Roscovitine (Seliciclib)

For research use only. Not for use in humans.

目录号:S1153 别名: CYC202, R-roscovitine

Roscovitine (Seliciclib) Chemical Structure

CAS No. 186692-46-6

Roscovitine (Seliciclib, CYC202, R-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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1573.18 现货
RMB 1212.83 现货
RMB 2104.83 现货
RMB 3829.77 现货
RMB 7938.98 现货
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客户使用Selleck生产的Roscovitine (Seliciclib)发表文献88篇:

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, R-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

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
LB771-HNC M{XpXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPIPGZKSzVyPUS4MlkzOTJizszN MkPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVQ4PjJxJ{7TRW5ITVJ:L3G+
LB2241-RCC MlT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHna[pNKSzVyPUS4MlYzODJizszN MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOFc3Oi9pPmPBUmdGWjxxYU6=
DU-4475 NF;VdWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3myWGlEPTB;NEiuOFk{PyEQvF2= NUHsWlNORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTR5NkKvK|5USU6JRWK8M4E,
LB2518-MEL MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrkNIFlUUN3ME20O{4xPDR6IN88US=> NX;De3hiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTR5NkKvK|5USU6JRWK8M4E,
NCI-H209 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILDe5NKSzVyPUS2MlAyOTVizszN MlHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVQ4PjJxJ{7TRW5ITVJ:L3G+
CGTH-W-1 M2nl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPZTJEyUUN3ME20OE46Pjl5IN88US=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOFc3Oi9pPmPBUmdGWjxxYU6=
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GI-ME-N M4\QWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPSfmFKSzVyPUSyMlY3PzFizszN MmH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVQ4PjJxJ{7TRW5ITVJ:L3G+
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NCI-H1882 NH;JNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXlTWM2OD12MD61PVk5KM7:TR?= Ml7zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVQ4PjJxJ{7TRW5ITVJ:L3G+
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MONO-MAC-6 MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYH5WYtrUUN3ME2zPE4zPDd5IN88US=> NVvYV4t5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTR5NkKvK|5USU6JRWK8M4E,
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ML-2 NI\SN2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrVTWM2OD1|Nz62O|EzKM7:TR?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOFc3Oi9pPmPBUmdGWjxxYU6=
OPM-2 NH;4c|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnWcW1KSzVyPUO3MlI6PDlizszN M4DaO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE1PzZ{Lze+V2FPT0WUPD;hQi=>
LU-139 NUjK[2R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTN5LkG4OVYh|ryP NYXIdZdyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTR5NkKvK|5USU6JRWK8M4E,
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MOLT-4 MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[wb2lEPTB;M{[uN|I4PiEQvF2= M3PuN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE1PzZ{Lze+V2FPT0WUPD;hQi=>
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TE-441-T MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDvPWNVUUN3ME2zOk4yOTR6IN88US=> NVfGSotmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTR5NkKvK|5USU6JRWK8M4E,
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TE-10 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\T[|N[UUN3ME2zOE46PDJ{IN88US=> MoHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVQ4PjJxJ{7TRW5ITVJ:L3G+
NCI-H2141 Mm\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfPTWM2OD1|ND62OVM{KM7:TR?= M3PoS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE1PzZ{Lze+V2FPT0WUPD;hQi=>
KGN NIDKcVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTMTWM2OD1|ND6yOVI1KM7:TR?= Ml7BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVQ4PjJxJ{7TRW5ITVJ:L3G+
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A673 MkLPdWhVWyCjc4PhfS=> MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY NGCy[ZNyUFSVIHHzd4F6 Mm\SdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? NGjGPHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 NFHlb3hyUFSVIHHzd4F6 M{nUfpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NEPIfo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MlyydWhVWyCjc4PhfS=> NIC5e2ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> M4HjZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NEnFfZNyUFSVIHHzd4F6 NWizfWZ[eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NWewNIFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MmKxdWhVWyCjc4PhfS=> MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NGW0XXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG5PVcxOid-M{CxPVk4ODJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Rb / p-CDK2 / CDK2 / Cyclin D1 / Cyclin A2 / ERα / ERβ/ AIB1 / PELP1 ; 

PubMed: 21834972     


(a) The model cells MCF7, MCF7-TamR, MCF7-HER2, and MCF7-LTLTca were treated with roscovitine and the status of cell cycle regulators and the estrogen receptor (ERα) signaling proteins was analyzed by western blotting. 

pT231-tau / pS202-tau / tau; 

PubMed: 30915013     


SH-SY5Y-(P301L) cells were exposed for 6 h to a range of roscovitine concentrations. Cells were harvested and proteins were resolved by SDS-PAGE followed by western blotting.

21834972 30915013
Immunofluorescence
E2F1 / FASN / Bmi1 / Cyclin D2 / CDK2 / CDK4 ; 

PubMed: 20890301     


Immunofluorescence analysis of E2F1, FASN, E2F1/Shh target Bmi1, cyclin D2, cdk 2, and cdk 4 in Pzp53med cells treated with DMSO (control) or the cdk inhibitor roscovitine (10 nM) for 18 hours.

CDK1 / Smek2 / FUBP1 / Cdc20 ; 

PubMed: 24534090     


A-D Validation of changes in chromatin affinity following Cdk inhibition of indicated candidates (2 h, 50 μM roscovitine) using Triton extraction and immunofluorescence (IF) in HeLa cells. Quantification of IF data was performed by measuring changes in signal intensities in Image J.

20890301 24534090
Growth inhibition assay
Cell viability; 

PubMed: 29996940     


Cell viability assay on OVCAR5, OAW42, SKOV3 and NL3507 cells treated with roscovitine (2, 5, 10, 20, 40 μM) up to 96 h. Each point represents the mean of three replicates. Error bars, SD

29996940
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]
- 合并

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]
- 合并
  • 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
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 71 mg/mL (200.31 mM)
Water Insoluble
Ethanol '6 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
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
储存条件 粉状
溶于溶剂
别名 CYC202, R-roscovitine

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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

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

相关CDK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID