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 MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrZTVVKSzVyPUWuO|YyOTZizszN MVXTRW5ITVJ?
MRK-nu-1 NG\MTllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\2TWM2OD15LkGyPVY6KM7:TR?= NHXIZmhUSU6JRWK=
NCCIT MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTdwNUW0PFIh|ryP NEPPN5dUSU6JRWK=
JiyoyeP-2003 NIXiW21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRThwNUCyOlQh|ryP NGHK[JZUSU6JRWK=
KS-1 NWjMWmhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjTTWM2OD17LkS1O|g2KM7:TR?= M3TtdHNCVkeHUh?=
Becker NGe5SpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnBTnVNUUN3ME25MlQ3ODh{IN88US=> M1j5VnNCVkeHUh?=
KARPAS-422 NUTnUYpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\mPGJKSzVyPUmuPVY{OzZizszN Mn7WV2FPT0WU
BB65-RCC M{jve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\uTWM2OD17Lkm3OFk2KM7:TR?= MmTsV2FPT0WU
SK-UT-1 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX2TWM2OD1zMD6zOUDPxE1? NWflUmJ1W0GQR1XS
ST486 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LI[mlEPTB;MUCuN|UyKM7:TR?= NWOxe|hNW0GQR1XS
LB831-BLC M1yyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;6WWZKSzVyPUGxMlU3OjRizszN M4\od3NCVkeHUh?=
COR-L279 MkT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fYdmlEPTB;MUKuNlkxPyEQvF2= M1[yO3NCVkeHUh?=
NB1 NWDZ[WM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF{LkOzNFgh|ryP NWS2Xo06W0GQR1XS
D-247MG NV3uOJdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXSWm1qUUN3ME2xNk4{PTF4IN88US=> MYTTRW5ITVJ?
697 NWm3NVZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTF{Lk[wNFch|ryP NGTDSm1USU6JRWK=
GCIY NUj1Xm1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInIXHlKSzVyPUGyMlg3OTNizszN MnfhV2FPT0WU
RPMI-8402 NVfrco5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrhfVhKSzVyPUGzMlYzPjJizszN NXzmZXI6W0GQR1XS
Raji MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvuSm9KSzVyPUGzMlc5QTRizszN NWHyb25OW0GQR1XS
MEG-01 Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\NTmJKSzVyPUGzMlg{PzlizszN NGXnbY1USU6JRWK=
RPMI-6666 NVrXZZR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTF|LkmxNlEh|ryP M3XBfXNCVkeHUh?=
SCC-3 MmrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonPTWM2OD1zND6yPVU3KM7:TR?= M{XXU3NCVkeHUh?=
HCC1599 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj4[GVKSzVyPUG0MlU6PzVizszN NFLNPXlUSU6JRWK=
OCI-AML2 M3rIbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnzT4ZKUUN3ME2xOU43PDh{IN88US=> NI\sN|dUSU6JRWK=
OS-RC-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TPS2lEPTB;MUWuPFM5OiEQvF2= M3X5d3NCVkeHUh?=
NCI-H1304 NVXVXnNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFG4e4xKSzVyPUG2MlM3ODFizszN MWrTRW5ITVJ?
HD-MY-Z M2HLUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnG3TWM2OD1zNj64NlQ3KM7:TR?= NXn2O|d7W0GQR1XS
JAR NVHE[JV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnRTWM2OD1zNz6wNVUzKM7:TR?= MXHTRW5ITVJ?
TGW M3zobWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\xOWlEPTB;MUeuPFEzPCEQvF2= MWTTRW5ITVJ?
BC-3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrhdlVrUUN3ME2xPE4xOzB3IN88US=> M3\3eHNCVkeHUh?=
A101D MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWO1S29GUUN3ME2xPE4{OjB6IN88US=> NHHOV|BUSU6JRWK=
COLO-320-HSR MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXrTWM2OD1zOD63Olg5KM7:TR?= NWXxUopbW0GQR1XS
LC4-1 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPzTWM2OD1zOD64O|M1KM7:TR?= NVTjfGNKW0GQR1XS
BC-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFe2TItKSzVyPUG5MlEyQThizszN MkWxV2FPT0WU
MHH-PREB-1 MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX4dWE3UUN3ME2yNE4xOzV4IN88US=> NFO3UmpUSU6JRWK=
BL-70 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJyLkOyO|Qh|ryP MVHTRW5ITVJ?
CESS MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfYVppKSzVyPUKwMlg2PDlizszN NHjJUHdUSU6JRWK=
ES8 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vvd2lEPTB;MkGuNFYh|ryP NXzuV2NNW0GQR1XS
NOMO-1 M131O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDDfoxKSzVyPUKxMlIxODhizszN M1vEcHNCVkeHUh?=
ACN NWf0bW9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPsTWM2OD1{MT6zN|g6KM7:TR?= NFTPN4VUSU6JRWK=
EB-3 NG\l[WJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13JPGlEPTB;MkOuNVg{OSEQvF2= MmnwV2FPT0WU
LS-513 M1HNUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XZR2lEPTB;MkOuOVE4QSEQvF2= M1PiNnNCVkeHUh?=
HH NUDBc4JHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTJ2LkO4NVkh|ryP NYS3W|V7W0GQR1XS
IST-SL2 Mk\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1uyfWlEPTB;MkSuOVM1OyEQvF2= NULSO5dvW0GQR1XS
HOP-62 M{LZfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TVcWlEPTB;MkWuOFQzPSEQvF2= M1P2OnNCVkeHUh?=
NCI-H2126 NEHQNmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETQVnhKSzVyPUK1MlY2OjlizszN NWL2b2ZbW0GQR1XS
BL-41 M32wSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX6cJdKSzVyPUK1Mlk2QTdizszN MoDyV2FPT0WU
KURAMOCHI NWLhSlNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfmNo84UUN3ME2yOk45ODh{IN88US=> Mm\5V2FPT0WU
KARPAS-299 NHy2[mRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzWeFNKSzVyPUK2Mlg3PDZizszN NEn6Wm5USU6JRWK=
QIMR-WIL M4fhSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFm4coFKSzVyPUK3MlkyPDRizszN M4X5UXNCVkeHUh?=
HL-60 NXz6d4xOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\xXGlEPTB;MkeuPVg3QSEQvF2= MUfTRW5ITVJ?
TE-9 Ml3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHSSoZKSzVyPUK4Mlc6PjlizszN Mmi0V2FPT0WU
TE-8 M4LQSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jQdWlEPTB;MkiuPVA5KM7:TR?= NX[zNnNCW0GQR1XS
NOS-1 NXLNUZBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjEZ2lKSzVyPUK4Mlk4OzNizszN MV\TRW5ITVJ?
GI-1 NUTJOZFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUe0SWt{UUN3ME2yPU4xOTF|IN88US=> M3;CVnNCVkeHUh?=
KM12 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDSOVhXUUN3ME2yPU43OjN7IN88US=> MoD1V2FPT0WU
BB30-HNC M3nuemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJ7Lkm0PFMh|ryP MX3TRW5ITVJ?
ES3 M{jQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDYV3VKSzVyPUK5Mlk2QDJizszN MoDHV2FPT0WU
NCI-H510A NYD2SGJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfzN4w5UUN3ME2zNE4xOzJ7IN88US=> M37lRXNCVkeHUh?=
NCI-H82 NIniSXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Lx[mlEPTB;M{GuNFE{PSEQvF2= NGfaUWpUSU6JRWK=
NCI-SNU-1 NXLHbG56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\CdlI6UUN3ME2zNU4yODV7IN88US=> NXrTRVFtW0GQR1XS
NKM-1 M1rwcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnSwTWM2OD1|MT6xN|k4KM7:TR?= NGLOWm5USU6JRWK=
SIG-M5 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTNzLk[4N|Mh|ryP NH:wSlNUSU6JRWK=
SK-N-FI NIm0e3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXPTWM2OD1|MT63OVM2KM7:TR?= M1y1PXNCVkeHUh?=
LOUCY MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTN{LkGyOVMh|ryP MWHTRW5ITVJ?
Calu-6 M{ji[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfVTWM2OD1|Mj60O|Q2KM7:TR?= NETXSVJUSU6JRWK=
GOTO M3TOUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTN{LkmxNlkh|ryP M2LIXHNCVkeHUh?=
NCI-H526 M1XwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DZR2lEPTB;M{OuOFk{PiEQvF2= M4DJNHNCVkeHUh?=
RKO M3T3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTN|LkW5Olkh|ryP Mk\LV2FPT0WU
NCI-H64 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPzfINKSzVyPUOzMlg2QTdizszN M37GTXNCVkeHUh?=
LP-1 NXHaclBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nlOWlEPTB;M{OuPFkxQCEQvF2= MXfTRW5ITVJ?
KGN M1XTbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTN2LkK1NlQh|ryP MlvkV2FPT0WU
NCI-H2141 NHLmfZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDPTWM2OD1|ND62OVM{KM7:TR?= NGPC[FdUSU6JRWK=
TE-10 NFrv[phIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT5TWM2OD1|ND65OFIzKM7:TR?= NIjTWmxUSU6JRWK=
K5 M1TlN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHSN2dKSzVyPUO1MlA5PjFizszN NX22TIg3W0GQR1XS
IMR-5 NFziNlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTN3LkOxN|kh|ryP M3TCSnNCVkeHUh?=
TE-441-T NHfZSJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTsTGl2UUN3ME2zOk4yOTR6IN88US=> NW\KWY8xW0GQR1XS
TE-6 M1rKbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LiWGlEPTB;M{[uN|I1PiEQvF2= M4rMd3NCVkeHUh?=
MOLT-4 NIrnPXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfuTFRKSzVyPUO2MlMzPzZizszN NUTzbGt2W0GQR1XS
COLO-684 NVvue|ZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvtTWM2OD1|Nz6wNVIh|ryP NHrxU3FUSU6JRWK=
LU-139 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XKd2lEPTB;M{euNVg2PiEQvF2= NETjfIJUSU6JRWK=
OPM-2 M3nhR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTN5LkK5OFkh|ryP NHzQU3pUSU6JRWK=
ML-2 M3TJUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjINIhKSzVyPUO3MlY4OTJizszN NGjMc3hUSU6JRWK=
RS4-11 MmLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULacnV7UUN3ME2zO{44ODZ7IN88US=> MYDTRW5ITVJ?
MONO-MAC-6 NWPGcI1mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\YTWM2OD1|OD6yOFc4KM7:TR?= M1voenNCVkeHUh?=
NCI-H345 M2TjSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe1fGFoUUN3ME2zPE46OTB4IN88US=> NHP5TGxUSU6JRWK=
NTERA-S-cl-D1 NFzKRW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTlVIpiUUN3ME2zPU42QDR{IN88US=> NHTMWXFUSU6JRWK=
NCI-H1882 M3LFdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\Bdo4zUUN3ME20NE42QTl6IN88US=> NV3GPIF5W0GQR1XS
LC-1F NVTLUpJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTGc3J3UUN3ME20NU42PzB3IN88US=> MUPTRW5ITVJ?
HT MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzNTFk2UUN3ME20Nk4xODJ6IN88US=> NFzhWmJUSU6JRWK=
MLMA MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\KV|JXUUN3ME20Nk4zPzh5IN88US=> Ml3wV2FPT0WU
DG-75 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TkXGlEPTB;NEKuOlU1PiEQvF2= MonaV2FPT0WU
GI-ME-N NXy0UmJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPjTWM2OD12Mj62OlcyKM7:TR?= NXv5NIpiW0GQR1XS
MS-1 MojmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTR{Lki5N{DPxE1? NIK1O|BUSU6JRWK=
CGTH-W-1 M1XyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWf3cnFZUUN3ME20OE46Pjl5IN88US=> M3X0XHNCVkeHUh?=
NCI-H209 M3nwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTR4LkCxNVUh|ryP NXjGXpVFW0GQR1XS
LB2518-MEL MnLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[5dZVKSzVyPUS3MlA1PDhizszN M17kVHNCVkeHUh?=
DU-4475 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvlcZN6UUN3ME20PE41QTN5IN88US=> M{\oVXNCVkeHUh?=
LB2241-RCC MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjBcVFKSzVyPUS4MlYzODJizszN MlLvV2FPT0WU
LB771-HNC MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrvXXROUUN3ME20PE46OjF{IN88US=> NEfqbFhUSU6JRWK=

... 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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