Roscovitine (Seliciclib,CYC202)

For research use only. Not for use in humans.

目录号:S1153

Roscovitine (Seliciclib,CYC202) Chemical Structure

Molecular Weight(MW): 354.45

Roscovitine (Seliciclib,CYC202)是一种有效的,选择性CDK抑制剂,作用于Cdc2CDK2CDK5时,无细胞试验中IC50分别为0.65 μM,0.7 μM和0.16 μM,对CDK4/6几乎没有作用。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1573.18 现货
RMB 1212.83 现货
RMB 3829.77 现货
RMB 7938.98 现货
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客户使用Selleck生产的Roscovitine (Seliciclib,CYC202)发表文献53篇:

产品安全说明书

CDK抑制剂选择性比较

生物活性

产品描述 Roscovitine (Seliciclib,CYC202)是一种有效的,选择性CDK抑制剂,作用于Cdc2CDK2CDK5时,无细胞试验中IC50分别为0.65 μM,0.7 μM和0.16 μM,对CDK4/6几乎没有作用。Phase 2。
靶点
CDK5/p35 [1]
(Cell-free assay)
Cdc2/CyclinB [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
ERK2 [1]
(Cell-free assay)
0.16 μM 0.65 μM 0.7 μM 0.7 μM 14 μM
体外研究

Roscovitine作用于细胞周期蛋白依赖性激酶具有高效性和高度选择性,作用于cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E和cdk5/p53时IC50分别为0.65,0.7,0.7和0.16 μM。纳摩尔级Roscovitine作用于海星卵母细胞和海胆胚胎,可逆抑制在前中期间转变, 在体外作用于非洲爪蟾卵提取物,抑制M期促进因子活性和体外DNA合成,且抑制哺乳动物细胞系增殖,IC50为16 μM。[1] 浓度为7.5, 12.5和 25 mM的 Roscovitine作用于肾小球系膜细胞,导致CDK2活性分别降低25,50% 和100%,这种作用存在剂量依赖性。[2] 最新研究显示Roscovitine作用于盘基网柄菌,抑制cdk5激酶活性,细胞增殖,多细胞发展,和cdk5核转运, 不会影响cdk5蛋白表达。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A3-KAW NYXxSGd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7YVFhLUUN3ME21Mlc3OTF4IN88US=> NYr6[JNsW0GQR1XS
MRK-nu-1 NV\QdGtwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnqTWM2OD15LkGyPVY6KM7:TR?= NUK1dJFiW0GQR1XS
NCCIT M2TtdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTdwNUW0PFIh|ryP M2HodXNCVkeHUh?=
JiyoyeP-2003 MnG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;IWI1KSzVyPUiuOVAzPjRizszN M1TMW3NCVkeHUh?=
KS-1 M3m1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn1TWM2OD17LkS1O|g2KM7:TR?= NIjLdI1USU6JRWK=
Becker NF7SWZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\rZ3JKSzVyPUmuOFYxQDJizszN NX;BTYhpW0GQR1XS
KARPAS-422 M3XUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7YNXN[UUN3ME25Mlk3OzN4IN88US=> Mn3HV2FPT0WU
BB65-RCC NULMVGNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTlwOUe0PVUh|ryP MWnTRW5ITVJ?
SK-UT-1 NXT1foNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu1TWM2OD1zMD6zOUDPxE1? MXLTRW5ITVJ?
ST486 NFm3N4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTFyLkO1NUDPxE1? M{\HdXNCVkeHUh?=
LB831-BLC M3\jN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTFzLkW2NlQh|ryP NFXTV|BUSU6JRWK=
COR-L279 NGHud5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYftc|VRUUN3ME2xNk4zQTB5IN88US=> M1faUnNCVkeHUh?=
NB1 NUPxcI1tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUW0V45uUUN3ME2xNk4{OzB6IN88US=> MXHTRW5ITVJ?
D-247MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTqNYdEUUN3ME2xNk4{PTF4IN88US=> MX3TRW5ITVJ?
697 NVL6b2l2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDKXpdKSzVyPUGyMlYxODdizszN M1XlenNCVkeHUh?=
GCIY M{LSdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PSWGlEPTB;MUKuPFYyOyEQvF2= MUfTRW5ITVJ?
RPMI-8402 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:5R5ZKSzVyPUGzMlYzPjJizszN NUPZdW4xW0GQR1XS
Raji NX7RbHRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\5bmlEPTB;MUOuO|g6PCEQvF2= M4ezVXNCVkeHUh?=
MEG-01 MkfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF|LkizO|kh|ryP MVnTRW5ITVJ?
RPMI-6666 NGLNWVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XjTmlEPTB;MUOuPVEzOSEQvF2= M2fnTnNCVkeHUh?=
SCC-3 NUOyfXVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF2LkK5OVYh|ryP NVXSeWZwW0GQR1XS
HCC1599 NXjFZZJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP5bGoxUUN3ME2xOE42QTd3IN88US=> NX7RZZh2W0GQR1XS
OCI-AML2 NGT0V3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fx[WlEPTB;MUWuOlQ5OiEQvF2= MYDTRW5ITVJ?
OS-RC-2 NFj5W|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF3LkizPFIh|ryP MXLTRW5ITVJ?
NCI-H1304 M17N[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\aUmlKSzVyPUG2MlM3ODFizszN NYezZpFXW0GQR1XS
HD-MY-Z MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTF4LkiyOFYh|ryP MoPsV2FPT0WU
JAR NYnHfolTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LIO2lEPTB;MUeuNFE2OiEQvF2= M17Qc3NCVkeHUh?=
TGW NETvOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfVTWM2OD1zNz64NVI1KM7:TR?= NXnlV5ZnW0GQR1XS
BC-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTF6LkCzNFUh|ryP NEjpeFNUSU6JRWK=
A101D NGX5[npIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTF6LkOyNFgh|ryP NIHYeohUSU6JRWK=
COLO-320-HSR M16xfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTMbolsUUN3ME2xPE44Pjh6IN88US=> NIL1ZlNUSU6JRWK=
LC4-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTF6Lki3N|Qh|ryP NWrT[lJQW0GQR1XS
BC-1 MlrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWH4RY41UUN3ME2xPU4yOTl6IN88US=> NVPGco1zW0GQR1XS
MHH-PREB-1 NX:5XYNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mom4TWM2OD1{MD6wN|U3KM7:TR?= MUHTRW5ITVJ?
BL-70 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjZTXRKSzVyPUKwMlMzPzRizszN NYTJ[HF7W0GQR1XS
CESS NVzOWo1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUCwXI9yUUN3ME2yNE45PTR7IN88US=> NHf2PXBUSU6JRWK=
ES8 NFvHWoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfzSHlOUUN3ME2yNU4xPiEQvF2= NXKzfm1[W0GQR1XS
NOMO-1 NGLYeoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;NZm5IUUN3ME2yNU4zODB6IN88US=> NIDHSJRUSU6JRWK=
ACN M4[5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHOTWM2OD1{MT6zN|g6KM7:TR?= M{fWWXNCVkeHUh?=
EB-3 MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\6TWM2OD1{Mz6xPFMyKM7:TR?= NV7vO3NMW0GQR1XS
LS-513 M4LMdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\PdXhKSzVyPUKzMlUyPzlizszN NXHQcpNxW0GQR1XS
HH MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHiU2JKSzVyPUK0MlM5OTlizszN NHjqfGdUSU6JRWK=
IST-SL2 MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTJ2LkWzOFMh|ryP NF;SW5NUSU6JRWK=
HOP-62 NGHNN4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jmfGlEPTB;MkWuOFQzPSEQvF2= MoTKV2FPT0WU
NCI-H2126 NWTCVWpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJ3Lk[1Nlkh|ryP MX\TRW5ITVJ?
BL-41 NYrLbG1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzVTWM2OD1{NT65OVk4KM7:TR?= MV\TRW5ITVJ?
KURAMOCHI NH[4W4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH6R5lxUUN3ME2yOk45ODh{IN88US=> NEP1U|hUSU6JRWK=
KARPAS-299 MmXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XjOWlEPTB;Mk[uPFY1PiEQvF2= NU\rWldoW0GQR1XS
QIMR-WIL Mo\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDXTWM2OD1{Nz65NVQ1KM7:TR?= NVvocHpTW0GQR1XS
HL-60 NF7FdmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TqW2lEPTB;MkeuPVg3QSEQvF2= MX3TRW5ITVJ?
TE-9 M3PMRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmSyTWM2OD1{OD63PVY6KM7:TR?= MoXLV2FPT0WU
TE-8 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLUZ4pKSzVyPUK4MlkxQCEQvF2= MnznV2FPT0WU
NOS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLxdIFLUUN3ME2yPE46PzN|IN88US=> NFTRb2xUSU6JRWK=
GI-1 NW\OV4piT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;nZ2lEPTB;MkmuNFEyOyEQvF2= MkPqV2FPT0WU
KM12 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT2S4NSUUN3ME2yPU43OjN7IN88US=> MXHTRW5ITVJ?
BB30-HNC NVmxRZYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJ7Lkm0PFMh|ryP NYjDdo5iW0GQR1XS
ES3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTJ7Lkm1PFIh|ryP Mnj6V2FPT0WU
NCI-H510A MlO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nFVWlEPTB;M{CuNFMzQSEQvF2= MVLTRW5ITVJ?
NCI-H82 Mnf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXmTIluUUN3ME2zNU4xOTN3IN88US=> MYrTRW5ITVJ?
NCI-SNU-1 MmDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WwW2lEPTB;M{GuNVA2QSEQvF2= NXL3ZnVIW0GQR1XS
NKM-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTNzLkGzPVch|ryP MnzOV2FPT0WU
SIG-M5 NGSxelNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL3XpBKSzVyPUOxMlY5OzNizszN NV7F[|hqW0GQR1XS
SK-N-FI M1XBbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPUSVRkUUN3ME2zNU44PTN3IN88US=> NFnmTGhUSU6JRWK=
LOUCY MnrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHTNGw4UUN3ME2zNk4yOjV|IN88US=> NFXyOnpUSU6JRWK=
Calu-6 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTN{LkS3OFUh|ryP MkT2V2FPT0WU
GOTO NUPPVG5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTN{LkmxNlkh|ryP MUjTRW5ITVJ?
NCI-H526 NULOZ3FCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXmzRlJrUUN3ME2zN{41QTN4IN88US=> M3PlPXNCVkeHUh?=
RKO MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLlTWM2OD1|Mz61PVY6KM7:TR?= M4TYcnNCVkeHUh?=
NCI-H64 M3rtVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDoN5B2UUN3ME2zN{45PTl5IN88US=> NFfiV|BUSU6JRWK=
LP-1 NH[ySmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTN|Lki5NFgh|ryP MmXaV2FPT0WU
KGN MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TCTWlEPTB;M{SuNlUzPCEQvF2= MoPxV2FPT0WU
NCI-H2141 NV3nXW45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfH[WZKSzVyPUO0MlY2OzNizszN MmnuV2FPT0WU
TE-10 NVjr[XExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTN2Lkm0NlIh|ryP M2W5WnNCVkeHUh?=
K5 MnvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjHV3FKSzVyPUO1MlA5PjFizszN NHv5fVBUSU6JRWK=
IMR-5 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTN3LkOxN|kh|ryP MYjTRW5ITVJ?
TE-441-T MlHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTN4LkGxOFgh|ryP M4HaWnNCVkeHUh?=
TE-6 M1\BdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTN4LkOyOFYh|ryP NYPkSXJCW0GQR1XS
MOLT-4 NXzQV5NET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f2WGlEPTB;M{[uN|I4PiEQvF2= NWr2SWoyW0GQR1XS
COLO-684 M2jT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorOTWM2OD1|Nz6wNVIh|ryP Mn7QV2FPT0WU
LU-139 M{LWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTN5LkG4OVYh|ryP NVOzR|l6W0GQR1XS
OPM-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGH3VYNKSzVyPUO3MlI6PDlizszN M13rOHNCVkeHUh?=
ML-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTN5Lk[3NVIh|ryP M3vJTXNCVkeHUh?=
RS4-11 NWn0N4t6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HIR2lEPTB;M{euO|A3QSEQvF2= M{TORXNCVkeHUh?=
MONO-MAC-6 MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTN6LkK0O|ch|ryP M1TQS3NCVkeHUh?=
NCI-H345 M2DPTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrz[WRMUUN3ME2zPE46OTB4IN88US=> MYnTRW5ITVJ?
NTERA-S-cl-D1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTN7LkW4OFIh|ryP NEHjVI9USU6JRWK=
NCI-H1882 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTRyLkW5PVgh|ryP MVnTRW5ITVJ?
LC-1F NWnYVI5[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2G4dWlEPTB;NEGuOVcxPSEQvF2= MV3TRW5ITVJ?
HT MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PwT2lEPTB;NEKuNFAzQCEQvF2= M4TMd3NCVkeHUh?=
MLMA NXXxdYl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTR{LkK3PFch|ryP Mn3OV2FPT0WU
DG-75 NVi0WZZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR{Lk[1OFYh|ryP MXTTRW5ITVJ?
GI-ME-N NXT4RVFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HOXWlEPTB;NEKuOlY4OSEQvF2= MkHBV2FPT0WU
MS-1 NYfRSnF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3r3UWlEPTB;NEKuPFk{KM7:TR?= MmjaV2FPT0WU
CGTH-W-1 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnRRYFlUUN3ME20OE46Pjl5IN88US=> M1:wdXNCVkeHUh?=
NCI-H209 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HYNGlEPTB;NE[uNFEyPSEQvF2= MknOV2FPT0WU
LB2518-MEL NWTNVYM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTR5LkC0OFgh|ryP M{HsenNCVkeHUh?=
DU-4475 Moe3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTR6LkS5N|ch|ryP NULCfJpRW0GQR1XS
LB2241-RCC NFHIbG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXITWM2OD12OD62NlAzKM7:TR?= MonsV2FPT0WU
LB771-HNC MlrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDnXmxKSzVyPUS4MlkzOTJizszN M2L0RXNCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Rb / p-CDK2 / CDK2 / Cyclin D1 / Cyclin A2 / ERα / ERβ/ AIB1 / PELP1 ; 

PubMed: 21834972     


(a) The model cells MCF7, MCF7-TamR, MCF7-HER2, and MCF7-LTLTca were treated with roscovitine and the status of cell cycle regulators and the estrogen receptor (ERα) signaling proteins was analyzed by western blotting. 

pT231-tau / pS202-tau / tau; 

PubMed: 30915013     


SH-SY5Y-(P301L) cells were exposed for 6 h to a range of roscovitine concentrations. Cells were harvested and proteins were resolved by SDS-PAGE followed by western blotting.

21834972 30915013
Immunofluorescence
E2F1 / FASN / Bmi1 / Cyclin D2 / CDK2 / CDK4 ; 

PubMed: 20890301     


Immunofluorescence analysis of E2F1, FASN, E2F1/Shh target Bmi1, cyclin D2, cdk 2, and cdk 4 in Pzp53med cells treated with DMSO (control) or the cdk inhibitor roscovitine (10 nM) for 18 hours.

CDK1 / Smek2 / FUBP1 / Cdc20 ; 

PubMed: 24534090     


A-D Validation of changes in chromatin affinity following Cdk inhibition of indicated candidates (2 h, 50 μM roscovitine) using Triton extraction and immunofluorescence (IF) in HeLa cells. Quantification of IF data was performed by measuring changes in signal intensities in Image J.

20890301 24534090
Growth inhibition assay
Cell viability; 

PubMed: 29996940     


Cell viability assay on OVCAR5, OAW42, SKOV3 and NL3507 cells treated with roscovitine (2, 5, 10, 20, 40 μM) up to 96 h. Each point represents the mean of three replicates. Error bars, SD

29996940
体内研究 Roscovitine按50 mg/kg剂量作用于Ewing's肉瘤家族(ESFT)移植瘤,明显抑制肿瘤生长。[4] Roscovitine作用于携带MCF7移植瘤的裸鼠,增强抗癌Doxorubicin抗癌效果,不会提高毒性,机制是使细胞周期停滞而不是引起凋亡。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

酶实验:

激酶活性实验在30oC下buffer C中进行。从数据中除去空白值,在10分钟的温育期中测定渗透到蛋白受体中的磷酸摩尔数,来计算活性。对照组用适当稀释的DMSO处理。在一些情况下, SDS/PAGE后通过自动射线照相术测定底物磷酸化。p34cdc2/cyclin B通过亲和色谱从 M期海星卵母细胞中纯化。使用 1 mg 组蛋白Hl/mL,在15 μM [γ-32P]ATP存在时进行实验,终浓度为 30 μL。在 30oC下温育10分钟, 25-μL上清液 转移到Whatman P81磷酸纤维素纸上, 20秒后, 用10mL磷酸/L水冲洗过滤器5次,每次至少5分钟。湿式过滤器转移到 6 mL闪烁管,加入5 mL ACS闪烁液,使用Packard 计数器测定放射性。测定在10分钟温育期中组蛋白H1渗透放入磷酸摩尔数评估激酶活性或者最大活性百分数。感染不同杆状病毒的sf9昆虫细胞抽提物中再生p33cdk2/cyclin A和p33cdk2/cyclinE。Cyclins A 和E是谷胱甘肽S-转移酶融合蛋白,复合体从谷胱甘肽-琼脂糖珠上纯化。使用 1 mg/mL 组蛋白Hl/mL,在15 μM [γ-32P]ATP存在时,进行激酶活性实验10分钟,终体积为30 μL,测定p34cdc2/cyclin B激酶。p33cdk5/p35从牛脑中纯化,除了Mono S-色层分离一步法。 Superose 12柱的活性片段汇集,终浓度为25 μg 酶/mL。使用1 mg/mL 组蛋白Hl, 在15 μM [γ-32P]ATP存在时,进行激酶活性实验10分钟,终体积为 30 μL,测定p34cdc2/cyclin B激酶。
细胞实验:[1]
- 合并
  • Cell lines: 白血病, 非小细胞肺癌,结肠癌, 中枢神经系统肿瘤, 恶性黑色素瘤,卵巢癌,肾癌, 前列腺癌,胸腺癌细胞系
  • Concentrations: 0.01到100 μM
  • Incubation Time: 48小时
  • Method: 包括9种肿瘤类型的60种人类肿瘤细胞系培养24小时,然后用 0.01-100 μM Roscovitine持续处理48小时。进行sulforhodaminine B蛋白实验测评毒性。
    (Only for Reference)
动物实验:[4
- 合并
  • Animal Models: 右后侧皮下注射A4573细胞的CD1 nu/nu鼠
  • Formulation: Roscovitine 溶于无水甲醇或DMSO,然后用 10% Tween-80, 20% N-N-二甲基乙酰胺, 和70% PEG 400稀释
  • Dosages: ≤50 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 71 mg/mL (200.31 mM)
Ethanol 6 mg/mL (16.92 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+69% PEG 400
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 354.45
化学式

C19H26N6O

CAS号 186692-46-6
储存条件 粉状
溶于溶剂
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How can I reconstitute the drug for in vivo studies?

  • 回答:

    S1153 in 1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+PEG 400 is a clear solution which is okay for injection. And S1153 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30mg/ml is a suspension, which is fine for oral gavage.

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

相关CDK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID