Roscovitine (Seliciclib,CYC202)

Roscovitine (Seliciclib,CYC202)は有効な細胞週期卵白の依存性キナーゼ選択阻害剤、cdc2/ cyclin B、cdk2/ cyclin A、cdk2/ cyclin Eとcdk5/ p53に作用する時、IC50それぞれ0.65、0.7、0.7と0.16μM。

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Roscovitine (Seliciclib,CYC202) 化学構造
分子量: 354.45

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製品説明

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    CDK製品生物活性の比較
  • 研究分野
  • Roscovitine (Seliciclib,CYC202)のメカニズム

製品の説明

生物活性

製品説明 Roscovitine (Seliciclib,CYC202)は有効な細胞週期卵白の依存性キナーゼ選択阻害剤、cdc2/ cyclin B、cdk2/ cyclin A、cdk2/ cyclin Eとcdk5/ p53に作用する時、IC50それぞれ0.65、0.7、0.7と0.16μM。
ターゲット Cdc2/cyclin B CDK2/cyclin A CDK2/cyclin E CDK5/p35
IC50 0.65 μM 0.7 μM 0.7 μM 0.16 μM [1]
In vitro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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
A3-KAW M4fzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF24V4ZKSzVyPUWuO|YyOTZizszN NUjpbIZKW0GQR1XS
MRK-nu-1 NGXQSGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjXTpRSUUN3ME23MlEzQTZ7IN88US=> MlTSV2FPT0WU
NCCIT M2TSU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TEbGlEPTB;Nz61OVQ5OiEQvF2= NUDW[HQyW0GQR1XS
JiyoyeP-2003 NHXiXoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRThwNUCyOlQh|ryP NF\nSmZUSU6JRWK=
KS-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTlwNEW3PFUh|ryP MVPTRW5ITVJ?
Becker MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnjOIhKSzVyPUmuOFYxQDJizszN NYjLSG81W0GQR1XS
KARPAS-422 NE\LWFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13XdWlEPTB;OT65OlM{PiEQvF2= NWXIWppFW0GQR1XS
BB65-RCC MmqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDrWI9KSzVyPUmuPVc1QTVizszN NUDxeGk2W0GQR1XS
SK-UT-1 M{jLWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorQTWM2OD1zMD6zOUDPxE1? NYm2[3hjW0GQR1XS
ST486 NV6yRWt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nXWGlEPTB;MUCuN|UyKM7:TR?= NE\obpRUSU6JRWK=
LB831-BLC NF7NNphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHqTWM2OD1zMT61OlI1KM7:TR?= NYL1VXNwW0GQR1XS
COR-L279 NWfzeYx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvJTWM2OD1zMj6yPVA4KM7:TR?= MknEV2FPT0WU
NB1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF{LkOzNFgh|ryP MYHTRW5ITVJ?
D-247MG NFXV[plIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPXN45KSzVyPUGyMlM2OTZizszN MUnTRW5ITVJ?
697 NUjZW2VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3FPXAyUUN3ME2xNk43ODB5IN88US=> NVPnO4Q{W0GQR1XS
GCIY NHO1SG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jxPWlEPTB;MUKuPFYyOyEQvF2= MlTqV2FPT0WU
RPMI-8402 M1nibWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLYTWM2OD1zMz62NlYzKM7:TR?= M1XVbXNCVkeHUh?=
Raji MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjPe45CUUN3ME2xN{44QDl2IN88US=> NIPBd3BUSU6JRWK=
MEG-01 NVzWd3VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF|LkizO|kh|ryP NXPBTopJW0GQR1XS
RPMI-6666 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDXTWM2OD1zMz65NVIyKM7:TR?= NEXv[5VUSU6JRWK=
SCC-3 MnjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjGWZhKSzVyPUG0MlI6PTZizszN Ml;5V2FPT0WU
HCC1599 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTF2LkW5O|Uh|ryP Mmn5V2FPT0WU
OCI-AML2 MkH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD1TWM2OD1zNT62OFgzKM7:TR?= M1;4eHNCVkeHUh?=
OS-RC-2 MkPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;6TWM2OD1zNT64N|gzKM7:TR?= NY[1VnZRW0GQR1XS
NCI-H1304 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL1ZXFKSzVyPUG2MlM3ODFizszN NH71VYlUSU6JRWK=
HD-MY-Z MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrqb|hCUUN3ME2xOk45OjR4IN88US=> NInLZ5ZUSU6JRWK=
JAR MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjTVphKSzVyPUG3MlAyPTJizszN M3\veHNCVkeHUh?=
TGW NIX1SoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq5OFRKSzVyPUG3MlgyOjRizszN M4P3[nNCVkeHUh?=
BC-3 NWr0cItIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHTZpRIUUN3ME2xPE4xOzB3IN88US=> NHnvd2ZUSU6JRWK=
A101D MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPMSnFQUUN3ME2xPE4{OjB6IN88US=> NXrJTG5yW0GQR1XS
COLO-320-HSR MorPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTF6Lke2PFgh|ryP Ml3zV2FPT0WU
LC4-1 M{W1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHVW5pKSzVyPUG4Mlg4OzRizszN Mo\rV2FPT0WU
BC-1 NGTMRXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULtVGVoUUN3ME2xPU4yOTl6IN88US=> NEnwbYlUSU6JRWK=
MHH-PREB-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPmcGExUUN3ME2yNE4xOzV4IN88US=> NW\tO29FW0GQR1XS
BL-70 M2\CPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mli2TWM2OD1{MD6zNlc1KM7:TR?= NG[zcHBUSU6JRWK=
CESS NXjUb25VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDsOVZSUUN3ME2yNE45PTR7IN88US=> NUn3TpFnW0GQR1XS
ES8 NH3BfGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPkWGhuUUN3ME2yNU4xPiEQvF2= NXjtSIUxW0GQR1XS
NOMO-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTJzLkKwNFgh|ryP MV3TRW5ITVJ?
ACN NUDwWlFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DUUGlEPTB;MkGuN|M5QSEQvF2= NWqyfoNPW0GQR1XS
EB-3 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPVOXJKSzVyPUKzMlE5OzFizszN NEjEU25USU6JRWK=
LS-513 NXvsboJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[1TWM2OD1{Mz61NVc6KM7:TR?= MoXBV2FPT0WU
HH M3TS[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELqZmhKSzVyPUK0MlM5OTlizszN MWPTRW5ITVJ?
IST-SL2 Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJ2LkWzOFMh|ryP MmfrV2FPT0WU
HOP-62 NFHL[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLsSo5KSzVyPUK1MlQ1OjVizszN MXPTRW5ITVJ?
NCI-H2126 NIHYeY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPYTpZKSzVyPUK1MlY2OjlizszN MVLTRW5ITVJ?
BL-41 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDYTWM2OD1{NT65OVk4KM7:TR?= MUHTRW5ITVJ?
KURAMOCHI MmHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJ4LkiwPFIh|ryP NFLVS|RUSU6JRWK=
KARPAS-299 NFG5V5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjFUmRVUUN3ME2yOk45PjR4IN88US=> MlK2V2FPT0WU
QIMR-WIL NIn1PYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG2W|dKSzVyPUK3MlkyPDRizszN NUOx[49lW0GQR1XS
HL-60 NXTC[mN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDYTWM2OD1{Nz65PFY6KM7:TR?= MYPTRW5ITVJ?
TE-9 MnfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfTbmlWUUN3ME2yPE44QTZ7IN88US=> NW\Tb2tYW0GQR1XS
TE-8 NYXCPVgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[x[WlEPTB;MkiuPVA5KM7:TR?= NVHHS5VVW0GQR1XS
NOS-1 NF;s[Y1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH4PZNkUUN3ME2yPE46PzN|IN88US=> NXzEPFJOW0GQR1XS
GI-1 M3LhXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ7LkCxNVMh|ryP NYP6Z5I3W0GQR1XS
KM12 NILjc5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTJ7Lk[yN|kh|ryP NXvPc2doW0GQR1XS
BB30-HNC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTJ7Lkm0PFMh|ryP MX7TRW5ITVJ?
ES3 NXzWZ4hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXITm83UUN3ME2yPU46PTh{IN88US=> MXvTRW5ITVJ?
NCI-H510A M4TWVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTNyLkCzNlkh|ryP NWnhTo05W0GQR1XS
NCI-H82 M1rjcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTNzLkCxN|Uh|ryP NIS5b25USU6JRWK=
NCI-SNU-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHoTWM2OD1|MT6xNFU6KM7:TR?= MVjTRW5ITVJ?
NKM-1 MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPpTWM2OD1|MT6xN|k4KM7:TR?= NH;aNWpUSU6JRWK=
SIG-M5 NWewU4VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPrTWM2OD1|MT62PFM{KM7:TR?= MVHTRW5ITVJ?
SK-N-FI Ml;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrtTWM2OD1|MT63OVM2KM7:TR?= NVzaRWhYW0GQR1XS
LOUCY NWjsRphuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPQeG9KSzVyPUOyMlEzPTNizszN NXTZRYJiW0GQR1XS
Calu-6 NWX0NHVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XyXWlEPTB;M{KuOFc1PSEQvF2= MnvJV2FPT0WU
GOTO MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTN{LkmxNlkh|ryP MYDTRW5ITVJ?
NCI-H526 Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTN|LkS5N|Yh|ryP MnjRV2FPT0WU
RKO M{nQSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7pO2RKSzVyPUOzMlU6PjlizszN MYfTRW5ITVJ?
NCI-H64 M4fqT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLRN4NbUUN3ME2zN{45PTl5IN88US=> NXnzVGJjW0GQR1XS
LP-1 NFLqS49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXMdoRvUUN3ME2zN{45QTB6IN88US=> NGDGcHFUSU6JRWK=
KGN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly1TWM2OD1|ND6yOVI1KM7:TR?= MlzVV2FPT0WU
NCI-H2141 M3Lxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nnOWlEPTB;M{SuOlU{OyEQvF2= NX;xbVBuW0GQR1XS
TE-10 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;tNmJJUUN3ME2zOE46PDJ{IN88US=> NX7PXWZyW0GQR1XS
K5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnTNG5DUUN3ME2zOU4xQDZzIN88US=> NIKxWoZUSU6JRWK=
IMR-5 Mo\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTN3LkOxN|kh|ryP NIXQ[4xUSU6JRWK=
TE-441-T NW\UdIFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC5TWM2OD1|Nj6xNVQ5KM7:TR?= M4DyS3NCVkeHUh?=
TE-6 NIfy[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXSOmZHUUN3ME2zOk4{OjR4IN88US=> NYfLc|lpW0GQR1XS
MOLT-4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXJRW9lUUN3ME2zOk4{Ojd4IN88US=> M2DleHNCVkeHUh?=
COLO-684 M3rXSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;lTWM2OD1|Nz6wNVIh|ryP NXy4T3R7W0GQR1XS
LU-139 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTxOJZ5UUN3ME2zO{4yQDV4IN88US=> NETRb2RUSU6JRWK=
OPM-2 Mnz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fsPWlEPTB;M{euNlk1QSEQvF2= M1HmdnNCVkeHUh?=
ML-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTN5Lk[3NVIh|ryP MkLCV2FPT0WU
RS4-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLpfVFEUUN3ME2zO{44ODZ7IN88US=> MlXwV2FPT0WU
MONO-MAC-6 M3LIfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYSxZ3BPUUN3ME2zPE4zPDd5IN88US=> NX\TcVBrW0GQR1XS
NCI-H345 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLXTWM2OD1|OD65NVA3KM7:TR?= MmPJV2FPT0WU
NTERA-S-cl-D1 MoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T6PGlEPTB;M{muOVg1OiEQvF2= Ml;EV2FPT0WU
NCI-H1882 NWLEcZhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1i1[GlEPTB;NECuOVk6QCEQvF2= MUXTRW5ITVJ?
LC-1F NFPuUY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU[2NVBjUUN3ME20NU42PzB3IN88US=> Ml21V2FPT0WU
HT M4[wNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTR{LkCwNlgh|ryP M4m4UXNCVkeHUh?=
MLMA M{HpXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTR{LkK3PFch|ryP MlmyV2FPT0WU
DG-75 NYPrU2I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi0fI1KSzVyPUSyMlY2PDZizszN M3jiWXNCVkeHUh?=
GI-ME-N MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIGy[5lKSzVyPUSyMlY3PzFizszN NUmyWXI{W0GQR1XS
MS-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj0dmxKSzVyPUSyMlg6OyEQvF2= M2XQT3NCVkeHUh?=
CGTH-W-1 M3rEbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn3UHdoUUN3ME20OE46Pjl5IN88US=> NF64Z2lUSU6JRWK=
NCI-H209 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVruXGhiUUN3ME20Ok4xOTF3IN88US=> M2rMenNCVkeHUh?=
LB2518-MEL M2qxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTR5LkC0OFgh|ryP NGm1S4ZUSU6JRWK=
DU-4475 M3fsR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LLS2lEPTB;NEiuOFk{PyEQvF2= NGjnZYRUSU6JRWK=
LB2241-RCC NX;YdHQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PMWmlEPTB;NEiuOlIxOiEQvF2= MmS3V2FPT0WU
LB771-HNC M{XNZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFiwNmpKSzVyPUS4MlkzOTJizszN Mor5V2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験 Roscovitine is currently in Phase I clinical trial in patients with advanced solid tumors.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

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.

動物実験: [4]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Roscovitine (Seliciclib,CYC202) SDF
分子量 354.45
化学式

C19H26N6O

CAS No. 186692-46-6
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (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.
化学名 (R)-2-(6-(benzylamino)-9-isopropyl-9H-purin-2-ylamino)butan-1-ol

文献中の引用 (9)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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