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Roscovitine

別名: CYC202, Seliciclib, R-roscovitine

Roscovitine是一種有效的，選擇性CDK抑制劑，作用于Cdc2，CDK2和CDK5時，無細胞試驗中IC50分別為0.65 μM，0.7 μM和0.16 μM，對CDK4/6幾乎沒有作用。Phase 2。

Roscovitine Chemical Structure

Roscovitine Chemical Structure

CAS: 186692-46-6

規(guī)格 價格 庫存 購買數(shù)量
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
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Roscovitine相關(guān)產(chǎn)品

相關(guān)信號通路圖

CDK Signaling Pathways

CDK信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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 Roscovitine是一種有效的，選擇性CDK抑制劑，作用于Cdc2，CDK2和CDK5時，無細胞試驗中IC50分別為0.65 μM，0.7 μM和0.16 μM，對CDK4/6幾乎沒有作用。Phase 2。
靶點
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作用于細胞周期蛋白依賴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IC50分別為0.65,0.7,0.7和0.16 μM。納摩爾級Roscovitine作用于海星卵母細胞和海膽胚胎，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期促進因子活性和體外DNA合成,且抑制哺乳動物細胞系增殖，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性。[2] 最新研究顯示Roscovitine作用于盤基網(wǎng)柄菌，抑制cdk5激酶活性,細胞增殖,多細胞發(fā)展,和cdk5核轉(zhuǎn)運, 不會影響cdk5蛋白表達。[3]
激酶實驗 酶實驗
激酶活性實驗在30oC下buffer C中進行。從數(shù)據(jù)中除去空白值，在10分鐘的溫育期中測定滲透到蛋白受體中的磷酸摩爾數(shù)，來計算活性。對照組用適當稀釋的DMSO處理。在一些情況下, SDS/PAGE后通過自動射線照相術(shù)測定底物磷酸化。p34cdc2/cyclin B通過親和色譜從 M期海星卵母細胞中純化。使用 1 mg 組蛋白Hl/mL,在15 μM [γ-32P]ATP存在時進行實驗，終濃度為 30 μL。在 30oC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水沖洗過濾器5次，每次至少5分鐘。濕式過濾器轉(zhuǎn)移到 6 mL閃爍管,加入5 mL ACS閃爍液，使用Packard 計數(shù)器測定放射性。測定在10分鐘溫育期中組蛋白H1滲透放入磷酸摩爾數(shù)評估激酶活性或者最大活性百分數(shù)。感染不同桿狀病毒的sf9昆蟲細胞抽提物中再生p33cdk2/cyclin A和p33cdk2/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，進行激酶活性實驗10分鐘，終體積為30 μL，測定p34cdc2/cyclin B激酶。p33cdk5/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，進行激酶活性實驗10分鐘，終體積為 30 μL，測定p34cdc2/cyclin B激酶。
細胞實驗 細胞系 白血病, 非小細胞肺癌,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，胸腺癌細胞系
濃度 0.01到100 μM
孵育時間 48小時
方法

包括9種腫瘤類型的60種人類腫瘤細胞系培養(yǎng)24小時，然后用 0.01-100 μM Roscovitine持續(xù)處理48小時。進行sulforhodaminine B蛋白實驗測評毒性。
實驗圖片 檢測方法 檢測指標 實驗圖片 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。[4] Roscovitine作用于攜帶MCF7移植瘤的裸鼠，增強抗癌Doxorubicin抗癌效果,不會提高毒性，機制是使細胞周期停滯而不是引起凋亡。[5]
動物實驗 Animal Models 右后側(cè)皮下注射A4573細胞的CD1 nu/nu鼠
Dosages ≤50 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02649751 Terminated
Cystic Fibrosis
University Hospital Brest|ManRos Therapeutics|Cyclacel Pharmaceuticals Inc.
 February 22 2016 Phase 2

化學(xué)信息&溶解度

分子量 354.45 分子式

C19H26N6O
CAS號 186692-46-6 SDF Download Roscovitine SDF
Smiles CCC(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=CC=C3
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 71 mg/mL ( (200.31 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 71 mg/mL (200.31 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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.

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