Roscovitine

別名: CYC202, Seliciclib, R-roscovitine

目錄號(hào)：S1153 Purity: 99.85%

Roscovitine是一種有效的，選擇性CDK抑制劑，作用于Cdc2，CDK2和CDK5時(shí)，無(wú)細(xì)胞試驗(yàn)中IC50分別為0.65 μM，0.7 μM和0.16 μM，對(duì)CDK4/6幾乎沒(méi)有作用。Phase 2。

Roscovitine Chemical Structure

CAS: 186692-46-6

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1573.18	現(xiàn)貨
10mg	1212.83	現(xiàn)貨
25mg	2104.83	現(xiàn)貨
50mg	3829.77	現(xiàn)貨
200mg	7938.98	現(xiàn)貨
1g	13677.3	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.85%

99.85

Roscovitine相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)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	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) MAPK抑制劑庫(kù) DNA損傷/ DNA修復(fù)化合物庫(kù) 細(xì)胞周期化合物庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
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

產(chǎn)品描述

靶點(diǎn)

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

體外研究(In Vitro)
體外研究活性	Roscovitine作用于細(xì)胞周期蛋白依賴(lài)性激酶具有高效性和高度選擇性，作用于cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E和cdk5/p53時(shí)IC50分別為0.65,0.7,0.7和0.16 μM。納摩爾級(jí)Roscovitine作用于海星卵母細(xì)胞和海膽胚胎，可逆抑制在前中期間轉(zhuǎn)變, 在體外作用于非洲爪蟾卵提取物，抑制M期促進(jìn)因子活性和體外DNA合成,且抑制哺乳動(dòng)物細(xì)胞系增殖，IC50為16 μM。^[1] 濃度為7.5, 12.5和 25 mM的 Roscovitine作用于腎小球系膜細(xì)胞,導(dǎo)致CDK2活性分別降低25,50% 和100%，這種作用存在劑量依賴(lài)性。^[2] 最新研究顯示Roscovitine作用于盤(pán)基網(wǎng)柄菌，抑制cdk5激酶活性,細(xì)胞增殖,多細(xì)胞發(fā)展,和cdk5核轉(zhuǎn)運(yùn), 不會(huì)影響cdk5蛋白表達(dá)。^[3]
激酶實(shí)驗(yàn)	酶實(shí)驗(yàn)
激酶實(shí)驗(yàn)	激酶活性實(shí)驗(yàn)在30^oC下buffer C中進(jìn)行。從數(shù)據(jù)中除去空白值，在10分鐘的溫育期中測(cè)定滲透到蛋白受體中的磷酸摩爾數(shù)，來(lái)計(jì)算活性。對(duì)照組用適當(dāng)稀釋的DMSO處理。在一些情況下, SDS/PAGE后通過(guò)自動(dòng)射線照相術(shù)測(cè)定底物磷酸化。p34^cdc2/cyclin B通過(guò)親和色譜從 M期海星卵母細(xì)胞中純化。使用 1 mg 組蛋白Hl/mL,在15 μM [γ-³²P]ATP存在時(shí)進(jìn)行實(shí)驗(yàn)，終濃度為 30 μL。在 30^oC下溫育10分鐘, 25-μL上清液轉(zhuǎn)移到Whatman P81磷酸纖維素紙上, 20秒后, 用10mL磷酸/L水沖洗過(guò)濾器5次，每次至少5分鐘。濕式過(guò)濾器轉(zhuǎn)移到 6 mL閃爍管,加入5 mL ACS閃爍液，使用Packard 計(jì)數(shù)器測(cè)定放射性。測(cè)定在10分鐘溫育期中組蛋白H1滲透放入磷酸摩爾數(shù)評(píng)估激酶活性或者最大活性百分?jǐn)?shù)。感染不同桿狀病毒的sf9昆蟲(chóng)細(xì)胞抽提物中再生p33^cdk2/cyclin A和p33^cdk2/cyclinE。Cyclins A 和E是谷胱甘肽S-轉(zhuǎn)移酶融合蛋白，復(fù)合體從谷胱甘肽-瓊脂糖珠上純化。使用 1 mg/mL 組蛋白Hl/mL,在15 μM [γ-³²P]ATP存在時(shí)，進(jìn)行激酶活性實(shí)驗(yàn)10分鐘，終體積為30 μL，測(cè)定p34^cdc2/cyclin B激酶。p33^cdk5/p35從牛腦中純化,除了Mono S-色層分離一步法。 Superose 12柱的活性片段匯集，終濃度為25 μg 酶/mL。使用1 mg/mL 組蛋白Hl, 在15 μM [γ-³²P]ATP存在時(shí)，進(jìn)行激酶活性實(shí)驗(yàn)10分鐘，終體積為 30 μL，測(cè)定p34^cdc2/cyclin B激酶。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	白血病, 非小細(xì)胞肺癌,結(jié)腸癌, 中樞神經(jīng)系統(tǒng)腫瘤，惡性黑色素瘤,卵巢癌，腎癌, 前列腺癌，胸腺癌細(xì)胞系
	濃度	0.01到100 μM
	孵育時(shí)間	48小時(shí)
	方法	包括9種腫瘤類(lèi)型的60種人類(lèi)腫瘤細(xì)胞系培養(yǎng)24小時(shí)，然后用 0.01-100 μM Roscovitine持續(xù)處理48小時(shí)。進(jìn)行sulforhodaminine B蛋白實(shí)驗(yàn)測(cè)評(píng)毒性。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Roscovitine按50 mg/kg劑量作用于Ewing's肉瘤家族(ESFT)移植瘤，明顯抑制腫瘤生長(zhǎng)。^[4] Roscovitine作用于攜帶MCF7移植瘤的裸鼠，增強(qiáng)抗癌Doxorubicin抗癌效果,不會(huì)提高毒性，機(jī)制是使細(xì)胞周期停滯而不是引起凋亡。^[5]
動(dòng)物實(shí)驗(yàn)	Animal Models	右后側(cè)皮下注射A4573細(xì)胞的CD1 nu/nu鼠
	Dosages	≤50 mg/kg
	Administration	腹腔注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (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

參考文獻(xiàn)
[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(kāi)

參考文獻(xiàn)

[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.

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