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 NH3OZlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfCTFdKSzVyPUWuO|YyOTZizszN NETJN5JUSU6JRWK=
MRK-nu-1 NHPz[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETDSWxKSzVyPUeuNVI6PjlizszN MWrTRW5ITVJ?
NCCIT MljRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH1No1KSzVyPUeuOVU1QDJizszN MmXaV2FPT0WU
JiyoyeP-2003 NIfD[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[xUWlEPTB;OD61NFI3PCEQvF2= NUHBWoVvW0GQR1XS
KS-1 MkmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH62TnNKSzVyPUmuOFU4QDVizszN MmmxV2FPT0WU
Becker NEDaUoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf2NZpKSzVyPUmuOFYxQDJizszN NXHpWJAxW0GQR1XS
KARPAS-422 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXINGtKSzVyPUmuPVY{OzZizszN MoL3V2FPT0WU
BB65-RCC NXOzZYlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTlwOUe0PVUh|ryP NEjRUHpUSU6JRWK=
SK-UT-1 MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVziS2ZkUUN3ME2xNE4{PSEQvF2= MXrTRW5ITVJ?
ST486 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzjVIRoUUN3ME2xNE4{PTFizszN NWCwZWwxW0GQR1XS
LB831-BLC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLOTWM2OD1zMT61OlI1KM7:TR?= M2HYTHNCVkeHUh?=
COR-L279 NGL1T21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTF{LkK5NFch|ryP NGPxS4lUSU6JRWK=
NB1 NUTvcIV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTF{LkOzNFgh|ryP MlyzV2FPT0WU
D-247MG NIfiOXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjVPWlKSzVyPUGyMlM2OTZizszN NX3ROo5TW0GQR1XS
697 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Lv[2lEPTB;MUKuOlAxPyEQvF2= MW\TRW5ITVJ?
GCIY NGHDRZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlKxTWM2OD1zMj64OlE{KM7:TR?= NVvL[5l3W0GQR1XS
RPMI-8402 MlviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1i5bWlEPTB;MUOuOlI3OiEQvF2= NHvCUmhUSU6JRWK=
Raji MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXj4eodsUUN3ME2xN{44QDl2IN88US=> MUPTRW5ITVJ?
MEG-01 NXXiZ5lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnuboFvUUN3ME2xN{45Ozd7IN88US=> NYP2fXY4W0GQR1XS
RPMI-6666 M33PdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDvOnExUUN3ME2xN{46OTJzIN88US=> MVLTRW5ITVJ?
SCC-3 Mlz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF2LkK5OVYh|ryP NVPrU4RJW0GQR1XS
HCC1599 M13MT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrlTWM2OD1zND61PVc2KM7:TR?= NVnLUm0xW0GQR1XS
OCI-AML2 NH;5SZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vNNWlEPTB;MUWuOlQ5OiEQvF2= MWfTRW5ITVJ?
OS-RC-2 NHSwN2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K3R2lEPTB;MUWuPFM5OiEQvF2= NUfUWpA1W0GQR1XS
NCI-H1304 NIjHUXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF4LkO2NFEh|ryP MXnTRW5ITVJ?
HD-MY-Z M{nmVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\NTWM2OD1zNj64NlQ3KM7:TR?= NGftWFJUSU6JRWK=
JAR Mn;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGewb2tKSzVyPUG3MlAyPTJizszN MYrTRW5ITVJ?
TGW MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r3V2lEPTB;MUeuPFEzPCEQvF2= M1O2VHNCVkeHUh?=
BC-3 MofnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\JWmlEPTB;MUiuNFMxPSEQvF2= NHfBSG1USU6JRWK=
A101D MnjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF6LkOyNFgh|ryP MUDTRW5ITVJ?
COLO-320-HSR Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3EVFlJUUN3ME2xPE44Pjh6IN88US=> NYPzdFZmW0GQR1XS
LC4-1 NEXkXIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF6Lki3N|Qh|ryP MXzTRW5ITVJ?
BC-1 MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTF7LkGxPVgh|ryP MmrYV2FPT0WU
MHH-PREB-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr5TWM2OD1{MD6wN|U3KM7:TR?= MkfyV2FPT0WU
BL-70 M3XUNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jNWWlEPTB;MkCuN|I4PCEQvF2= NXfmRmtZW0GQR1XS
CESS MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHMUZlKSzVyPUKwMlg2PDlizszN M4DT[3NCVkeHUh?=
ES8 NFTTVHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOyTWM2OD1{MT6wOkDPxE1? MorGV2FPT0WU
NOMO-1 NG\IfmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJzLkKwNFgh|ryP M1L0fXNCVkeHUh?=
ACN M17zbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17BU2lEPTB;MkGuN|M5QSEQvF2= NH7BZW1USU6JRWK=
EB-3 NFPyWGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPFS3BFUUN3ME2yN{4yQDNzIN88US=> M2\QfHNCVkeHUh?=
LS-513 M1HEWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS5TWM2OD1{Mz61NVc6KM7:TR?= MoX3V2FPT0WU
HH M1\kXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJ2LkO4NVkh|ryP MUPTRW5ITVJ?
IST-SL2 M37sR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1yyXWlEPTB;MkSuOVM1OyEQvF2= NHS5[2NUSU6JRWK=
HOP-62 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHOSY9lUUN3ME2yOU41PDJ3IN88US=> M2TlVHNCVkeHUh?=
NCI-H2126 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L6RmlEPTB;MkWuOlUzQSEQvF2= M{O1b3NCVkeHUh?=
BL-41 NYnDeXZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPSWpUxUUN3ME2yOU46PTl5IN88US=> Mn\GV2FPT0WU
KURAMOCHI MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXYbWtKSzVyPUK2MlgxQDJizszN M3zCbHNCVkeHUh?=
KARPAS-299 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq4TWM2OD1{Nj64OlQ3KM7:TR?= MVLTRW5ITVJ?
QIMR-WIL NWPwd216T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH73NJJKSzVyPUK3MlkyPDRizszN MXXTRW5ITVJ?
HL-60 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHuTYVrUUN3ME2yO{46QDZ7IN88US=> NYfldlF7W0GQR1XS
TE-9 NEjFRXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHoTWM2OD1{OD63PVY6KM7:TR?= MVPTRW5ITVJ?
TE-8 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHwZ3FKSzVyPUK4MlkxQCEQvF2= NV3rOI5QW0GQR1XS
NOS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7SZ5ZKSzVyPUK4Mlk4OzNizszN NFr1XphUSU6JRWK=
GI-1 M17WeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf4[GJKSzVyPUK5MlAyOTNizszN MW\TRW5ITVJ?
KM12 MljqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD5TWM2OD1{OT62NlM6KM7:TR?= M33kbHNCVkeHUh?=
BB30-HNC MkezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknzTWM2OD1{OT65OFg{KM7:TR?= NUKzSmJpW0GQR1XS
ES3 M4j2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonDTWM2OD1{OT65OVgzKM7:TR?= MU\TRW5ITVJ?
NCI-H510A Mlu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvTTWM2OD1|MD6wN|I6KM7:TR?= NXq3dnNOW0GQR1XS
NCI-H82 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPobWFKSzVyPUOxMlAyOzVizszN M2G4UnNCVkeHUh?=
NCI-SNU-1 NUPKW4NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\tfIF[UUN3ME2zNU4yODV7IN88US=> NGXIeWFUSU6JRWK=
NKM-1 NYLlPXpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXqT21FUUN3ME2zNU4yOzl5IN88US=> NUfBPJU4W0GQR1XS
SIG-M5 MkHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEGzNmRKSzVyPUOxMlY5OzNizszN MXTTRW5ITVJ?
SK-N-FI NF3QOm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTNzLke1N|Uh|ryP NXvEd5h{W0GQR1XS
LOUCY M1fZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zV[2lEPTB;M{KuNVI2OyEQvF2= NYfKbFNlW0GQR1XS
Calu-6 MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3kcFdKSzVyPUOyMlQ4PDVizszN NUXU[|lsW0GQR1XS
GOTO MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjZTFdKSzVyPUOyMlkyOjlizszN M3XmT3NCVkeHUh?=
NCI-H526 M{DrXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkm4TWM2OD1|Mz60PVM3KM7:TR?= MYjTRW5ITVJ?
RKO MmTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTN|LkW5Olkh|ryP NGradIVUSU6JRWK=
NCI-H64 NH3uPZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj0dmZKSzVyPUOzMlg2QTdizszN NHTSPJFUSU6JRWK=
LP-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrZc3VKSzVyPUOzMlg6ODhizszN MVHTRW5ITVJ?
KGN NEmyXIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITIVFZKSzVyPUO0MlI2OjRizszN NXzLXmRCW0GQR1XS
NCI-H2141 MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUm4TGVHUUN3ME2zOE43PTN|IN88US=> MUjTRW5ITVJ?
TE-10 NVTlN3psT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojYTWM2OD1|ND65OFIzKM7:TR?= MXLTRW5ITVJ?
K5 NG\sXXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u4N2lEPTB;M{WuNFg3OSEQvF2= M3jmVHNCVkeHUh?=
IMR-5 NFP0dYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnZTWM2OD1|NT6zNVM6KM7:TR?= MkjnV2FPT0WU
TE-441-T MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTN4LkGxOFgh|ryP NYPXR4hOW0GQR1XS
TE-6 M1v5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnuU5lMUUN3ME2zOk4{OjR4IN88US=> MYnTRW5ITVJ?
MOLT-4 Mn\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTN4LkOyO|Yh|ryP MXrTRW5ITVJ?
COLO-684 MnLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTN5LkCxNkDPxE1? NH7nbnZUSU6JRWK=
LU-139 M1vue2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon5TWM2OD1|Nz6xPFU3KM7:TR?= MlmwV2FPT0WU
OPM-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKzTWM2OD1|Nz6yPVQ6KM7:TR?= NWfLTGppW0GQR1XS
ML-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LXSmlEPTB;M{euOlcyOiEQvF2= MYDTRW5ITVJ?
RS4-11 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz2TWM2OD1|Nz63NFY6KM7:TR?= NFjL[GdUSU6JRWK=
MONO-MAC-6 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rlS2lEPTB;M{iuNlQ4PyEQvF2= MljlV2FPT0WU
NCI-H345 MnfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrLW3RiUUN3ME2zPE46OTB4IN88US=> NU\IdIRpW0GQR1XS
NTERA-S-cl-D1 NULiR4FwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTN7LkW4OFIh|ryP MWjTRW5ITVJ?
NCI-H1882 NFyxZnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHr[m1KSzVyPUSwMlU6QThizszN MkPOV2FPT0WU
LC-1F M1PVXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTRzLkW3NFUh|ryP MUXTRW5ITVJ?
HT M4fXfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTR{LkCwNlgh|ryP NFvlVVBUSU6JRWK=
MLMA NUPmWZE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXKTWM2OD12Mj6yO|g4KM7:TR?= NWC4WHBHW0GQR1XS
DG-75 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j2bGlEPTB;NEKuOlU1PiEQvF2= M2T0fHNCVkeHUh?=
GI-ME-N MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTR{Lk[2O|Eh|ryP NFHBOXpUSU6JRWK=
MS-1 Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTSOWdNUUN3ME20Nk45QTNizszN NVTZN2hoW0GQR1XS
CGTH-W-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLoTWM2OD12ND65Olk4KM7:TR?= MnvPV2FPT0WU
NCI-H209 M3PHNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnBTWM2OD12Nj6wNVE2KM7:TR?= MnPwV2FPT0WU
LB2518-MEL MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTR5LkC0OFgh|ryP M{TBWHNCVkeHUh?=
DU-4475 NX7qdZJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzvU|JKSzVyPUS4MlQ6OzdizszN NFHjWm5USU6JRWK=
LB2241-RCC NIiwfmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrNW2xTUUN3ME20PE43OjB{IN88US=> M1jwOXNCVkeHUh?=
LB771-HNC NVu5VHB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1y4bWlEPTB;NEiuPVIyOiEQvF2= M4SyNXNCVkeHUh?=

... 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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