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 MkflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlOxTWM2OD13Lke2NVE3KM7:TR?= MXTTRW5ITVJ?
MRK-nu-1 NUTRdm9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTdwMUK5Olkh|ryP NYewS49DW0GQR1XS
NCCIT MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nJT2lEPTB;Nz61OVQ5OiEQvF2= MULTRW5ITVJ?
JiyoyeP-2003 NHqyfmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnJcItKSzVyPUiuOVAzPjRizszN NFLOcZBUSU6JRWK=
KS-1 NWLucnQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH6ZmY6UUN3ME25MlQ2Pzh3IN88US=> NUjxVGxJW0GQR1XS
Becker NIftVJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPVdFBKSzVyPUmuOFYxQDJizszN MXfTRW5ITVJ?
KARPAS-422 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3NV5lKSzVyPUmuPVY{OzZizszN MUnTRW5ITVJ?
BB65-RCC NGXveYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUeyNpdFUUN3ME25Mlk4PDl3IN88US=> NYPMfHF{W0GQR1XS
SK-UT-1 MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr3cXZIUUN3ME2xNE4{PSEQvF2= MWnTRW5ITVJ?
ST486 M4jnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37mOmlEPTB;MUCuN|UyKM7:TR?= M1\GZnNCVkeHUh?=
LB831-BLC NX;iOnFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1O1V2lEPTB;MUGuOVYzPCEQvF2= NHjlUGdUSU6JRWK=
COR-L279 NFfCOINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTSTlBKSzVyPUGyMlI6ODdizszN NWTMZY06W0GQR1XS
NB1 NGXONlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi0XmVmUUN3ME2xNk4{OzB6IN88US=> M33FU3NCVkeHUh?=
D-247MG NFryNZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[4S2lEPTB;MUKuN|UyPiEQvF2= M3i2b3NCVkeHUh?=
697 NW\yTopPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;xfmlEPTB;MUKuOlAxPyEQvF2= NUjCVZlvW0GQR1XS
GCIY NELEVFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF{Lki2NVMh|ryP MWHTRW5ITVJ?
RPMI-8402 M3XDOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P0O2lEPTB;MUOuOlI3OiEQvF2= NXfUfpF2W0GQR1XS
Raji NV7QO2lrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPteZJKSzVyPUGzMlc5QTRizszN MYnTRW5ITVJ?
MEG-01 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT2d4luUUN3ME2xN{45Ozd7IN88US=> MWLTRW5ITVJ?
RPMI-6666 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi2dYZTUUN3ME2xN{46OTJzIN88US=> MW\TRW5ITVJ?
SCC-3 NFPGNnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3yTWM2OD1zND6yPVU3KM7:TR?= NEX4W4RUSU6JRWK=
HCC1599 M4DxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTF2LkW5O|Uh|ryP M2\Oc3NCVkeHUh?=
OCI-AML2 M3TkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjTXItEUUN3ME2xOU43PDh{IN88US=> M3Ln[HNCVkeHUh?=
OS-RC-2 M2jjbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjhSFFQUUN3ME2xOU45Ozh{IN88US=> NY\YdVRWW0GQR1XS
NCI-H1304 NEe5SItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfUelc5UUN3ME2xOk4{PjBzIN88US=> NVflc|J6W0GQR1XS
HD-MY-Z MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnneIhCUUN3ME2xOk45OjR4IN88US=> MnPZV2FPT0WU
JAR MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLYTWM2OD1zNz6wNVUzKM7:TR?= NVPId|BiW0GQR1XS
TGW MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHkfHBKSzVyPUG3MlgyOjRizszN MU\TRW5ITVJ?
BC-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTF6LkCzNFUh|ryP NWjMd25LW0GQR1XS
A101D NEKyR4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF6LkOyNFgh|ryP NVn4UXk4W0GQR1XS
COLO-320-HSR NGLMTXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljXTWM2OD1zOD63Olg5KM7:TR?= M{f2Z3NCVkeHUh?=
LC4-1 MlvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjrTWM2OD1zOD64O|M1KM7:TR?= NX7SPZRjW0GQR1XS
BC-1 MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoflTWM2OD1zOT6xNVk5KM7:TR?= MoTkV2FPT0WU
MHH-PREB-1 NFrtN|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfQU|VKSzVyPUKwMlA{PTZizszN M{\uZXNCVkeHUh?=
BL-70 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LmOGlEPTB;MkCuN|I4PCEQvF2= NH7qWYxUSU6JRWK=
CESS NYjaT5FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j5UGlEPTB;MkCuPFU1QSEQvF2= MlfuV2FPT0WU
ES8 M1XKWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[xZYlKSzVyPUKxMlA3KM7:TR?= NVSzNlNEW0GQR1XS
NOMO-1 NID4R4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzie3RKSzVyPUKxMlIxODhizszN NHjJZoNUSU6JRWK=
ACN M362e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTvNYFKSzVyPUKxMlM{QDlizszN NV3LdmVwW0GQR1XS
EB-3 MlTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NET3UFJKSzVyPUKzMlE5OzFizszN NHjNR5FUSU6JRWK=
LS-513 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPQVm5[UUN3ME2yN{42OTd7IN88US=> MUXTRW5ITVJ?
HH Mof2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnsR4x6UUN3ME2yOE4{QDF7IN88US=> M4TEVnNCVkeHUh?=
IST-SL2 NYf0TGplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPsTWM2OD1{ND61N|Q{KM7:TR?= MWXTRW5ITVJ?
HOP-62 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX5TWM2OD1{NT60OFI2KM7:TR?= MXfTRW5ITVJ?
NCI-H2126 MnziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDpTWM2OD1{NT62OVI6KM7:TR?= MlLQV2FPT0WU
BL-41 Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETqTVFKSzVyPUK1Mlk2QTdizszN MUfTRW5ITVJ?
KURAMOCHI NX;wN4RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfLbHNKSzVyPUK2MlgxQDJizszN NIWzc4pUSU6JRWK=
KARPAS-299 NXPOTlFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJ4Lki2OFYh|ryP MmrUV2FPT0WU
QIMR-WIL NH\PNmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\2Vol6UUN3ME2yO{46OTR2IN88US=> MmG0V2FPT0WU
HL-60 NEHXeIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJ5Lkm4Olkh|ryP NYjjWoJnW0GQR1XS
TE-9 NVWwT|ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLjTWM2OD1{OD63PVY6KM7:TR?= NXKzNopFW0GQR1XS
TE-8 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYCzdo1XUUN3ME2yPE46ODhizszN NYDSOY5KW0GQR1XS
NOS-1 NYHh[WtjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHUeYlKSzVyPUK4Mlk4OzNizszN NG[2VnBUSU6JRWK=
GI-1 NX;DV3V2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTJ7LkCxNVMh|ryP NYDaPGlxW0GQR1XS
KM12 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJ7Lk[yN|kh|ryP MWjTRW5ITVJ?
BB30-HNC NVf6R4tVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPUTWM2OD1{OT65OFg{KM7:TR?= M1G4WnNCVkeHUh?=
ES3 MoS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWzVWRPUUN3ME2yPU46PTh{IN88US=> M13GSXNCVkeHUh?=
NCI-H510A Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXITWM2OD1|MD6wN|I6KM7:TR?= MXHTRW5ITVJ?
NCI-H82 NUT4TYdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rW[WlEPTB;M{GuNFE{PSEQvF2= MXLTRW5ITVJ?
NCI-SNU-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13HNmlEPTB;M{GuNVA2QSEQvF2= MX\TRW5ITVJ?
NKM-1 MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrO[YdPUUN3ME2zNU4yOzl5IN88US=> MWfTRW5ITVJ?
SIG-M5 M3Lr[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITO[VZKSzVyPUOxMlY5OzNizszN NUfoXWJ5W0GQR1XS
SK-N-FI NVzldnJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTNzLke1N|Uh|ryP M1zvWHNCVkeHUh?=
LOUCY M4XvUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;oNG9KSzVyPUOyMlEzPTNizszN Mn7SV2FPT0WU
Calu-6 NFO4VXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\MSm9KSzVyPUOyMlQ4PDVizszN NEXwbYpUSU6JRWK=
GOTO NHzvfm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\TZWlEPTB;M{KuPVEzQSEQvF2= NVe2eItJW0GQR1XS
NCI-H526 NIexZ5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPrSHZwUUN3ME2zN{41QTN4IN88US=> NFLRU|FUSU6JRWK=
RKO M17WbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\nemlKSzVyPUOzMlU6PjlizszN NFXvPWFUSU6JRWK=
NCI-H64 M4mxb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzJOId3UUN3ME2zN{45PTl5IN88US=> NF:xNW5USU6JRWK=
LP-1 M1v6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLB[pdKSzVyPUOzMlg6ODhizszN NG\xOGRUSU6JRWK=
KGN NIfpd5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSwU4RoUUN3ME2zOE4zPTJ2IN88US=> NGj2TmVUSU6JRWK=
NCI-H2141 MkL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTN2Lk[1N|Mh|ryP NUn4c2ZOW0GQR1XS
TE-10 M2OxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX70NpJ7UUN3ME2zOE46PDJ{IN88US=> NYfy[2JxW0GQR1XS
K5 NGK5NlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7mUGhKSzVyPUO1MlA5PjFizszN NGjnW5JUSU6JRWK=
IMR-5 NGrQ[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjETWM2OD1|NT6zNVM6KM7:TR?= NH3ZWJBUSU6JRWK=
TE-441-T MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mki0TWM2OD1|Nj6xNVQ5KM7:TR?= MWXTRW5ITVJ?
TE-6 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDLSXBLUUN3ME2zOk4{OjR4IN88US=> MnfyV2FPT0WU
MOLT-4 NHv5WmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzSXnpKSzVyPUO2MlMzPzZizszN MWrTRW5ITVJ?
COLO-684 NUTWNVVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfBTWM2OD1|Nz6wNVIh|ryP Mkn1V2FPT0WU
LU-139 NWXKfopQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXCTWM2OD1|Nz6xPFU3KM7:TR?= MWDTRW5ITVJ?
OPM-2 NG\0ZoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;2TWM2OD1|Nz6yPVQ6KM7:TR?= MUTTRW5ITVJ?
ML-2 M1rRTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTN5Lk[3NVIh|ryP MlrkV2FPT0WU
RS4-11 NFTkTldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rmWGlEPTB;M{euO|A3QSEQvF2= NHHtVJZUSU6JRWK=
MONO-MAC-6 NHrlTVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTN6LkK0O|ch|ryP M3\tNXNCVkeHUh?=
NCI-H345 NWHMTWZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr1[3JUUUN3ME2zPE46OTB4IN88US=> NH3oZphUSU6JRWK=
NTERA-S-cl-D1 M{DJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIf5eXdKSzVyPUO5MlU5PDJizszN MmCwV2FPT0WU
NCI-H1882 NFX1bJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjvW|A1UUN3ME20NE42QTl6IN88US=> NXG4UHU6W0GQR1XS
LC-1F NELDcmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TXOWlEPTB;NEGuOVcxPSEQvF2= MoX6V2FPT0WU
HT Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rCWWlEPTB;NEKuNFAzQCEQvF2= NIGwfnZUSU6JRWK=
MLMA NFTPdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfJXHlKSzVyPUSyMlI4QDdizszN NYnKRWptW0GQR1XS
DG-75 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvITWM2OD12Mj62OVQ3KM7:TR?= NVPseHZkW0GQR1XS
GI-ME-N MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTR{Lk[2O|Eh|ryP M3TWcnNCVkeHUh?=
MS-1 MlLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTR{Lki5N{DPxE1? NWrwXo5PW0GQR1XS
CGTH-W-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LiW2lEPTB;NESuPVY6PyEQvF2= MmS1V2FPT0WU
NCI-H209 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW2UWVKSzVyPUS2MlAyOTVizszN NH:4TXVUSU6JRWK=
LB2518-MEL NFTBW4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR5LkC0OFgh|ryP M1jHZXNCVkeHUh?=
DU-4475 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i0[GlEPTB;NEiuOFk{PyEQvF2= MXXTRW5ITVJ?
LB2241-RCC NF3uW3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXaTW9TUUN3ME20PE43OjB{IN88US=> M4HD[XNCVkeHUh?=
LB771-HNC NIS3co5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLNTWM2OD12OD65NlEzKM7:TR?= NE\JU3FUSU6JRWK=

... 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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