCVkeHUh?=
OS-RC-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3iTWM2OD1zNT64N|gzKM7:TR?= M4LwT3NCVkeHUh?=
NCI-H1304 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLT[JJNUUN3ME2xOk4{PjBzIN88US=> NGjSeHlUSU6JRWK=
HD-MY-Z NXXxem9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDuSmtiUUN3ME2xOk45OjR4IN88US=> NVnB[IFKW0GQR1XS
JAR NGPIUppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17scmlEPTB;MUeuNFE2OiEQvF2= M1voR3NCVkeHUh?=
TGW M4naTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTpUoJKSzVyPUG3MlgyOjRizszN M{XidXNCVkeHUh?=
BC-3 M1PrNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rsOGlEPTB;MUiuNFMxPSEQvF2= NGnCfYJUSU6JRWK=
A101D MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDlTWM2OD1zOD6zNlA5KM7:TR?= NEfoXJVUSU6JRWK=
COLO-320-HSR NGHvU4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF6Lke2PFgh|ryP NULsZ4xtW0GQR1XS
LC4-1 NIf0So1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jEdmlEPTB;MUiuPFc{PCEQvF2= MUTTRW5ITVJ?
BC-1 M1:zNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHFe|dKSzVyPUG5MlEyQThizszN M1e3RXNCVkeHUh?=
MHH-PREB-1 NFy0UoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYO5SZQyUUN3ME2yNE4xOzV4IN88US=> M1\0c3NCVkeHUh?=
BL-70 NHO5XWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXucpdKSzVyPUKwMlMzPzRizszN NWDyclB7W0GQR1XS
CESS NV3yR29oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELpVGZKSzVyPUKwMlg2PDlizszN Mn7XV2FPT0WU
ES8 NXHJeVFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:yTWM2OD1{MT6wOkDPxE1? MoG1V2FPT0WU
NOMO-1 NEXDdHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlryTWM2OD1{MT6yNFA5KM7:TR?= NVTMR2xQW0GQR1XS
ACN M2K0b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfnR4pWUUN3ME2yNU4{Ozh7IN88US=> Mnu4V2FPT0WU
EB-3 Mn\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEK5S5pKSzVyPUKzMlE5OzFizszN MoLYV2FPT0WU
LS-513 NFTkfYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPqTWM2OD1{Mz61NVc6KM7:TR?= MYHTRW5ITVJ?
HH MoXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LpZmlEPTB;MkSuN|gyQSEQvF2= Ml;rV2FPT0WU
IST-SL2 NHfoZYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrHPJhQUUN3ME2yOE42OzR|IN88US=> NV\OVW5zW0GQR1XS
HOP-62 NIjuNFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHLTWM2OD1{NT60OFI2KM7:TR?= MYrTRW5ITVJ?
NCI-H2126 Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr6RYdKSzVyPUK1MlY2OjlizszN Mke5V2FPT0WU
BL-41 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLuTWM2OD1{NT65OVk4KM7:TR?= M4r6UXNCVkeHUh?=
KURAMOCHI MkHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nNUWlEPTB;Mk[uPFA5OiEQvF2= NVG3TGV2W0GQR1XS
KARPAS-299 NWPlO|IxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJ4Lki2OFYh|ryP NI\1bXRUSU6JRWK=
QIMR-WIL NGfzV5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S0bGlEPTB;MkeuPVE1PCEQvF2= M1HVSHNCVkeHUh?=
HL-60 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHYNlhKSzVyPUK3Mlk5PjlizszN M2\jWnNCVkeHUh?=
TE-9 M4rv[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTOR3dTUUN3ME2yPE44QTZ7IN88US=> NYjDSFJ4W0GQR1XS
TE-8 M4XXbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nxb2lEPTB;MkiuPVA5KM7:TR?= NHPjcpNUSU6JRWK=
NOS-1 MkLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTJ6Lkm3N|Mh|ryP NUfXTFVOW0GQR1XS
GI-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTJ7LkCxNVMh|ryP M1n1T3NCVkeHUh?=
KM12 NEDEWlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX0WItKSzVyPUK5MlYzOzlizszN MYDTRW5ITVJ?
BB30-HNC NETOWldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHYTWM2OD1{OT65OFg{KM7:TR?= MVXTRW5ITVJ?
ES3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjjTWM2OD1{OT65OVgzKM7:TR?= NFToOJlUSU6JRWK=
NCI-H510A MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP5TWM2OD1|MD6wN|I6KM7:TR?= MofPV2FPT0WU
NCI-H82 NWG0T4E2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnxO5M{UUN3ME2zNU4xOTN3IN88US=> NUXZUpg5W0GQR1XS
NCI-SNU-1 NXi4eFF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPhe4RqUUN3ME2zNU4yODV7IN88US=> MVfTRW5ITVJ?
NKM-1 MorES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTNzLkGzPVch|ryP M{fHb3NCVkeHUh?=
SIG-M5 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\FXGlEPTB;M{GuOlg{OyEQvF2= M3WyUHNCVkeHUh?=
SK-N-FI MmPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTNzLke1N|Uh|ryP NY\Od41iW0GQR1XS
LOUCY M1\ISmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTN{LkGyOVMh|ryP MlntV2FPT0WU
Calu-6 M2DOVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTN{LkS3OFUh|ryP MlLvV2FPT0WU
GOTO MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG4bnhKSzVyPUOyMlkyOjlizszN MULTRW5ITVJ?
NCI-H526 M1rpUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXwZY1[UUN3ME2zN{41QTN4IN88US=> NISyU5dUSU6JRWK=
RKO NHLhNnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTN|LkW5Olkh|ryP MY\TRW5ITVJ?
NCI-H64 M2P4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjKeJdiUUN3ME2zN{45PTl5IN88US=> MV3TRW5ITVJ?
LP-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHa[|U3UUN3ME2zN{45QTB6IN88US=> NV7EOWxSW0GQR1XS
KGN NHXleHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PXN2lEPTB;M{SuNlUzPCEQvF2= MXLTRW5ITVJ?
NCI-H2141 M2LSWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7PTWM2OD1|ND62OVM{KM7:TR?= M1nXXXNCVkeHUh?=
TE-10 NYLSfGVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P6UWlEPTB;M{SuPVQzOiEQvF2= NU\P[4w5W0GQR1XS
K5 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjQToFuUUN3ME2zOU4xQDZzIN88US=> MkX4V2FPT0WU
IMR-5 MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfiOnprUUN3ME2zOU4{OTN7IN88US=> NF;QcXNUSU6JRWK=
TE-441-T MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPCTWM2OD1|Nj6xNVQ5KM7:TR?= Mkm1V2FPT0WU
TE-6 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnFSYZtUUN3ME2zOk4{OjR4IN88US=> MkjpV2FPT0WU
MOLT-4 M2\jd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7aTWM2OD1|Nj6zNlc3KM7:TR?= MYfTRW5ITVJ?
COLO-684 NYHRZVY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHIS2NIUUN3ME2zO{4xOTJizszN MVHTRW5ITVJ?
LU-139 M3jEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDmWllKSzVyPUO3MlE5PTZizszN MX;TRW5ITVJ?
OPM-2 MoGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u0cGlEPTB;M{euNlk1QSEQvF2= MUTTRW5ITVJ?
ML-2 NVy1ZpZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS1N49jUUN3ME2zO{43PzF{IN88US=> NETrXW9USU6JRWK=
RS4-11 M{jRZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXpV3dKSzVyPUO3MlcxPjlizszN MV3TRW5ITVJ?
MONO-MAC-6 NIPkXVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTN6LkK0O|ch|ryP MXPTRW5ITVJ?
NCI-H345 NYL5[YF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\hc5VUUUN3ME2zPE46OTB4IN88US=> MojDV2FPT0WU
NTERA-S-cl-D1 M1\s[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHyc5VzUUN3ME2zPU42QDR{IN88US=> NHLkdnJUSU6JRWK=
NCI-H1882 MnjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jvPGlEPTB;NECuOVk6QCEQvF2= M{fySHNCVkeHUh?=
LC-1F NXPnT21DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjMTWM2OD12MT61O|A2KM7:TR?= M1LWXXNCVkeHUh?=
HT MnzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTR{LkCwNlgh|ryP MnS1V2FPT0WU
MLMA NVz1UWpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLwTWM2OD12Mj6yO|g4KM7:TR?= M4DzPHNCVkeHUh?=
DG-75 MmLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\YTWM2OD12Mj62OVQ3KM7:TR?= MmfIV2FPT0WU
GI-ME-N NF24eoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq0TWM2OD12Mj62OlcyKM7:TR?= MVvTRW5ITVJ?
MS-1 NWDWTFc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37JTGlEPTB;NEKuPFk{KM7:TR?= NFrCUFJUSU6JRWK=
CGTH-W-1 M1vwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTGRXFmUUN3ME20OE46Pjl5IN88US=> M4\vVXNCVkeHUh?=
NCI-H209 NWjyNFNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDmPIRKSzVyPUS2MlAyOTVizszN MlX0V2FPT0WU
LB2518-MEL MlrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu4PZRKSzVyPUS3MlA1PDhizszN Mmj1V2FPT0WU
DU-4475 MnjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXqTWM2OD12OD60PVM4KM7:TR?= MofPV2FPT0WU
LB2241-RCC MmDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTR6Lk[yNFIh|ryP NGO3b|VUSU6JRWK=
LB771-HNC NVvhNXlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXyTWM2OD12OD65NlEzKM7:TR?= NGjoS3pUSU6JRWK=

... 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
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 )

  • 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID