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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Quality Control & MSDS

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 M4jZfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXiXJM5UUN3ME21Mlc3OTF4IN88US=> MkL1V2FPT0WU
MRK-nu-1 M1jRU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\iWW5PUUN3ME23MlEzQTZ7IN88US=> M3;UdnNCVkeHUh?=
NCCIT M4PGRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:2XWlEPTB;Nz61OVQ5OiEQvF2= NXH6eJI1W0GQR1XS
JiyoyeP-2003 NHfaSJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPTUnpsUUN3ME24MlUxOjZ2IN88US=> MXzTRW5ITVJ?
KS-1 NECxUYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCweoluUUN3ME25MlQ2Pzh3IN88US=> NVXyN5dmW0GQR1XS
Becker NIrWUVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe1bWRKSzVyPUmuOFYxQDJizszN MoC1V2FPT0WU
KARPAS-422 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonOTWM2OD17Lkm2N|M3KM7:TR?= NW\s[XBvW0GQR1XS
BB65-RCC MnjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTlwOUe0PVUh|ryP NELKfHdUSU6JRWK=
SK-UT-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFyLkO1JO69VQ>? MWnTRW5ITVJ?
ST486 NU\qXmFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFyLkO1NUDPxE1? NXPoUHBlW0GQR1XS
LB831-BLC M17nNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXvN41YUUN3ME2xNU42PjJ2IN88US=> M1r1V3NCVkeHUh?=
COR-L279 NIXXfnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml6zTWM2OD1zMj6yPVA4KM7:TR?= NFq0ZnlUSU6JRWK=
NB1 NETUSHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfPc|dKSzVyPUGyMlM{ODhizszN NIfLT2ZUSU6JRWK=
D-247MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXKU3JKSzVyPUGyMlM2OTZizszN MojnV2FPT0WU
697 M3r6SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTF{Lk[wNFch|ryP MVTTRW5ITVJ?
GCIY NEXxRYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF{Lki2NVMh|ryP NIXpT5FUSU6JRWK=
RPMI-8402 NEDQbHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XJVGlEPTB;MUOuOlI3OiEQvF2= NEnGWVhUSU6JRWK=
Raji NUjubppRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoWyTWM2OD1zMz63PFk1KM7:TR?= NH:2cG9USU6JRWK=
MEG-01 MorJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvuTWM2OD1zMz64N|c6KM7:TR?= MkTDV2FPT0WU
RPMI-6666 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF|LkmxNlEh|ryP Mle2V2FPT0WU
SCC-3 M1jHVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrTSWU5UUN3ME2xOE4zQTV4IN88US=> NWfpW4tbW0GQR1XS
HCC1599 M13wdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF2LkW5O|Uh|ryP NEXTenNUSU6JRWK=
OCI-AML2 M1zic2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDOTWM2OD1zNT62OFgzKM7:TR?= MnrZV2FPT0WU
OS-RC-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF3LkizPFIh|ryP MVLTRW5ITVJ?
NCI-H1304 NH[1dpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHCN5RKUUN3ME2xOk4{PjBzIN88US=> NGXNPIhUSU6JRWK=
HD-MY-Z NV7yfnByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTF4LkiyOFYh|ryP NH;Y[JJUSU6JRWK=
JAR MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi4b4tKSzVyPUG3MlAyPTJizszN MUDTRW5ITVJ?
TGW MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTF5LkixNlQh|ryP NYHGWpBRW0GQR1XS
BC-3 MoruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{GxdGlEPTB;MUiuNFMxPSEQvF2= NFj2VnFUSU6JRWK=
A101D NH\rT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSwT3BMUUN3ME2xPE4{OjB6IN88US=> NXyyXJFzW0GQR1XS
COLO-320-HSR NHrodmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX25Ro0{UUN3ME2xPE44Pjh6IN88US=> NV3KUmpFW0GQR1XS
LC4-1 MlrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTV[VNPUUN3ME2xPE45PzN2IN88US=> M33iW3NCVkeHUh?=
BC-1 M1nIdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGmxPYxKSzVyPUG5MlEyQThizszN MnSzV2FPT0WU
MHH-PREB-1 M{jyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L4SGlEPTB;MkCuNFM2PiEQvF2= NGLU[ZhUSU6JRWK=
BL-70 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnsbJVJUUN3ME2yNE4{Ojd2IN88US=> MmjVV2FPT0WU
CESS MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fvcmlEPTB;MkCuPFU1QSEQvF2= MkXDV2FPT0WU
ES8 NHXreGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr4SGtOUUN3ME2yNU4xPiEQvF2= MmDvV2FPT0WU
NOMO-1 NYTkSVVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPjTWM2OD1{MT6yNFA5KM7:TR?= NXfTcmp5W0GQR1XS
ACN NFLpbFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\QUHRrUUN3ME2yNU4{Ozh7IN88US=> MmizV2FPT0WU
EB-3 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XySGlEPTB;MkOuNVg{OSEQvF2= NW\SZ5JMW0GQR1XS
LS-513 NXPQR4RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfQV2hKUUN3ME2yN{42OTd7IN88US=> NHvrSHJUSU6JRWK=
HH NFPXc3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDYUIxGUUN3ME2yOE4{QDF7IN88US=> MYfTRW5ITVJ?
IST-SL2 M3y2W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEWyO2pKSzVyPUK0MlU{PDNizszN Mly0V2FPT0WU
HOP-62 NIfhTWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PGeGlEPTB;MkWuOFQzPSEQvF2= MWDTRW5ITVJ?
NCI-H2126 NXvOcXJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1WyeWlEPTB;MkWuOlUzQSEQvF2= M3z2enNCVkeHUh?=
BL-41 MkSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zsWmlEPTB;MkWuPVU6PyEQvF2= MV7TRW5ITVJ?
KURAMOCHI M1\NSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfvbHpKSzVyPUK2MlgxQDJizszN NIHoNJpUSU6JRWK=
KARPAS-299 M3\1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H3emlEPTB;Mk[uPFY1PiEQvF2= NE\PZVNUSU6JRWK=
QIMR-WIL NU\ybok5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJ5LkmxOFQh|ryP NH3Ue4hUSU6JRWK=
HL-60 Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4W2NWlEPTB;MkeuPVg3QSEQvF2= NXS3cVlXW0GQR1XS
TE-9 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG1XXUyUUN3ME2yPE44QTZ7IN88US=> MnjLV2FPT0WU
TE-8 NYHkbJk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nwT2lEPTB;MkiuPVA5KM7:TR?= MXPTRW5ITVJ?
NOS-1 MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTJ6Lkm3N|Mh|ryP MYPTRW5ITVJ?
GI-1 NEfsZXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjsSZhKSzVyPUK5MlAyOTNizszN M1zNZXNCVkeHUh?=
KM12 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnXTWM2OD1{OT62NlM6KM7:TR?= NVzsS2NEW0GQR1XS
BB30-HNC MknvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEToXo5KSzVyPUK5Mlk1QDNizszN MmXOV2FPT0WU
ES3 M4G0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\rZplKSzVyPUK5Mlk2QDJizszN MkHlV2FPT0WU
NCI-H510A M4ftWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HEO2lEPTB;M{CuNFMzQSEQvF2= MXvTRW5ITVJ?
NCI-H82 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPYT|dKSzVyPUOxMlAyOzVizszN MoDYV2FPT0WU
NCI-SNU-1 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjBVmpKSzVyPUOxMlExPTlizszN M37UT3NCVkeHUh?=
NKM-1 M{Hlc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDlTWM2OD1|MT6xN|k4KM7:TR?= MmS0V2FPT0WU
SIG-M5 M1\XRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPyTWM2OD1|MT62PFM{KM7:TR?= M2judHNCVkeHUh?=
SK-N-FI MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEi5b|NKSzVyPUOxMlc2OzVizszN NX\xNWlXW0GQR1XS
LOUCY MmHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fMdGlEPTB;M{KuNVI2OyEQvF2= NY\LfY9XW0GQR1XS
Calu-6 NF;XZoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LheWlEPTB;M{KuOFc1PSEQvF2= M1G5TnNCVkeHUh?=
GOTO M3LjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTN{LkmxNlkh|ryP Mlj5V2FPT0WU
NCI-H526 NWW3WVhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrG[oRKSzVyPUOzMlQ6OzZizszN NVXWeJFqW0GQR1XS
RKO NFribYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4THemlEPTB;M{OuOVk3QSEQvF2= NH3UVZdUSU6JRWK=
NCI-H64 NYTReoNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkeyTWM2OD1|Mz64OVk4KM7:TR?= M3fk[XNCVkeHUh?=
LP-1 NF60S4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfGO|ZKSzVyPUOzMlg6ODhizszN M3LVTXNCVkeHUh?=
KGN Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN2LkK1NlQh|ryP NFzkRohUSU6JRWK=
NCI-H2141 NFrScIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nTb2lEPTB;M{SuOlU{OyEQvF2= MkW0V2FPT0WU
TE-10 MlHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7nTWM2OD1|ND65OFIzKM7:TR?= NGDCeolUSU6JRWK=
K5 M3;zUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jpdGlEPTB;M{WuNFg3OSEQvF2= M1vme3NCVkeHUh?=
IMR-5 M{jweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXNeI1QUUN3ME2zOU4{OTN7IN88US=> M2fnfXNCVkeHUh?=
TE-441-T M4TOZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\iWZFnUUN3ME2zOk4yOTR6IN88US=> NYDEbYRJW0GQR1XS
TE-6 M2L3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTN4LkOyOFYh|ryP NWPxRnlJW0GQR1XS
MOLT-4 M3;Vemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDZSFBKSzVyPUO2MlMzPzZizszN MlewV2FPT0WU
COLO-684 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXxT|FqUUN3ME2zO{4xOTJizszN NInvU2hUSU6JRWK=
LU-139 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrXTWM2OD1|Nz6xPFU3KM7:TR?= MULTRW5ITVJ?
OPM-2 M2fZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTN5LkK5OFkh|ryP NX;yfml7W0GQR1XS
ML-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrRbI5KSzVyPUO3MlY4OTJizszN MWHTRW5ITVJ?
RS4-11 NGrDbmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\r[5psUUN3ME2zO{44ODZ7IN88US=> Mn;JV2FPT0WU
MONO-MAC-6 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTN6LkK0O|ch|ryP NFvnW3RUSU6JRWK=
NCI-H345 MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTN6LkmxNFYh|ryP MmPaV2FPT0WU
NTERA-S-cl-D1 MmfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\BUmlEPTB;M{muOVg1OiEQvF2= MYfTRW5ITVJ?
NCI-H1882 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrTeos3UUN3ME20NE42QTl6IN88US=> NG\JeZhUSU6JRWK=
LC-1F MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Ll[GlEPTB;NEGuOVcxPSEQvF2= M13WOnNCVkeHUh?=
HT NF[ycmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTR{LkCwNlgh|ryP M2X3enNCVkeHUh?=
MLMA NHLucHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTR{LkK3PFch|ryP MXrTRW5ITVJ?
DG-75 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPXSFdKSzVyPUSyMlY2PDZizszN MlPpV2FPT0WU
GI-ME-N NHfVZ4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LwSGlEPTB;NEKuOlY4OSEQvF2= NX\BU2NqW0GQR1XS
MS-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnuyTWM2OD12Mj64PVMh|ryP MoXsV2FPT0WU
CGTH-W-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGH3NWdKSzVyPUS0Mlk3QTdizszN Ml7kV2FPT0WU
NCI-H209 NGTubWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfKfHM{UUN3ME20Ok4xOTF3IN88US=> NVLrbXpyW0GQR1XS
LB2518-MEL NVzBeGJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXPU4J2UUN3ME20O{4xPDR6IN88US=> Ml73V2FPT0WU
DU-4475 M2X6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTwTWM2OD12OD60PVM4KM7:TR?= NWLlfpc6W0GQR1XS
LB2241-RCC Mme0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUH5bWx{UUN3ME20PE43OjB{IN88US=> NHXzNZFUSU6JRWK=
LB771-HNC M2r0NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTR6LkmyNVIh|ryP MnyyV2FPT0WU

... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 71 mg/mL (200.31 mM)
エタノール 6 mg/mL (16.92 mM)
<1 mg/mL (<1 mM)
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

カスタマーフィードバック (4)


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Source PNAS, 2011, 108, 8417. Roscovitine (Seliciclib,CYC202) purchased from Selleck
Method Western blotting, Wst-1 proliferation assay, radioimmunoassays
Cell Lines AtT20 cells
Concentrations 0-20 µM
Incubation Time 24/48 h
Results Treatment with R-roscovitine led to decreased cell number by 24 h (Fig. A). Western blot analysis of protein extracts derived from R-roscovitine-treated cells revealed evidence for cell cycle arrest, including decreased cyclin E, increased p27Kip1, p57Kip2, and p21Cip1 expression, as well as reduced Thr821 phosphorylation of Rb (Fig. B). R-roscovitine treatment also induced senescent features by 48 h as evidenced by increased β -gal expression (Fig. C). Consistent with decreased cell viability, we detected decreased ACTH concentrations in culture medium derived from R-roscovitine-treated AtT20 cells (Fig. D). Western blot analysis of protein extracts derived from R-roscovitine-treated AtT20 cells showed suppressed ACTH expression (Fig. E). These results indicate that R-roscovitine targets cdk2/cyclin E-mediated cell cycle progression, and also inhibits corticotroph ACTH protein expression.

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Source PNAS, 2011, 108, 8417. Roscovitine (Seliciclib,CYC202) purchased from Selleck
Method Western blotting, Fluorescent Microscopy, Confocal Imaging
Cell Lines Tumor xenografts
Concentrations 150 mg/kg
Incubation Time 15 d
Results R-roscovitine caused approximately 50% weight reduction of dissected tumor xenografts(Fig. A). Consistent with the in vitro observations, Western blot and immunohistochemistry analysis of tumor specimens showed suppressed ACTH and PCNA protein expression by R-roscovitine (Fig. B and C). R-roscovitine-treated mice exhibited more than 50% reduction in plasma ACTH levels ), and approximately 50% reduction in serum corticosterone levels.

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Source J Hematol Oncol, 2012, 7, 53. Roscovitine (Seliciclib,CYC202) purchased from Selleck
Method Western Blot/immunofluoresence
Cell Lines Isolated granular neurons
Concentrations 20 uM
Incubation Time 24 h
Results Application of roscovitine significantly suppressed T288 phosphorylation of Aurora-A associated with reduction of S251 phosphorylation of NDEL1, which was confirmed by Western blotting and immunocytochemistry.

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Source University of Hong Kong. Roscovitine (Seliciclib,CYC202) purchased from Selleck
Method Oil-Red-O/SA-β-gal staining
Cell Lines ApoE-/- mice
Concentrations
Incubation Time 18 weeks
Results Chronic treatment with roscovitine attenuates the development of atherosclerosis in ApoE-/- mice.

文献中の引用 (8)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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