Roscovitine

別名：CYC202, Seliciclib, R-roscovitine

製品コード：S1153 純度：99.85%

Roscovitine is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.

CAS No. 186692-46-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 28600	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 70500	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 250500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（124）

製品安全説明書

現在のバッチを見る：純度： 99.85%

99.85

Roscovitine関連製品

関連ターゲット	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	もっと見る
関連製品	Ro-3306 Dinaciclib Flavopiridol (Alvocidib) SNS-032 (BMS-387032) Flavopiridol (Alvocidib) HCl AT7519 LDC000067 PHA-767491 HCl THZ1 2HCl XL413 JNJ-7706621 AZD5438 Purvalanol A Milciclib BS-181 HCl K03861 (AUZ454) PHA-793887 BMS-265246 AT7519 HCl AZD4573 MSC2530818 Riviciclib hydrochloride (P276-00) CVT-313 TG003 Kenpaullone R547 Atuveciclib (BAY-1143572) YKL-5-124 LDC4297 Enitociclib (BAY 1251152) PF-06873600 Wogonin SU9516 SEL120 (SEL120-34A) hydrochloride THZ531 Senexin A Samuraciclib (ICEC0942) hydrochloride LY2857785 ON123300 CDK2-IN-73 (CDK2-IN-4) NU2058 BRD6989 HLM006474 AS2863619 CDKI-73 MC180295 ML167 Simurosertib Simurosertib NSC95397 NU6027	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

CDKシグナル伝達経路

CDK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
LP-1	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human LP-1 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry	15958589
LP-1	Cytotoxicity assay	20 to 30 uM	24 hrs	Cytotoxicity against human LP-1 cells assessed as reduction of cell viability at 20 to 30 uM treated for 24 hrs followed by washout measured after total 72 hrs growth period alamar blue assay relative to control	15958589
LP-1	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human LP-1 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
LP-1	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human LP-1 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting	15958589
LP-1	Apoptosis assay	30 uM	3 to 5 hrs	Induction of apoptosis in human LP-1 cells assessed as increase in level of cleaved PARP at 30 uM after 3 to 5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as increase in level of cleaved PARP at 30 uM after 5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as fast slow migrating hyperphosphorylated RNA polymerase 2O form at 30 uM after 1.5 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human RPM18226 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human RPM18226 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	3 to 5 hrs	Induction of apoptosis in human RPM18226 cells assessed as increase in level of cleaved PARP at 30 uM after 3 to 5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as changes in XIAP protein level at 30 uM after 3 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as changes in survivin protein level at 30 uM after 3 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human RPM18226 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as dephosphorylation of pRb at S249/T252 at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Cytotoxicity assay	20 to 30 uM	16 hrs	Cytotoxicity against human NCI-H929 cells assessed as reduction of cell viability at 20 to 30 uM treated for 16 hrs followed by washout measured after total 72 hrs growth period alamar blue assay relative to control	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as changes in Bcl-2 protein level at 30 uM after 3 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of RNA polymerase 2 phosphoserine 5 level at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of Hdm2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as increase of p53 accumulation at 30 uM after 1.5 hrs by immunoblotting	15958589
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of cyclin A in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of cyclin B in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of cyclin D1 in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of CDK2 in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HT-29	Function assay	2.5 to 40 uM	24 hrs	Inhibition of retinoblastoma protein in human HT-29 cells assessed as reduction of cyclin A level at 2.5 to 40 uM after 24 hrs by immunoblotting	21417417
MCF7	Cell cycle assay	80 uM	24 hrs	Cell cycle arrest in human MCF7 cells assessed as reduction of actively replicating DNA level at 80 uM after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
MCF7	Function assay	20 uM	24 hrs	Induction of p53-dependent transcriptional activity in human MCF7 cells assessed as increase of p21 WAF1 level at 20 uM after 24 hrs by immunofluorescence assay	21417417
RPMI8226	Cell cycle assay	80 uM	24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as reduction of actively replicating DNA level at 80 uM after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
A549	Apoptosis assay	2 uM	48 hrs	Induction of apoptosis in human A549 cells assessed as DNA fragmentation at 2 uM after 48 hrs by agarose gel electrophoresis	23623491
BJ	Function assay	10 uM	10 days	Suppression of senescence in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay	24681986
BJ	Function assay	10 uM	10 days	Inhibition of ataxia telangiectasia-mutated in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay	24681986
MCF7	Function assay	10 uM	10 mins	Sensitization of infrared-induced DNA damage in human MCF7 cells assessed as reduction in colony formation at 10 uM pretreated for 10 mins followed by irradiation for 4 hrs measured after 10 days by crystal violet staining analysis	26851505
MCF7	Cell cycle assay		24 hrs	Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
RPMI8226	Cell cycle assay		24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
MCF7	Cell cycle assay		24 hrs	Cell cycle arrest in human MCF7 cells assessed as decrease in S phase cell population after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
MCF7	Cell cycle assay		24 hrs	Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
RPMI8226	Cell cycle assay		24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at sub-G1 phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
RPMI8226	Cell cycle assay		24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as decrease in S phase cell population after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
Sf9	Function assay		10 mins	Inhibition of His-6-tagged recombinant human CDK2/cyclinE expressed in baculovirus-infected sf9 cells using histone H1 as substrate after 10 mins by liquid scintillation counting in presence of [gamma-32P]ATP, IC50 = 0.1 μM.	24417566
NCI-SNU-1	Growth Inhibition Assay			IC50=31.1059 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=31.1397 μM	SANGER
SIG-M5	Growth Inhibition Assay			IC50=31.6833 μM	SANGER
SK-N-FI	Growth Inhibition Assay			IC50=31.7535 μM	SANGER
LOUCY	Growth Inhibition Assay			IC50=32.1253 μM	SANGER
Calu-6	Growth Inhibition Assay			IC50=32.4745 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=32.9129 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=33.4936 μM	SANGER
RKO	Growth Inhibition Assay			IC50=33.5969 μM	SANGER
NCI-H64	Growth Inhibition Assay			IC50=33.8597 μM	SANGER
LP-1	Growth Inhibition Assay			IC50=33.8908 μM	SANGER
KGN	Growth Inhibition Assay			IC50=34.2524 μM	SANGER
NCI-H2141	Growth Inhibition Assay			IC50=34.6533 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=34.9422 μM	SANGER
K5	Growth Inhibition Assay			IC50=35.0861 μM	SANGER
IMR-5	Growth Inhibition Assay			IC50=35.3139 μM	SANGER
TE-441-T	Growth Inhibition Assay			IC50=36.1148 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=36.3246 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=36.3276 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=37.012 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=37.1856 μM	SANGER
OPM-2	Growth Inhibition Assay			IC50=37.2949 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=37.6712 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=37.7069 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=38.2477 μM	SANGER
NCI-H345	Growth Inhibition Assay			IC50=38.9106 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=39.5842 μM	SANGER
NCI-H1882	Growth Inhibition Assay			IC50=40.5998 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=41.5705 μM	SANGER
HT	Growth Inhibition Assay			IC50=42.0028 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=42.2787 μM	SANGER
DG-75	Growth Inhibition Assay			IC50=42.6546 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=42.6671 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=42.893 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=44.9697 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=46.0115 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=47.0448 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=48.4937 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=48.6202 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=48.9212 μM	SANGER
NCI-H82	Growth Inhibition Assay			IC50=31.0135 μM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=30.0329 μM	SANGER
ES3	Growth Inhibition Assay			IC50=29.9582 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=29.9483 μM	SANGER
KM12	Growth Inhibition Assay			IC50=29.6239 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=29.0113 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=28.9733 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=28.908 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=28.7969 μM	SANGER
HL-60	Growth Inhibition Assay			IC50=27.9869 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=27.9144 μM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=26.8646 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=26.8082 μM	SANGER
BL-41	Growth Inhibition Assay			IC50=25.9597 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=25.6529 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=25.4425 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=24.5343 μM	SANGER
HH	Growth Inhibition Assay			IC50=24.3819 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=23.5179 μM	SANGER
EB-3	Growth Inhibition Assay			IC50=23.1831 μM	SANGER
ACN	Growth Inhibition Assay			IC50=21.3389 μM	SANGER
NOMO-1	Growth Inhibition Assay			IC50=21.2008 μM	SANGER
ES8	Growth Inhibition Assay			IC50=21.06 μM	SANGER
CESS	Growth Inhibition Assay			IC50=20.8549 μM	SANGER
BL-70	Growth Inhibition Assay			IC50=20.3274 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=20.0356 μM	SANGER
BC-1	Growth Inhibition Assay			IC50=19.1198 μM	SANGER
LC4-1	Growth Inhibition Assay			IC50=18.8734 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=18.7688 μM	SANGER
A101D	Growth Inhibition Assay			IC50=18.3208 μM	SANGER
BC-3	Growth Inhibition Assay			IC50=18.0305 μM	SANGER
TGW	Growth Inhibition Assay			IC50=17.8124 μM	SANGER
JAR	Growth Inhibition Assay			IC50=17.0152 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=16.8246 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=16.3601 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=15.8382 μM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=15.6482 μM	SANGER
HCC1599	Growth Inhibition Assay			IC50=14.5975 μM	SANGER
SCC-3	Growth Inhibition Assay			IC50=14.2956 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=13.9121 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=13.8379 μM	SANGER
Raji	Growth Inhibition Assay			IC50=13.7894 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=13.6262 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=12.8613 μM	SANGER
697	Growth Inhibition Assay			IC50=12.6007 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=12.3516 μM	SANGER
NB1	Growth Inhibition Assay			IC50=12.3308 μM	SANGER
COR-L279	Growth Inhibition Assay			IC50=12.2907 μM	SANGER
LB831-BLC	Growth Inhibition Assay			IC50=11.5624 μM	SANGER
ST486	Growth Inhibition Assay			IC50=10.351 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=10.35 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=9.97495 μM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=9.96336 μM	SANGER
Becker	Growth Inhibition Assay			IC50=9.46082 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=9.45785 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=8.50264 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=7.55482 μM	SANGER
MRK-nu-1	Growth Inhibition Assay			IC50=7.12969 μM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=5.76116 μM	SANGER
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	15958589
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	21080703
Caco2	Cell cycle assay			Cell cycle arrest in human Caco2 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HaCaT	Cell cycle assay			Cell cycle arrest in human HaCaT cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HuH7	Cell cycle assay			Cell cycle arrest in human HuH7 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
PC3	Cell cycle assay			Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase by Hoechst staining based fluorescence assay	28214231
MDA-MB-231	Cell cycle assay			Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HCT116	Cell cycle assay			Cell cycle arrest in human HCT116 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	28557430
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	30199702
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生物活性

製品説明

Roscovitine is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.

Targets

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

In Vitro
In vitro	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]
Kinase Assay	Enzymes
Kinase Assay	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. p34^cdc2/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. p33^cdk2/cyclin A and p33^cdk2/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 p34^cdc2/cyclin B kinase. p33^cdk5/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 p34^cdc2/cyclin B kinase. p33^cdk5/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. p33^cdk4/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 p34^cdc2cyclin 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. 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 p34^cdc2/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 p34^cdc2/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 p34^cdc2/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 p34^cdc2/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 p34^cdc2/cyclin B kinase.
細胞実験	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	pT231-tau / pS202-tau / tau p-Rb / p-CDK2 / CDK2 / Cyclin D1 / Cyclin A2 / ERα / ERβ/ AIB1 / PELP1		30915013
	Immunofluorescence	CDK1 / Smek2 / FUBP1 / Cdc20 E2F1 / FASN / Bmi1 / Cyclin D2 / CDK2 / CDK4		24534090
	Growth inhibition assay	Cell viability		29996940

In Vivo
In Vivo	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]
動物実験	動物モデル	A4573 cells are injected s.c. into the right posterior flank of CD1 nu/nu mice.
	投与量	≤50 mg/kg
	投与経路	Administered via i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02649751	Terminated	Cystic Fibrosis	University Hospital Brest\|ManRos Therapeutics\|Cyclacel Pharmaceuticals Inc.	February 22 2016	Phase 2

参考
[1] Meijer L, et al. Eur J Biochem, 1997, 243(1-2), 527-536. [2] Pippin JW, et al. J Clin Invest, 1997, 100(10), 2512-2520. [3] Huber RJ, et al. J Cell Biochem, 2012, 113(3), 868-876. [4] Tirado OM, et al. Cancer Res, 2005, 65(20), 9320-9327. [5] Appleyard MV, et al. Int J Cancer, 2009, 124(2), 465-472. + 展開

参考

+ 展開

化学情報

分子量	354.45	化学式	C₁₉H₂₆N₆O
CAS No.	186692-46-6	SDF	Download Roscovitine SDFをダウンロードする
Smiles	CCC(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=CC=C3
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 71 mg/mL ( (200.31 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 71 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

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よくある質問（FAQ）

質問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.

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):