Roscovitine (Seliciclib,CYC202)

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。

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客户使用该产品的5个实验数据:

  • In vitro inhibition of mouse corticotroph tumor cells by R-roscovitine. (A) Treatment of ACTH-secreting AtT20 cells with R-roscovitine (1-2 × 10-5 μM) led to decreased number of viable cells at 24 and 48 h, as depicted by Wst-1 proliferation assay (mean ± SE; **P < 0.01). (B) Western blot of protein extracts derived from AtT20 cells treated with vehicle or R-roscovitine. (C) R-roscovitine treatment (10 μM) for 48 h induced senescence as indicated by increased β-gal expression. (D) ACTH concentration by radioimmunoassays of culture medium from AtT20 cells treated with vehicle or R-roscovitine (mean ±SE; **P < 0.01 and ***P < 0.001). (E) Western blot of protein extracts derived from AtT20 cells treated with R-roscovitine. Vehicle is 0.2% DMSO.

    PNAS 2011 108, 8417. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

    In vivo action of R-roscovitine inmouse corticotroph adenomas. Athymic nude mice were s.c. inoculated with corticotroph tumor AtT20 cells (1 × 105 cells). Three days after injection, mice were randomized to receive Rroscovitine (150 mg/kg) or vehicle by oral gavage twice daily, 5 d/wk. After 3 wk, tumor xenografts were dissected and (A) tumor volumes were decreased in R-roscovitine-treated animals. (B) Western blot of representative tumor specimens showed decreased ACTH and PCNA expression in R-roscovitine-treated tumors. (C) R-roscovitine-treated corticotroph tumors exhibited decreased PCNA and ACTH coexpressing cells. Fluorescence microscopy image of immunohistochemistry detecting PCNA (red) and ACTH (green) expression in control (a-c) and R-roscovitine-treated tumors (d-f). Cryosection slides were counterstained with DAPI (blue). (D) Blood was collected from each animal for measurement of plasma ACTH and serum corticosterone levels (mean ±SE; n = 13-14 mice for each group; **P < 0.01).

    PNAS 2011 108, 8417. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

  • (a-c) Relative viability of Cis-R cells and parental MDA-MB-231 (Cis-S) cells in the presence of cisplatin (10 μM) and the increasing concentrations of WEE1i (a), ATRi (b) and CHK1i (c). (d) Illustration of the experimental setup, with incorporation of IdU and CldU shown in red and green, respectively. (e) As shown in (d), MDA-MB-231 cells were incubated with IdU for 10 min as indicated, followed by cisplatin treatment for 3 hours, with or without indicated inhibitor(s) (top) for indicated total 40 min and CIdU was applied for 10 min. Cells were fixed and stained with IdU and CIdU antibodies. Nuclear DNA was counterstained by DAPI. (f) Quantification of indicated part of three separate experiments as in (e) represented as the mean ± SEM. CDKi:Roscovitine.

    Sci Rep, 2017, 7:43517. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

    Inhibition of CDK5 by roscovitine resulted in defective neuronal migration, which was rescued by expression of GFP-Ndel1 (S251E). a, Granular neurons were treated with roscovitine. Western blotting was performed 24 h after start of culture. Aurora-A and NDEL1 displayed similar expression levels with untreated neurons, whereas the levels of phosphorylated Aurora-A and NDEL1 proteins were decreased after treatment with roscovitine. Relative intensities of the bands of Western blotting are shown at the bottom.

    J Hematol Oncol 2012 7, 53. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

  •  

    Chronic treatment with roscovitine attenuates the development of atherosclerosis in ApoE-/- mice. Vehicle, roscovitine or resveratrol were daily administered to ApoE-/- mice under high fat high cholesterol diet, from the age of four weeks old. After 18 weeks of treatment, Oil-Red-O (A) and SA-β-gal (B) staining was performed using aortae collected from all groups of mice.Chronic treatment with roscovitine attenuates the development of atherosclerosis in ApoE-/- mice. Vehicle, roscovitine or resveratrol were daily administered to ApoE-/- mice under high fat high cholesterol diet, from the age of four weeks old. After 18 weeks of treatment, Oil-Red-O (A) and SA-β-gal (B) staining was performed using aortae collected from all groups of mice.

    University of Hong Kong. Roscovitine (Seliciclib,CYC202) purchased from Selleck.

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 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DYc2lEPTB;NT63OlEyPiEQvF2= M{LxOXNCVkeHUh?=
MRK-nu-1 Mnv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;mVpNpUUN3ME23MlEzQTZ7IN88US=> NYqzV5J{W0GQR1XS
NCCIT M2DhUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;ETGlEPTB;Nz61OVQ5OiEQvF2= NWL5c4I2W0GQR1XS
JiyoyeP-2003 NXK4Z4RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRThwNUCyOlQh|ryP NIPKTVJUSU6JRWK=
KS-1 NG\O[VBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXTWVZKSzVyPUmuOFU4QDVizszN M1zwPXNCVkeHUh?=
Becker M{\ONWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mli1TWM2OD17LkS2NFgzKM7:TR?= MlLYV2FPT0WU
KARPAS-422 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;tV41KSzVyPUmuPVY{OzZizszN NHjp[lhUSU6JRWK=
BB65-RCC NIT5epdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWOzZY5zUUN3ME25Mlk4PDl3IN88US=> NHPvV4VUSU6JRWK=
SK-UT-1 NHG4THBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfMZXNKSzVyPUGwMlM2KM7:TR?= NX7GbXRZW0GQR1XS
ST486 NUPtTmd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFyLkO1NUDPxE1? NU\EUG1vW0GQR1XS
LB831-BLC M2XPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFzLkW2NlQh|ryP NYToXVV[W0GQR1XS
COR-L279 NHvoO49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi0dZVKSzVyPUGyMlI6ODdizszN NVPFOZVNW0GQR1XS
NB1 NU\SZlR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF{LkOzNFgh|ryP MlXxV2FPT0WU
D-247MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF{LkO1NVYh|ryP MWjTRW5ITVJ?
697 NWruNnJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGroOZpKSzVyPUGyMlYxODdizszN MVjTRW5ITVJ?
GCIY NW\zSW1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPaVJdGUUN3ME2xNk45PjF|IN88US=> M4DIS3NCVkeHUh?=
RPMI-8402 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTsdo1SUUN3ME2xN{43OjZ{IN88US=> Mm\4V2FPT0WU
Raji Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTYXpFKSzVyPUGzMlc5QTRizszN NGfXco1USU6JRWK=
MEG-01 MoPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvaTWM2OD1zMz64N|c6KM7:TR?= NWXWWoc5W0GQR1XS
RPMI-6666 NF\uSWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF|LkmxNlEh|ryP M{GwT3NCVkeHUh?=
SCC-3 M{TiTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zTZ2lEPTB;MUSuNlk2PiEQvF2= MWfTRW5ITVJ?
HCC1599 NIXNRXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP6dWVTUUN3ME2xOE42QTd3IN88US=> M4P2WnNCVkeHUh?=
OCI-AML2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGCwTolKSzVyPUG1MlY1QDJizszN MX\TRW5ITVJ?
OS-RC-2 NFr6[2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTF3LkizPFIh|ryP M3T3bHNCVkeHUh?=
NCI-H1304 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[yWmlEPTB;MU[uN|YxOSEQvF2= NET6e5JUSU6JRWK=
HD-MY-Z Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTnPW1nUUN3ME2xOk45OjR4IN88US=> NE\1b2pUSU6JRWK=
JAR NF;RO3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH0cHcyUUN3ME2xO{4xOTV{IN88US=> Mli3V2FPT0WU
TGW NF\pZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnKTWM2OD1zNz64NVI1KM7:TR?= NGDsb5ZUSU6JRWK=
BC-3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGG2WlBKSzVyPUG4MlA{ODVizszN NFXBeIRUSU6JRWK=
A101D MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkWwTWM2OD1zOD6zNlA5KM7:TR?= NUK0bGhpW0GQR1XS
COLO-320-HSR MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTF6Lke2PFgh|ryP NW\sdGwzW0GQR1XS
LC4-1 NITVSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTheIZKSzVyPUG4Mlg4OzRizszN MUHTRW5ITVJ?
BC-1 NETic2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:4TWM2OD1zOT6xNVk5KM7:TR?= M3PEcHNCVkeHUh?=
MHH-PREB-1 MmGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:zcXdtUUN3ME2yNE4xOzV4IN88US=> NXe4eHd{W0GQR1XS
BL-70 M3;iSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j6bmlEPTB;MkCuN|I4PCEQvF2= MYPTRW5ITVJ?
CESS MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTWTYhKSzVyPUKwMlg2PDlizszN NHLodnZUSU6JRWK=
ES8 MoewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf5RmtKSzVyPUKxMlA3KM7:TR?= NVnRN21SW0GQR1XS
NOMO-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTJzLkKwNFgh|ryP M3jlW3NCVkeHUh?=
ACN Mnj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvifW1xUUN3ME2yNU4{Ozh7IN88US=> NEHTcJBUSU6JRWK=
EB-3 MkDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJ|LkG4N|Eh|ryP M{C5U3NCVkeHUh?=
LS-513 M3vmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7pN|NKSzVyPUKzMlUyPzlizszN M2G5b3NCVkeHUh?=
HH M4DlOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJ2LkO4NVkh|ryP NESzUZNUSU6JRWK=
IST-SL2 M{W0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\1dWlEPTB;MkSuOVM1OyEQvF2= NXvxUWtjW0GQR1XS
HOP-62 M3zUTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnDTWM2OD1{NT60OFI2KM7:TR?= M4OyW3NCVkeHUh?=
NCI-H2126 NFrZXZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTQZWNKUUN3ME2yOU43PTJ7IN88US=> M2fafHNCVkeHUh?=
BL-41 NYq5eFJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zCRWlEPTB;MkWuPVU6PyEQvF2= MWTTRW5ITVJ?
KURAMOCHI MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJ4LkiwPFIh|ryP Mm\3V2FPT0WU
KARPAS-299 MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLxTWM2OD1{Nj64OlQ3KM7:TR?= NFn4d3BUSU6JRWK=
QIMR-WIL MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJ5LkmxOFQh|ryP NHPJXmdUSU6JRWK=
HL-60 NFy1dWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DzNmlEPTB;MkeuPVg3QSEQvF2= NYfnOnFNW0GQR1XS
TE-9 Mn6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID4fJVKSzVyPUK4Mlc6PjlizszN M2X5WXNCVkeHUh?=
TE-8 NVrKWplET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmm1TWM2OD1{OD65NFgh|ryP Mm\TV2FPT0WU
NOS-1 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnHcZA1UUN3ME2yPE46PzN|IN88US=> NX\jUohYW0GQR1XS
GI-1 M{LpT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:wfWlEPTB;MkmuNFEyOyEQvF2= MmnDV2FPT0WU
KM12 NF\BdYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;iTWM2OD1{OT62NlM6KM7:TR?= NYe1T3hsW0GQR1XS
BB30-HNC MnfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJ7Lkm0PFMh|ryP NIDvbnZUSU6JRWK=
ES3 NVPVTpRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\FWWhQUUN3ME2yPU46PTh{IN88US=> Mn;LV2FPT0WU
NCI-H510A M2LBXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DxSGlEPTB;M{CuNFMzQSEQvF2= NGX5bVhUSU6JRWK=
NCI-H82 NYTjdlFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXK0NGtnUUN3ME2zNU4xOTN3IN88US=> NVLjOmRrW0GQR1XS
NCI-SNU-1 NILSSWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zaSmlEPTB;M{GuNVA2QSEQvF2= NH3VcHhUSU6JRWK=
NKM-1 NEfSXINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3CRWg5UUN3ME2zNU4yOzl5IN88US=> NXnNfFVuW0GQR1XS
SIG-M5 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nCUmlEPTB;M{GuOlg{OyEQvF2= M4\EfnNCVkeHUh?=
SK-N-FI NGfhWWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm2bmpyUUN3ME2zNU44PTN3IN88US=> MUjTRW5ITVJ?
LOUCY Mm\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mln4TWM2OD1|Mj6xNlU{KM7:TR?= M2fOUXNCVkeHUh?=
Calu-6 NYT3OnJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDXcIxXUUN3ME2zNk41PzR3IN88US=> NIP2NVhUSU6JRWK=
GOTO NYHFb2x1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\iR3dHUUN3ME2zNk46OTJ7IN88US=> NXT2cXdRW0GQR1XS
NCI-H526 M4\CPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rEbGlEPTB;M{OuOFk{PiEQvF2= NYHLdI04W0GQR1XS
RKO M3O4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\PTXNKSzVyPUOzMlU6PjlizszN NHPx[2ZUSU6JRWK=
NCI-H64 NELaRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTN|Lki1PVch|ryP Mn76V2FPT0WU
LP-1 MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rGcmlEPTB;M{OuPFkxQCEQvF2= NFfjb4VUSU6JRWK=
KGN M{DiXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjoTWM2OD1|ND6yOVI1KM7:TR?= MVXTRW5ITVJ?
NCI-H2141 M1PDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTN2Lk[1N|Mh|ryP MUPTRW5ITVJ?
TE-10 MnXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[1TWM2OD1|ND65OFIzKM7:TR?= Mme5V2FPT0WU
K5 M4XEPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTN3LkC4OlEh|ryP MlntV2FPT0WU
IMR-5 M1ziW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPTTWM2OD1|NT6zNVM6KM7:TR?= NVvZTHdKW0GQR1XS
TE-441-T Mm\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUH2UFZKUUN3ME2zOk4yOTR6IN88US=> NX7XVpRNW0GQR1XS
TE-6 M4G4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX2TmpKSzVyPUO2MlMzPDZizszN MoXEV2FPT0WU
MOLT-4 NFSw[3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TnRWlEPTB;M{[uN|I4PiEQvF2= MXXTRW5ITVJ?
COLO-684 NXLOWIRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfSTWM2OD1|Nz6wNVIh|ryP NXLKTYVnW0GQR1XS
LU-139 MkLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIi3XW5KSzVyPUO3MlE5PTZizszN NFfXe|VUSU6JRWK=
OPM-2 NFfPRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXviZWNiUUN3ME2zO{4zQTR7IN88US=> NVHER|lEW0GQR1XS
ML-2 NXK4WoR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTN5Lk[3NVIh|ryP MlLwV2FPT0WU
RS4-11 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXrTWM2OD1|Nz63NFY6KM7:TR?= NW[ySllwW0GQR1XS
MONO-MAC-6 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWGweWdGUUN3ME2zPE4zPDd5IN88US=> MnrGV2FPT0WU
NCI-H345 M1rXZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjOU3RyUUN3ME2zPE46OTB4IN88US=> MnL2V2FPT0WU
NTERA-S-cl-D1 NULpNnRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPMTWM2OD1|OT61PFQzKM7:TR?= NHGxW2ZUSU6JRWK=
NCI-H1882 NGDSSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTRyLkW5PVgh|ryP NXPnTJA6W0GQR1XS
LC-1F MoXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfLSFloUUN3ME20NU42PzB3IN88US=> MkLQV2FPT0WU
HT Mn;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LPOmlEPTB;NEKuNFAzQCEQvF2= M{C3c3NCVkeHUh?=
MLMA Mli0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvlbYJKSzVyPUSyMlI4QDdizszN M1jzOHNCVkeHUh?=
DG-75 NXzKSlY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPUN2hTUUN3ME20Nk43PTR4IN88US=> MmDmV2FPT0WU
GI-ME-N M17jVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XaR2lEPTB;NEKuOlY4OSEQvF2= NVnlSXVGW0GQR1XS
MS-1 NHXISZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrMTWM2OD12Mj64PVMh|ryP NUHER4dEW0GQR1XS
CGTH-W-1 NIG2eWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfITWM2OD12ND65Olk4KM7:TR?= NUmyXmZ3W0GQR1XS
NCI-H209 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3vTWM2OD12Nj6wNVE2KM7:TR?= NX\sS49IW0GQR1XS
LB2518-MEL MkHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor4TWM2OD12Nz6wOFQ5KM7:TR?= M4HZeXNCVkeHUh?=
DU-4475 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T0PWlEPTB;NEiuOFk{PyEQvF2= Mmr0V2FPT0WU
LB2241-RCC Mnf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr3eVl3UUN3ME20PE43OjB{IN88US=> MorDV2FPT0WU
LB771-HNC M1PS[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXNUHFKSzVyPUS4MlkzOTJizszN NIfIdFlUSU6JRWK=

... Click to View More Cell Line Experimental Data

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]
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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]
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  • 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
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  • 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:
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
稳定性 powder
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 (g) = 浓度 (mol/L) x 体积 (L) 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

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02649751 Recruiting Cystic Fibrosis University Hospital, Brest|ManRos Therapeutics|Cyclacel Pharmaceuticals, Inc. February 2016 Phase 2
NCT02160730 Recruiting Cushings Disease Shlomo Melmed, MD|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Cedars-Sinai Medical Center May 2014 Phase 2
NCT01333423 Withdrawn Breast Cancer M.D. Anderson Cancer Center|National Institutes of Health (NIH) September 2012 Phase 1
NCT00999401 Recruiting Advanced Solid Tumors Cyclacel Pharmaceuticals, Inc. April 2009 Phase 1
NCT00372073 Terminated Non-small Cell Lung Cancer Cyclacel Pharmaceuticals, Inc. July 2006 Phase 2

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID