Roscovitine

别名: CYC202, Seliciclib, R-roscovitine

Roscovitine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。

Roscovitine Chemical Structure

Roscovitine Chemical Structure

CAS: 186692-46-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1573.18 现货
10mg 1212.83 现货
25mg 2104.83 现货
50mg 3829.77 现货
200mg 7938.98 现货
1g 13677.3 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

Roscovitine相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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
点击查看更多细胞系数据

生物活性

产品描述 Roscovitine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(In Vitro)
体外研究活性

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]

激酶实验 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 细胞系 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
浓度 0.01到100 μM
孵育时间 48小时
方法

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。

实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性

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]

动物实验 Animal Models 右后侧皮下注射A4573细胞的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

化学信息&溶解度

分子量 354.45 分子式

C19H26N6O

CAS号 186692-46-6 SDF Download Roscovitine SDF
Smiles CCC(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=CC=C3
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 71 mg/mL ( (200.31 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 71 mg/mL (200.31 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们

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.

Tags: buy Roscovitine | Roscovitine supplier | purchase Roscovitine | Roscovitine cost | Roscovitine manufacturer | order Roscovitine | Roscovitine distributor
在线咨询
联系我们