Roscovitine (Seliciclib,CYC202)

製品コードS1153

Roscovitine (Seliciclib,CYC202)化学構造

分子量(MW):354.45

Roscovitine (Seliciclib,CYC202)は一種の有効で、選択性的なCDK阻害剤、Cdc2、CDK2とCDK5に作用する時のIC50値が0.65μM、0.7μMと0.16μMにそれぞれ分かれることですが、CDK4/6に殆ど作用しません。臨床2期。

サイズ 価格(税別)  
JPY 31722.00
JPY 24402.00
JPY 78020.00
JPY 161020.00

カスタマーフィードバック(5)

  • 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.

製品安全説明書

CDK阻害剤の選択性比較

生物活性

製品説明 Roscovitine (Seliciclib,CYC202)は一種の有効で、選択性的なCDK阻害剤、Cdc2、CDK2とCDK5に作用する時のIC50値が0.65μM、0.7μMと0.16μMにそれぞれ分かれることですが、CDK4/6に殆ど作用しません。臨床2期。
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A3-KAW MnPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHi4[3BKSzVyPUWuO|YyOTZizszN NX[wT2tvW0GQR1XS
MRK-nu-1 NUDHRY92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrITWM2OD15LkGyPVY6KM7:TR?= NYG1RXRoW0GQR1XS
NCCIT M1rBOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWT5OllnUUN3ME23MlU2PDh{IN88US=> MWXTRW5ITVJ?
JiyoyeP-2003 M13lS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRThwNUCyOlQh|ryP NWDGZnFMW0GQR1XS
KS-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7kflI6UUN3ME25MlQ2Pzh3IN88US=> MVfTRW5ITVJ?
Becker Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYWxelZwUUN3ME25MlQ3ODh{IN88US=> NYC3d|ZwW0GQR1XS
KARPAS-422 NHnzZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTlwOU[zN|Yh|ryP M2\QVXNCVkeHUh?=
BB65-RCC MkHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDKTWM2OD17Lkm3OFk2KM7:TR?= NH;5dW9USU6JRWK=
SK-UT-1 NXrCR5d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\0[mlEPTB;MUCuN|Uh|ryP NEK0XodUSU6JRWK=
ST486 M33G[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[zXVF1UUN3ME2xNE4{PTFizszN NH2zelVUSU6JRWK=
LB831-BLC MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTFzLkW2NlQh|ryP NWjOU5YzW0GQR1XS
COR-L279 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2GwUWlEPTB;MUKuNlkxPyEQvF2= NW[4bWN[W0GQR1XS
NB1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\ud|lGUUN3ME2xNk4{OzB6IN88US=> Mni3V2FPT0WU
D-247MG NWfVXVhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLLSHhrUUN3ME2xNk4{PTF4IN88US=> NYS3dW1lW0GQR1XS
697 M33hfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnVXYhKSzVyPUGyMlYxODdizszN M37PbnNCVkeHUh?=
GCIY MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTF{Lki2NVMh|ryP M4fiPXNCVkeHUh?=
RPMI-8402 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH6TWM2OD1zMz62NlYzKM7:TR?= NF:wOGpUSU6JRWK=
Raji M1\TXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvMTWM2OD1zMz63PFk1KM7:TR?= NGiyUFRUSU6JRWK=
MEG-01 M{LXSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD0b2VKUUN3ME2xN{45Ozd7IN88US=> M{DBcHNCVkeHUh?=
RPMI-6666 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD2SGdQUUN3ME2xN{46OTJzIN88US=> MkX1V2FPT0WU
SCC-3 NG\6b2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTF2LkK5OVYh|ryP M3zKbXNCVkeHUh?=
HCC1599 MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M136PWlEPTB;MUSuOVk4PSEQvF2= M4PVSnNCVkeHUh?=
OCI-AML2 NVPkW45YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vIcWlEPTB;MUWuOlQ5OiEQvF2= NVXNeol2W0GQR1XS
OS-RC-2 MnHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF3LkizPFIh|ryP NFvQT|BUSU6JRWK=
NCI-H1304 NFvHT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTF4LkO2NFEh|ryP MWXTRW5ITVJ?
HD-MY-Z M1\WTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfxRm5KSzVyPUG2MlgzPDZizszN MlTHV2FPT0WU
JAR NVvUOmFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfwTWM2OD1zNz6wNVUzKM7:TR?= MV\TRW5ITVJ?
TGW NETISGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fKcmlEPTB;MUeuPFEzPCEQvF2= NETkU4dUSU6JRWK=
BC-3 NWTqdo9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13HSWlEPTB;MUiuNFMxPSEQvF2= NVnDO3lHW0GQR1XS
A101D MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rvUmlEPTB;MUiuN|IxQCEQvF2= MoXSV2FPT0WU
COLO-320-HSR M3r5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDZVWlKSzVyPUG4Mlc3QDhizszN MWTTRW5ITVJ?
LC4-1 M1nPW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHqTWM2OD1zOD64O|M1KM7:TR?= NHHnUYFUSU6JRWK=
BC-1 NU\KPFN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3qycGlEPTB;MUmuNVE6QCEQvF2= NIHFSZRUSU6JRWK=
MHH-PREB-1 NECz[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\EUG5KSzVyPUKwMlA{PTZizszN NVKzN3E2W0GQR1XS
BL-70 MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLsTWM2OD1{MD6zNlc1KM7:TR?= NUT0eGd{W0GQR1XS
CESS M33Cemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXLTWM2OD1{MD64OVQ6KM7:TR?= M1TCcnNCVkeHUh?=
ES8 MoPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTJzLkC2JO69VQ>? MY\TRW5ITVJ?
NOMO-1 NW\GdIx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmzN5lQUUN3ME2yNU4zODB6IN88US=> MmD1V2FPT0WU
ACN NFf3OopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjI[oJWUUN3ME2yNU4{Ozh7IN88US=> NIjXVotUSU6JRWK=
EB-3 NHXLeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zHWGlEPTB;MkOuNVg{OSEQvF2= MlTaV2FPT0WU
LS-513 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXznU2luUUN3ME2yN{42OTd7IN88US=> NGnQcIxUSU6JRWK=
HH MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PEO2lEPTB;MkSuN|gyQSEQvF2= MUfTRW5ITVJ?
IST-SL2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTvTWM2OD1{ND61N|Q{KM7:TR?= MnLhV2FPT0WU
HOP-62 Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJ3LkS0NlUh|ryP MVvTRW5ITVJ?
NCI-H2126 NHTHOWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MormTWM2OD1{NT62OVI6KM7:TR?= NFW5OI5USU6JRWK=
BL-41 Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTJ3Lkm1PVch|ryP NEDDfWFUSU6JRWK=
KURAMOCHI MkDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ4LkiwPFIh|ryP MXrTRW5ITVJ?
KARPAS-299 NHu4SoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfB[lhKSzVyPUK2Mlg3PDZizszN MYnTRW5ITVJ?
QIMR-WIL M4D3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmm3TWM2OD1{Nz65NVQ1KM7:TR?= M3Xsb3NCVkeHUh?=
HL-60 M1jpdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj4WJl5UUN3ME2yO{46QDZ7IN88US=> NUPXeG1mW0GQR1XS
TE-9 M{\kNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDITWM2OD1{OD63PVY6KM7:TR?= M3TKXXNCVkeHUh?=
TE-8 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjBRW9KSzVyPUK4MlkxQCEQvF2= NWXO[G9wW0GQR1XS
NOS-1 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTJ6Lkm3N|Mh|ryP NWnkNFJzW0GQR1XS
GI-1 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJ7LkCxNVMh|ryP NWWwXVdyW0GQR1XS
KM12 M1zsbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37mUmlEPTB;MkmuOlI{QSEQvF2= MVjTRW5ITVJ?
BB30-HNC NHfh[o5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PGeWlEPTB;MkmuPVQ5OyEQvF2= NVK4eWpqW0GQR1XS
ES3 M3vzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\BTWM2OD1{OT65OVgzKM7:TR?= M3\UbnNCVkeHUh?=
NCI-H510A NHjDTYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfMUZl2UUN3ME2zNE4xOzJ7IN88US=> NWXPSlNbW0GQR1XS
NCI-H82 Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTMTWM2OD1|MT6wNVM2KM7:TR?= M{\KZXNCVkeHUh?=
NCI-SNU-1 Ml3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PPbmlEPTB;M{GuNVA2QSEQvF2= NFjkfY1USU6JRWK=
NKM-1 M1TnXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfVRpFKSzVyPUOxMlE{QTdizszN MW\TRW5ITVJ?
SIG-M5 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTNzLk[4N|Mh|ryP NGSwTYxUSU6JRWK=
SK-N-FI MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjjVVRKSzVyPUOxMlc2OzVizszN NHe0[|NUSU6JRWK=
LOUCY NXO4TGlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTN{LkGyOVMh|ryP M4i4eHNCVkeHUh?=
Calu-6 Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTN{LkS3OFUh|ryP NUThcJNOW0GQR1XS
GOTO NHPaS4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG0SVliUUN3ME2zNk46OTJ7IN88US=> MUjTRW5ITVJ?
NCI-H526 MlH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33pVGlEPTB;M{OuOFk{PiEQvF2= NYjxW4FkW0GQR1XS
RKO M37nUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXDWFNKSzVyPUOzMlU6PjlizszN Mo\QV2FPT0WU
NCI-H64 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXuxbnZnUUN3ME2zN{45PTl5IN88US=> M1W1WXNCVkeHUh?=
LP-1 NWe1W2RNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTN|Lki5NFgh|ryP MUnTRW5ITVJ?
KGN NFjVNlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPyW2NKSzVyPUO0MlI2OjRizszN NF2xWmRUSU6JRWK=
NCI-H2141 MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn62TWM2OD1|ND62OVM{KM7:TR?= NFLQe|NUSU6JRWK=
TE-10 NXm2PZl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTN2Lkm0NlIh|ryP M3XW[3NCVkeHUh?=
K5 MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{H2fGlEPTB;M{WuNFg3OSEQvF2= MUXTRW5ITVJ?
IMR-5 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLRTHhKSzVyPUO1MlMyOzlizszN NX\FWWRrW0GQR1XS
TE-441-T NFjie5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\He2lEPTB;M{[uNVE1QCEQvF2= MV7TRW5ITVJ?
TE-6 NUWxVJptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTN4LkOyOFYh|ryP MX7TRW5ITVJ?
MOLT-4 NGfpfHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjlZ3hKSzVyPUO2MlMzPzZizszN NFfBO29USU6JRWK=
COLO-684 NInIeIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTN5LkCxNkDPxE1? MWnTRW5ITVJ?
LU-139 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLVWldKSzVyPUO3MlE5PTZizszN M2XtVHNCVkeHUh?=
OPM-2 M162ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTN5LkK5OFkh|ryP NXfUNmVsW0GQR1XS
ML-2 NVrKNoc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTsTWM2OD1|Nz62O|EzKM7:TR?= NGnoUoFUSU6JRWK=
RS4-11 NV3oSmp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnQU5VKSzVyPUO3MlcxPjlizszN MnHCV2FPT0WU
MONO-MAC-6 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LtTmlEPTB;M{iuNlQ4PyEQvF2= M1fDfHNCVkeHUh?=
NCI-H345 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX65e4JRUUN3ME2zPE46OTB4IN88US=> M2nFR3NCVkeHUh?=
NTERA-S-cl-D1 M3LBOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XaZWlEPTB;M{muOVg1OiEQvF2= MlrxV2FPT0WU
NCI-H1882 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\vco9KSzVyPUSwMlU6QThizszN MXjTRW5ITVJ?
LC-1F M2X1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LHVGlEPTB;NEGuOVcxPSEQvF2= M3T3R3NCVkeHUh?=
HT NXfKRoxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXoOYFKSzVyPUSyMlAxOjhizszN NFTsPHRUSU6JRWK=
MLMA NHLvOVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPU[lVIUUN3ME20Nk4zPzh5IN88US=> MVXTRW5ITVJ?
DG-75 NVf0SWp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\kZmlEPTB;NEKuOlU1PiEQvF2= MmXOV2FPT0WU
GI-ME-N NU\6TZliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPSTWM2OD12Mj62OlcyKM7:TR?= NGGxemNUSU6JRWK=
MS-1 NF3XdWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jNdWlEPTB;NEKuPFk{KM7:TR?= NXu1bWQ4W0GQR1XS
CGTH-W-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrFTWM2OD12ND65Olk4KM7:TR?= NV3ONmNEW0GQR1XS
NCI-H209 Mmj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTR4LkCxNVUh|ryP NG\Q[XhUSU6JRWK=
LB2518-MEL MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTR5LkC0OFgh|ryP NWrmXm9zW0GQR1XS
DU-4475 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33q[2lEPTB;NEiuOFk{PyEQvF2= M1u4THNCVkeHUh?=
LB2241-RCC Mo\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTR6Lk[yNFIh|ryP MXLTRW5ITVJ?
LB771-HNC NVO2RW1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;TTWM2OD12OD65NlEzKM7:TR?= MknQV2FPT0WU

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: Leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, breast cancer
  • 濃度: 0.01 - 100 μM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[4]
+ 展開
  • 動物モデル: A4573 cells are injected s.c. into the right posterior flank of CD1 nu/nu mice.
  • 製剤: 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.
  • 投薬量: ≤50 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 71 mg/mL (200.31 mM)
Ethanol 6 mg/mL (16.92 mM)
Water Insoluble
体内 順序で溶剤を入れること:
1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+69% PEG 400
5mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 354.45
化学式

C19H26N6O

CAS No. 186692-46-6
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    How can I reconstitute the drug for in vivo studies?

  • 回答:

    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.

Related Antibodies

CDK信号経路図

CDK Inhibitors with Unique Features

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