Dinaciclib (SCH727965)

目录号:S2768 别名: PS-095760

仅限科研使用

Dinaciclib (SCH727965, PS-095760) 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。Dinaciclib 可通过激活caspases 8caspases 9来诱导细胞凋亡。Phase 3。

Dinaciclib (SCH727965) Chemical Structure

CAS: 779353-01-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2226.36 现货
RMB 1409.03 现货
RMB 5479.23 现货
RMB 13677.3 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

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

客户使用Selleck生产的Dinaciclib (SCH727965)发表文献108篇:

产品安全说明书

CDK抑制剂选择性比较

相关CDK产品

生物活性

产品描述 Dinaciclib (SCH727965, PS-095760) 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。Dinaciclib 可通过激活caspases 8caspases 9来诱导细胞凋亡。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 MlXhRZBweHSxc3nzJGF{e2G7 NYHmSohqOTByIH7N M2j5flI1KGh? NGDvUXpqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ6OUi4O{c,OjV{OEm4PFc9N2F-
Kasumi-1 NUDBbIg{SXCxcITvd4l{KEG|c3H5 NETCTJgyODBibl2= MXqyOEBp M{jVW4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M1ey[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mki5PFg4Lz5{NUK4PVg5PzxxYU6=
U937 MV;GeY5kfGmxbjDBd5NigQ>? MWqyM|UwOTBibl2= NVi3R3U3OyCq NUiwVWZP[myxY3vzJIlv\HWldHnvckBw\iC[QmCtNZMh[W6mIHTve45{fHKnYX2geIFz\2W2cx?= Ml3lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
8226 MX3GeY5kfGmxbjDBd5NigQ>? MnvVNk82NzFyIH7N M17rZVQhcA>? Mn3HZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
H929 MUDGeY5kfGmxbjDBd5NigQ>? NXTzW3N{Oi93L{GwJI5O M1\rNVQhcA>? M4SzTIJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? Mnm1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
K562 M{jLV2Z2dmO2aX;uJGF{e2G7 NWn5NnZlOS53L{OvPEBvVQ>? NFyzXm83KGh? NIe2UYxjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| NGj1fJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
BaF3/Bcr-abl MXPGeY5kfGmxbjDBd5NigQ>? MYKxMlUwOy96IH7N MkjLOkBp MXzicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NWD0e|RWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
U937  NGPWNJdHfW6ldHnvckBCe3OjeR?= NFTSbVMzNzFyIH7N M4T5e|MhcA>? M1jvd4Jtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NIribXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
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BT-12 NUXp[VdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\oTWM2OD16LkWgcm0> NHSzRVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
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TC-71 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:xR2lEPTB;Mz65JI5O Mom0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-9 NXT1XYRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRThibl2= Mm\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-10 NXSyTVJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37oXGlEPTB;Nj6zJI5O NYXvT3I5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-258 NHrzUVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHweGFKSzVyPUmuPUBvVQ>? NVP4U5dSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
GBM2 NHv1N5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfObmh5UUN3ME22MlUhdk1? NFfBSYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
NB-1643 NGTDWYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnkTWM2OD1|LkOgcm0> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
NB-EBc1 NUCwcZpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTdibl2= NXLZSXMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-90 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\T[GlEPTB;Nz61JI5O MnHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-136 Moe2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInJfHVKSzVyPUmuPEBvVQ>? NYT4NJNTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
NALM-6 M4HsOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTRwNjDuUS=> MmjXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
COG-LL-317 Mn;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1juS2lEPTB;Nj61JI5O M4DZN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
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MOLT-4 MlXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHUTWpKSzVyPUmuN{BvVQ>? Mn7yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CCRF-CEM MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLQTotpUUN3ME21MlYhdk1? MonVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Kasumi-1 M1O1NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LnfmlEPTB;ND61JI5O Mn;iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Karpas-299 MnWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTNwOTDuUS=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Ramos-RA1 NIDHXWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jJS2lEPTB;Nz65JI5O M3PXN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
MIAPaCa-2 M3nVfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS3WodyPzJiaB?= MX;HTVUxRTFyIH7N M17S[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c6Lz5{MUe2PFc4QTxxYU6=
Pa20C  NET0VXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPJXGs4OiCq M33y[2dKPTB;MkCgcm0> NWTjOJUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3Olg4PzlpPkKxO|Y5Pzd7PD;hQi=>
ML-1 NEjzWnZCeG:ydH;zbZMhSXO|YYm= NF7oT4EyNTFyMECgcm0> M2jQOVQhcA>? M4nPVolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 NILHXG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe2PFc4Pyd-MkG3Olg4Pzd:L3G+
Cytotoxicity assay M3nJN21FSS2PQj20N|Y> MVm3NkBpenN? MnHjTWM2OCB;IECuNFA2KM7:TR?= NXfoZ3V6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MYfOR2kuUDl{OR?= MWq3NkBpenN? M1PwR2lEPTBiPTCwMlAxPSEQvF2= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NGDBeYdOTEFvTVKtNlMy NG\PUIY4OiCqcoO= M4L4O2lEPTBiPTCwMlAxPSEQvF2= NWDDboJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NUj4O48{W0tvRWOtNS=> NYi1OlNmPzJiaILz NVzKTVB{UUN3MDC9JFAvODB3IN88US=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NFTLVYRCPjd| NE\FNWE4OiCqcoO= NXHld2RsUUN3MDC9JFAvODB3IN88US=> M1fVU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MXHTT{1DWi1| NIjMTY84OiCqcoO= NFLLb45KSzVyIE2gNE4xODVizszN NWP2ZXpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay Ml\NUW5PTy2KT2O= MXy3NkBpenN? NYnaT2prUUN3MDC9JFAvODB3NTFOwG0> NHXDS2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NFLpenVUUy2XVD2x MY[3NkBpenN? M1nheWlEPTBiPTCwMlAxPiEQvF2= NEnzPIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NGTI[VVWOjZ4 NVTXRWp5PzJiaILz NXK5eYxJUUN3MDC9JFAvODB4IN88US=> MnvFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay MYfSVG1KOTh{Mk[= MXu3NkBpenN? NIfITFhKSzVyIE2gNE4xODlizszN NWPEZZdyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NWXrSm13W1d6N{K= NYPDPXB{PzJiaILz NIDWXXhKSzVyIE2gNE4xODl3IN88US=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MVjUOFdF NVjmemNPPzJiaILz NILtfINKSzVyIE2gNE4xOSEQvF2= M4nMSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Apoptosis assay NIDrcVVCPjd| MYiyOEBpenN? M2f3ZWVEPTBiPTCwMlAyOSEQvF2= M1zhZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MW\NR2Y4 NVvERVh7PzJiaILz M1nxTGlEPTBiPTCwMlAzKM7:TR?= M2nIWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Function assay NGDySFFU\jl? M{e3bGlEPTBiPTCwMlA4OiEQvF2= M4jLNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{SxPFU{Lz5{Nke0NVg2OzxxYU6=
Function assay MUfz[lk> NWDuUndWUUN3MDC9JFAvODB{IN88US=> MkjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NUG1NFUoRjJ4OEWxOVA2RC:jPh?=
Function assay M1TycHNnQQ>? NHzveoMyKGi{ NEX1WnpKSzVyIE2gNE4xODFizszN MkLMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M2DMfXNnQQ>? M{O0N|EhcHJ? NWXpXGtnUUN3MDC9JFAvODBzIN88US=> NIfvWWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay M1mwOXNnQQ>? NF\xZWUyKGi{ MYLJR|UxKD1iMD6wNFEh|ryP NXvKR2w4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay Ml\5V4Y6 MnvtNUBpeg>? MX;JR|UxKD1iMD6wNFEh|ryP MmnGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay MoDJV4Y6 MmLrNUBpeg>? NIj4Vo1KSzVyIE2gNE4xODNizszN Mn3qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay NVG4S3RnW2Z7 NVm5cpZlOSCqch?= NHW0OHpKSzVyIE2gNE4xODNizszN M2rMfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay NIniXW1U\jl? MoGyNUBpeg>? NYfZWWxtUUN3MDC9JFAvODB2IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay NIjqbJhU\jl? MV:xJIhz M1rYN2lEPTBiPTCwMlAxPCEQvF2= M1TPRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay NX7sb4VJW2Z7 NEfkTFgyOCC3TR?= MV7JR|UxKD1iMD6wNFQh|ryP MonOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl|Mkm2OVgoRjJ7M{K5OlU5RC:jPh?=
Function assay MX\T[lk> MkHwNUBpeg>? NVv1dllqUUN3MDC9JFAvODBzIN88US=> MnTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzN|goRjJ7OEWzN|M5RC:jPh?=
Function assay NFX6WXpU\jl? NGrmeYwyKGi{ MX7JR|UxKD1iMD6wNFEh|ryP MkLGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzN|goRjJ7OEWzN|M5RC:jPh?=
Function assay NHTPOZBU\jl? NHG4RZIyKGi{ NGD4d2RKSzVyIE2gNE4xODNizszN MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Function assay NFi3ZY9U\jl? MkLENUBpeg>? M2jUfWlEPTBiPTCwMlAxPCEQvF2= NYDHbZE3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Antiproliferative assay MnP0UW9NVTF| MlHJO|IhcHK| NXnkWIRMT0l3MDC9JFAvODB|MzFOwG0> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MUXNSWMy M3LXe|czKGi{cx?= Ml3ZS2k2OCB;IECuNFA{PiEQvF2= NHn4UW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NGTOXJZOV0yPMUS= NV3Ce2w{PzJiaILz MULHTVUxKD1iMD6wNFQ2KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MknoR29NVzJyNR?= MVK3NkBpenN? MkH4S2k2OCB;IECuNFA3QCEQvF2= M{faTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NFXwem1JVDZy NEfVems4OiCqcoO= MUTHTVUxKD1iMD6wNFgh|ryP NFPCUok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay M2XFXHJidW:| NH;obVI4OiCqcoO= MXLHTVUxKD1iMD6wNFg3KM7:TR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NWfaTlk1T0mVVGSx NILHd|E4OiCqcoO= M1HLVmdKPTBiPTCwMlAxQDhizszN NVixbnB4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay MWTVPVM4 NG\wbmY4OiCqcoO= NIXTS4NIUTVyIE2gNE4xOSEQvF2= M1nRSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay Ml;SRVQ{OQ>? MmHNO|IhcHK| NHvZXIlIUTVyIE2gNE4xOTFizszN NXnpT25URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay NXO5RXhlW0uPMR?= NILoUmc4OiCqcoO= NEO1dVBIUTVyIE2gNE4xOTFizszN NF\PbYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay M2D0NW1GSzJ? Mn7JO|IhcHK| MUTHTVUxKD1iMD6wNVEh|ryP NWrrcZI6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay NHvnXIdCOzd3 MXq3NkBpenN? M1TpTWdKPTBiPTCwMlAyOSEQvF2= M1X4UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MXXPR2kuSU2OMx?= NFuw[GU4OiCqcoO= NVHU[Wd{T0l3MDC9JFAvODF|IN88US=> NF\NdnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NV;ZR5B[SkVqMjmtUVE4 MoHTO|IhcHK| NGWxclVIUTVyIE2gNE4xOjFizszN MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NXPMdmZQS0iR Mn3NO|IhcHK| M3q4SGdKPTBiPTCwMlE3KM7:TR?= NFHkbHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Function assay M3LFWm5EUS2KOUK5 Mn7WNE4xODVidV2= Ml20NlQhcHK| MXXJcohq[mm2aX;uJI9nKEOGS{KtcYVlcWG2ZXSgVoIheGixc4Doc5J6dGG2aX;uJIF1KFOncjC4NFcwQDFzIHnuJIh2dWGwIF7DTU1JQTJ7IHPlcIx{KGG2IECuNFA2KHWPIHHmeIVzKDJ2IHjyd{BjgSCrbX31co9jdG:2dHnu[{BidmGueYPpdy=> NHnScGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Function assay MXXBOlc{ MVWwMlA2KHWP M{LvSFI1KGi{cx?= NIOzdVJKdmirYnn0bY9vKG:oIFPET|IudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IGPldkA5ODdxOEGxJIlvKGi3bXHuJGE3PzNiY3XscJMh[XRiMD6wOUB2VSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= M2nnWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Apoptosis assay NXm1NZdIVUWFMR?= NYD1PW5nOC5yMTD1US=> NXrlcHpHOjRiaILz MYTJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2HQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hVUOOLUGgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> MlftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NHnjTGpJVDZy NEDOcJAxNjBzIIXN MoPPNlQhcHK| M33HZmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCPQ1ytNUBt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay MYPNWlQuOTF? MknkNE4xOSC3TR?= MVmyOEBpenN? NYXMWmJFUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNWlQuOTFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gZ{1OYUNibHX2[Ywh[XRiMD6wNUB2VSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay Mk\yUWVEOQ>? MV6wMlAyKHWP Mn7mNlQhcHK| NUeyNnlSUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNSWMyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHOtUXlEKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| NFG5dGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Apoptosis assay Mmf0UXY1NTFz MYqwMlAyKHWP M3;idlI1KGi{cx?= MX7JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2YND2xNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCPQ1ytNUBt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay Mn7UTGw3OA>? MUSwMlAyKHWP MkWxNlQhcHK| MnX3TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGNvTWnDJIxmfmWuIHH0JFAvODFidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Cytotoxicity assay MW\VNm9U NX;QUpJJQTZiaILz NW[wRYF6UUN3MDC9JFAvODB4IN88US=> NFK5OHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OESwM{c,S2iHTVLMQE9iRg>?
Function assay NEey[mxWOk:V M{frPFEhcHJ? MlPqTWM2OCB;IECuNFA4KM7:TR?= Mn:3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh2MD:nQmNpTU2ETEyvZV4>
Assay
Methods Test Index PMID
Western blot Mcl-1 / Bcl-2 / Bcl-xl / Bax / Bak / PUMA / Noxa Cleaved PARP / c-Myc Survivin RNAP II (P-Ser2/P-Ser5) 28714472 25289887 28207834
Growth inhibition assay Cell viability Cell viability 27378523 28361959
Immunofluorescence cyclin B1 / α-tubulin / Aurora A OCT4 28207834 28361959
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]
  • 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]
  • 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。
动物实验:[1]
  • Animal Models: 携带A2780肿瘤的裸鼠
  • Dosages: 8 mg/kg, 16 mg/kg, 32 mg/kg,和 48 mg/kg
  • Administration: 腹腔注射

溶解度(25°C)

体外

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
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03484520 Active not recruiting Drug: Venetoclax|Drug: Dinaciclib Cancer - Acute Myeloid Leukemia AbbVie|Merck Sharp & Dohme LLC July 23 2018 Phase 1
NCT01434316 Recruiting Drug: Dinaciclib|Drug: Veliparib Advanced Malignant Solid Neoplasm National Cancer Institute (NCI) November 1 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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.

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