Dinaciclib (SCH727965)

目录号:S2768 别名: PS-095760

Dinaciclib (SCH727965) Chemical Structure

Molecular Weight(MW): 396.49

Dinaciclib (SCH727965)是一种新型有效的CDK抑制剂,作用于CDK2CDK5CDK1CDK9,无细胞试验中IC50分别为1 nM,1 nM,3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Phase 3。

规格 价格 库存 购买数量  
RMB 2226.36 现货
RMB 1409.03 现货
RMB 3859.45 现货
RMB 5479.23 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用该产品的5个实验数据:

  • (a) Western blot for RALB-GTP, total RALB and GAPDH proteins in KG1 AML cells treated for 8 h with DMSO or dinaciclib (representative of three independent experiments).

    Oncogene, 2017, 36(23):3263-3273. Dinaciclib (SCH727965) purchased from Selleck.

    Bcl-xL depleted (Bcl-xL shRNA) or non-target shRNA (NT) carrying LNZ308 and U87 cells were seeded at 60% confluence, allowed to attach overnight, and treated with indicated concentrations of dinaciclib for 24 h. Cytosolic (upper panel) and mitochondrial (lower panel) fractions were prepared, and equal amounts of protein were separated by SDS-PAGE and subjected to Western blotting analysis with the indicated antibodies. Lack of HSP70 in the cytosolic fraction clearly demonstrates that the cytoplasmic cytochrome c, AIF, or smac/DIABLO did not result from the mitochondrial damage during the extraction process.

    Mol Carcinog, 2018, 57(4):469-482. Dinaciclib (SCH727965) purchased from Selleck.

  • (B) Cells were treated with dinaciclib (25 nM) or placebo for 24 h and stained with fluorescent antibodies against DAPI (blue), cyclin B1 (red) and α-tubulin (green). Cyclin B1 level was significantly reduced after treatment of dinaciclib in prophase cells of BHP7-13, WRO82-1 and 8505C. (C) Cells were treated with dinaciclib (25 nM) or placebo for 24 h and stained with fluorescent antibodies against DAPI (blue), Aurora A (red) and α-tubulin (green). Aurora A level was significantly reduced after treatment of dinaciclib in BHP7-13, WRO82-1 and 8505C cells in prophase. Scale bar, 10 μm.

    PLoS One, 2017, 12(2):e0172315 . Dinaciclib (SCH727965) purchased from Selleck.

    CDK4/6 inhibition has potent cytostatic effect in HER2-positive models. The indicated cells were treated with PD-0332991 (1 uM) or Dinaciclib (1 uM) for 96 hours and plates were stained with crystal violet.

    Genes Cancer 2014 5(7-8), 261-72. Dinaciclib (SCH727965) purchased from Selleck.

  • It is a viability curve of various cell lines treated the dinaciclib.

    Dinaciclib (SCH727965) purchased from Selleck.

产品安全说明书

CDK抑制剂选择性比较

生物活性

产品描述 Dinaciclib (SCH727965)是一种新型有效的CDK抑制剂,作用于CDK2CDK5CDK1CDK9,无细胞试验中IC50分别为1 nM,1 nM,3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Phase 3。
特性 [1]
靶点
CDK2 [1]
(Cell-free assay)
CDK5 [1]
(Cell-free assay)
CDK1 [1]
(Cell-free assay)
CDK9 [1]
(Cell-free assay)
1 nM 1 nM 3 nM 4 nM
体外研究

Dinaciclib抑制CDK1和CDK9 效果差不多,但是抑制CDK2和CDK5效果则分别强12和14倍。Dinaciclib作用于A2780细胞,有效抑制的DNA复制,抑制胸甘(dThd)DNA摄入,IC50为4 nM。Dinaciclib 浓度大于6.25 nM时,强抑制Rb在Ser 807/811位点磷酸化。Rb磷酸化的完全抑制与凋亡发生相关,通过用浓度大于6.25 nM 的Dinaciclib处理的细胞中p85 PARP裂解产物的出现来表示。 Dinaciclib有效作用于广谱人肿瘤细胞系。[1] 在羟基脲处理期间加入Dinaciclib,也抑制γ-H2AX累积,这种作用存在剂量依赖性。[2] Dinaciclib 抑制恶性黑色素瘤细胞增殖,使恶性黑色素瘤细胞发生大规模凋亡。[3]Dinaciclib诱导一些骨肉瘤 细胞系凋亡,包括抗Doxorubicin和Dasatinib的细胞。Dinaciclib 降低RNAP II 在 serine 2位点磷酸化,也降低CDK抑制剂p27Kip1在threonine 187位点磷酸化。加入12 nM 到40 nM Dinaciclib处理4小时或16小时,最易使磷酸化作用降低。Dinaciclib也降低Rb在serine 807/811位点磷酸化。Dinaciclib诱导mock-和p53-耗尽的U2OS细胞凋亡,凋亡程度相似。 [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CA46 NX;HT5M3SXCxcITvd4l{KEG|c3H5 MVSxNFAhdk1? MonxNlQhcA>? M3\MXYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M2mxV|I2Ojh7OEi3
Kasumi-1 MUDBdI9xfG:|aYOgRZN{[Xl? MYWxNFAhdk1? MlzMNlQhcA>? NV23cVVicW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MkXzNlUzQDl6OEe=
U937 MmnxSpVv[3Srb36gRZN{[Xl? M4rldlIwPS9zMDDuUS=> MkTjN{Bp NX24WIVp[myxY3vzJIlv\HWldHnvckBw\iC[QmCtNZMh[W6mIHTve45{fHKnYX2geIFz\2W2cx?= NF\VTYkzPDN4MkS2OS=>
8226 MVvGeY5kfGmxbjDBd5NigQ>? MlvFNk82NzFyIH7N NFz3UYE1KGh? NELVcotjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| NF\BTXgzPDN4MkS2OS=>
H929 M2\E[WZ2dmO2aX;uJGF{e2G7 NVHXRm1SOi93L{GwJI5O M3;rO|QhcA>? MYjicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NEPISVYzPDN4MkS2OS=>
K562 M2nDTmZ2dmO2aX;uJGF{e2G7 MVGxMlUwOy96IH7N NYfnbZpvPiCq MXzicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NHvDfmszPDN4MkS2OS=>
BaF3/Bcr-abl MknUSpVv[3Srb36gRZN{[Xl? NXqyPZk1OS53L{OvPEBvVQ>? M3;3TVYhcA>? MnG2Zoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? NGrRZWszPDN4MkS2OS=>
U937  M3\Zb2Z2dmO2aX;uJGF{e2G7 MnXwNk8yOCCwTR?= Mmm4N{Bp MoDCZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MYqyOFM3OjR4NR?=
1205Lu MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;pNVAwOzBibl2= NH3ZSZg4OiCq NH3JZ|hqdmirYnn0d{Bk\WyuIHfyc5d1cCCjbnSgd5Vzfmm4YXy= MWeyN|UzPzJ{NR?=
WM1366 MmPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:0NVAwOzBibl2= NFO1UWg4OiCq M1LoSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGGwZDDzeZJ3cX[jbB?= NEDofG8zOzV{N{KyOS=>
RD MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrQTWM2OD16LkKgcm0> MmTNNlI{OTV{NEC=
Rh41 M13s[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFyLkWgcm0> NEPwXXAzOjNzNUK0NC=>
Rh18 NY\xXFVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPkd|RKSzVyPUGwMlUhdk1? MU[yNlMyPTJ2MB?=
Rh30 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojLTWM2OD17IH7N NFnzPIIzOjNzNUK0NC=>
BT-12 NGiwfohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;ld2t1UUN3ME24MlUhdk1? NGH2eVkzOjNzNUK0NC=>
CHLA-266 Ml3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rONmlEPTB;Nz6zJI5O NYS5bVMyOjJ|MUWyOFA>
TC-71 NHnyT4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWixU|BFUUN3ME2zMlkhdk1? NFLBZmUzOjNzNUK0NC=>
CHLA-9 NEToXWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3iOHF6UUN3ME24JI5O MnzyNlI{OTV{NEC=
CHLA-10 NYnOSI5XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXiVIZDUUN3ME22MlMhdk1? NF7hVpMzOjNzNUK0NC=>
CHLA-258 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn73TWM2OD17Lkmgcm0> NFn5S|YzOjNzNUK0NC=>
GBM2 NYjn[YVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH24fXdKSzVyPU[uOUBvVQ>? MYOyNlMyPTJ2MB?=
NB-1643 MmSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jpNmlEPTB;Mz6zJI5O NXv2fWpoOjJ|MUWyOFA>
NB-EBc1 NFzq[IVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfxTWM2OD15IH7N NUDrR5JOOjJ|MUWyOFA>
CHLA-90 NFO3WY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e2OmlEPTB;Nz61JI5O MnLQNlI{OTV{NEC=
CHLA-136 M3y1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zSOWlEPTB;OT64JI5O M1PmZ|IzOzF3MkSw
NALM-6 NHPaWVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T0XWlEPTB;ND62JI5O M1i5SFIzOzF3MkSw
COG-LL-317 MnPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTZwNTDuUS=> NHzCSlUzOjNzNUK0NC=>
RS4;11 M{D5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTVwMTDuUS=> MVWyNlMyPTJ2MB?=
MOLT-4 MlnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXte4ZKSzVyPUmuN{BvVQ>? NEjwNYszOjNzNUK0NC=>
CCRF-CEM NG[yXZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG1TWM2OD13Lk[gcm0> MUCyNlMyPTJ2MB?=
Kasumi-1 NIjPW2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTRwNTDuUS=> M3nZNlIzOzF3MkSw
Karpas-299 M{TmS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrDTWM2OD1|Lkmgcm0> MnviNlI{OTV{NEC=
Ramos-RA1 M{fiUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTdwOTDuUS=> NYn5b|JiOjJ|MUWyOFA>
MIAPaCa-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoniO|IhcA>? M4fnSmdKPTB;MUCgcm0> M3;ke|IyPzZ6N{e5
Pa20C  NGPzN4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVW3NkBp MVPHTVUxRTJyIH7N MVqyNVc3QDd5OR?=
ML-1 NVOzXFlOSXCxcITvd4l{KEG|c3H5 MVWxMVExODBibl2= M1vWcVQhcA>? MX\pcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= MWeyNVc3QDd5Nx?=

... Click to View More Cell Line Experimental Data

体内研究 Dinaciclib 每天按8, 16, 32,和48 mg/kg 剂量腹腔注射处理 ,持续10天,导致肿瘤受抑制分别为70%, 70%, 89%,和 96%。Dinaciclib MED(最低有效剂量)约为小于8 mg/kg。Dinaciclib耐药性良好, 且最高剂量处理组中体重损失最高为5%。Dinaciclib 在体内具有抗癌活性,存在剂量依赖性,按低于MTD(最高耐受剂量)的剂量水平处理,几乎完全抑制肿瘤生长。Dinaciclib作用于小鼠,具有短暂的血浆半衰期。[1]

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]
+ 展开

Cyclin/CDK激酶实验:

设计从Sf9细胞中纯化的重组cyclin/CDK 全酶,产生表达特定cyclin 或CDK的杆状病毒。 在含 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 1 mM DTT,和 0.1 mM原钒酸钠的反应buffer中,Cyclin/CDK 复合体稀释成终浓度为 50 μg/mL。每种激酶反应中, 1 μg酶和 20 μL 2-μM 底物溶液 (组蛋白 H1衍生的一种生物素化的肽段) 混合,然后与10 μL 稀释的Dinaciclib结合。加入 50 μL 2 μM ATP和 0.1 μCi 33P-ATP反应开始。激酶反应在室温下进行1小时,然后加入 0.1% Triton X-100, 1 mM ATP, 5 mM EDTA, 和5 mg/mL 链霉亲和素包被的SPA 磁珠而终止反应。使用96-孔GF/B过滤板和Filtermate广谱收集器 收集SPA 磁珠。用 2 M NaCl 冲洗磁珠两遍,然后用含磷酸的2 M NaCl 再冲洗两遍。使用TopCount 96孔液体闪烁计数器测定信号。
细胞实验:[1]
+ 展开
  • Cell lines: A2780细胞
  • Concentrations: 0 μM-5 μM
  • Incubation Time: 24小时
  • Method: A2780 细胞培养在含10%FBS的DMEM培养基上,每周移动两次,通过使用胰蛋白酶-EDTA分离单细胞层。在96孔Cytostar-T板上每孔加入 100 μL A2780细胞 (5 ×103个),然后在37oC下温育16到24小时。Dinaciclib 在含2% 14C标记 dThd的完全培养基上连续稀释。培养基从 Cytostar T板上转移,按一式四份加入200 μL 多种Dinaciclib 稀释液,然后细胞在37oC下温育24小时。使用闪烁亲近法测定,在TopCoun上测量累积的放射性标记物渗透率。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 携带A2780肿瘤的裸鼠
  • Formulation: 20%羟丙基-β-环糊精
  • Dosages: 8 mg/kg, 16 mg/kg, 32 mg/kg,和 48 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 26 mg/mL warmed (65.57 mM)
Ethanol 8 mg/mL warmed (20.17 mM)
Water Insoluble
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):
2% DMSO+30% PEG 300+ddH2O
10mg/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 396.49
化学式

C21H28N6O2

CAS号 779353-01-4
稳定性 powder
in solvent
别名 PS-095760

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 (g) = 浓度 (mol/L) x 体积 (L) 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

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02684617 Recruiting rrCLL|rrMM|rrDLBCL Merck Sharp & Dohme Corp. March 29 2016 Phase 1
NCT03484520 Recruiting Acute Myeloid Leukemia (AML) AbbVie|Merck Sharp & Dohme Corp. July 23 2018 Phase 1
NCT01624441 Completed Estrogen Receptor Negative|HER2/Neu Negative|Male Breast Carcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer AJCC v6 and v7|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) August 21 2012 Phase 1
NCT01676753 Recruiting Advanced or Metastatic Breast Cancer|Triple Negative Breast Cancer Jo Chien|Merck Sharp & Dohme Corp.|University of California San Francisco June 2016 Phase 1
NCT01650727 Completed Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Merck Sharp & Dohme Corp. October 2012 Phase 1
NCT01580228 Completed Chronic Lymphocytic Leukemia (CLL) Merck Sharp & Dohme Corp. August 2012 Phase 3

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:

    I want to know how to reconstitute the inhibitor for in vivo studies?

  • 回答:

    S2768 (SCH727965) in 15% Captisol at 8 mg/ml is a suspension for oral administration. And it can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as a clear solution for injection.

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

相关CDK产品

Tags: 购买Dinaciclib (SCH727965) | Dinaciclib (SCH727965)供应商 | 采购Dinaciclib (SCH727965) | Dinaciclib (SCH727965)价格 | Dinaciclib (SCH727965)生产 | 订购Dinaciclib (SCH727965) | Dinaciclib (SCH727965)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID