Dinaciclib (SCH727965)

For research use only. Not for use in humans.

目录号:S2768 别名: PS-095760

Dinaciclib (SCH727965) Chemical Structure

CAS No. 779353-01-4

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。

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
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客户使用Selleck生产的Dinaciclib (SCH727965)发表文献93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 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 MYXBdI9xfG:|aYOgRZN{[Xl? MXexNFAhdk1? M360O|I1KGh? MVvpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ6OUi4O{c,OjV{OEm4PFc9N2F-
Kasumi-1 NYq0RlB[SXCxcITvd4l{KEG|c3H5 MWOxNFAhdk1? MYWyOEBp NWH3W2NkcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M3zBR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mki5PFg4Lz5{NUK4PVg5PzxxYU6=
U937 M{PP[mZ2dmO2aX;uJGF{e2G7 Ml2yNk82NzFyIH7N NYrVfmR5OyCq MnLQZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MljxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
8226 NITLS3lHfW6ldHnvckBCe3OjeR?= M17DOlIwPS9zMDDuUS=> MV60JIg> M1KwOYJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? M1HFe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
H929 MX\GeY5kfGmxbjDBd5NigQ>? MoXtNk82NzFyIH7N M3HBeVQhcA>? M3m4ToJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NFfweno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
K562 NXzJNJp6TnWwY4Tpc44hSXO|YYm= MmTzNU42NzNxODDuUS=> NGTU[G43KGh? MVjicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
BaF3/Bcr-abl NWHiV|J7TnWwY4Tpc44hSXO|YYm= NVq5XGRSOS53L{OvPEBvVQ>? Mn\0OkBp NWn2NXAz[myxY3vzJIlv\HWldHnvckBw\iC[QmCtNZMh[W6mIHTve45{fHKnYX2geIFz\2W2cx?= MoOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
U937  NILl[lZHfW6ldHnvckBCe3OjeR?= Mn7lNk8yOCCwTR?= M2HVbVMhcA>? MUTicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NVK1eog1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
1205Lu NF\RR5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGxXW8yOC9|MDDuUS=> M4G4[lczKGh? MknrbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W6mIIP1dpZqfmGu MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV{N{KyOUc,OjN3MkeyNlU9N2F-
WM1366 NHLSSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzjNVAwOzBibl2= MUS3NkBp MWHpcohq[mm2czDj[YxtKGe{b4f0bEBidmRic4Xyeol3[Wx? NV7EWYVxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NlczOjVpPkKzOVI4OjJ3PD;hQi=>
RD MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRThwMjDuUS=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Rh41 M3Xxdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHDOo1KSzVyPUGwMlUhdk1? NXTybWdJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Rh18 NIrjR5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ruRmlEPTB;MUCuOUBvVQ>? NGPYToE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Rh30 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjpVIdKSzVyPUmgcm0> MnHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
BT-12 NVTrSlkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LUS2lEPTB;OD61JI5O MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-266 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvPTWM2OD15LkOgcm0> NX7UWGFpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
TC-71 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzYTWM2OD1|Lkmgcm0> NV;xcmE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-9 M4fLe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrxeppFUUN3ME24JI5O NF;EXZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-10 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnSOJlPUUN3ME22MlMhdk1? NE\1dnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-258 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTlwOTDuUS=> NEHzPWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
GBM2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHe2ZWFKSzVyPU[uOUBvVQ>? NGLCU3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
NB-1643 M2X5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTNwMzDuUS=> MlWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NB-EBc1 Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HI[2lEPTB;NzDuUS=> MmXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-90 M37SWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPwR2F[UUN3ME23MlUhdk1? NHzkNVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-136 NXHucnFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnIbHBKSzVyPUmuPEBvVQ>? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
NALM-6 M4fkSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7kTWM2OD12Lk[gcm0> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
COG-LL-317 NUfwWIc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTZwNTDuUS=> M2X3XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
RS4;11 NInyUGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonMTWM2OD13LkGgcm0> M3j6UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
MOLT-4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLMTWM2OD17LkOgcm0> NF3vbWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CCRF-CEM M3H5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPUVm9KSzVyPUWuOkBvVQ>? MmnHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Kasumi-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDoTWM2OD12LkWgcm0> NV3p[GZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Karpas-299 M3X5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjSTWM2OD1|Lkmgcm0> NV;K[JVlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Ramos-RA1 NUK3SnV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjoVm5KSzVyPUeuPUBvVQ>? M{HsOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
MIAPaCa-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjhNoFbPzJiaB?= NWW2XVROT0l3ME2xNEBvVQ>? M2LwW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c6Lz5{MUe2PFc4QTxxYU6=
Pa20C  M4Hj[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\1doY4OiCq NIWzN4RIUTVyPUKwJI5O MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd4OEe3PUc,OjF5Nki3O|k9N2F-
ML-1 MorIRZBweHSxc3nzJGF{e2G7 MnnINU0yODByIH7N M1noOlQhcA>? Ml3DbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NXX1VJNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3Olg4PzdpPkKxO|Y5Pzd5PD;hQi=>
Cytotoxicity assay NXnaNIlCVUSDLV3CMVQ{Pg>? NHfrWXo4OiCqcoO= NEmxcIFKSzVyIE2gNE4xODVizszN M3zMWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MV3OR2kuUDl{OR?= M{G2ZlczKGi{cx?= NFrNcVlKSzVyIE2gNE4xODVizszN MofEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay MVHNSGEuVUJvMkOx NFG5NHc4OiCqcoO= NWTYPFMyUUN3MDC9JFAvODB3IN88US=> NXfIdG41RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NXTTUnczW0tvRWOtNS=> NVTiTZd1PzJiaILz MYnJR|UxKD1iMD6wNFUh|ryP MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MoXURVY4Ow>? MYG3NkBpenN? NV3lZ2JrUUN3MDC9JFAvODB3IN88US=> M4TQdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay NF\jS25UUy2EUj2z NHmxcZg4OiCqcoO= MljhTWM2OCB;IECuNFA2KM7:TR?= NIrKOZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay MXTNUm5INUiRUx?= NFiz[VA4OiCqcoO= NGrvT4NKSzVyIE2gNE4xODV3IN88US=> NXyw[VlLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NVnMWHh5W0tvVWStNS=> MmDZO|IhcHK| MkLnTWM2OCB;IECuNFA3KM7:TR?= NXq1fnN1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay M1v3fXUzPjZ? MmrCO|IhcHK| MlXwTWM2OCB;IECuNFA3KM7:TR?= MoDPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay NX;iSIViWlCPSUG4NlI3 NWm2eottPzJiaILz NXnJN4JtUUN3MDC9JFAvODB7IN88US=> M2THc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MVnTW|g4Og>? Mm\aO|IhcHK| M4HtbGlEPTBiPTCwMlAxQTVizszN MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NWm5NZdYXDR5RB?= NF7PTHY4OiCqcoO= MXfJR|UxKD1iMD6wNUDPxE1? Ml7IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Apoptosis assay M{XXPWE3PzN? NH\6eGQzPCCqcoO= NGL5eWdGSzVyIE2gNE4xOTFizszN MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NGnXTY1OS0Z5 M3PCRVczKGi{cx?= M2\yfWlEPTBiPTCwMlAzKM7:TR?= NHTtVZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Function assay NFL2NllU\jl? NVHZOItKUUN3MDC9JFAvODd{IN88US=> MnvpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5NEG4OVMoRjJ4N{SxPFU{RC:jPh?=
Function assay M3\GcJNnQQ>? M1H0VmlEPTBiPTCwMlAxOiEQvF2= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh3MUWwOUc,OjZ6NUG1NFU9N2F-
Function assay Ml\4V4Y6 MUGxJIhz MXTJR|UxKD1iMD6wNFEh|ryP MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay NULhWmtDW2Z7 NHLPfmEyKGi{ NXrqZ2l{UUN3MDC9JFAvODBzIN88US=> NF[5O4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay M335e3NnQQ>? MnPZNUBpeg>? NFT0b4VKSzVyIE2gNE4xODFizszN M{nSWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay MWXT[lk> MoDINUBpeg>? NG\lS4VKSzVyIE2gNE4xODFizszN NU\RdVFPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay NEjaPZRU\jl? MX6xJIhz NXXlZ25mUUN3MDC9JFAvODB|IN88US=> M3TIclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay MnHKV4Y6 MlLkNUBpeg>? NGHSZ4hKSzVyIE2gNE4xODNizszN M{KyRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay M1HuVXNnQQ>? NG\kNm0yKGi{ NFHWcGxKSzVyIE2gNE4xODRizszN MlP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay NVf5UppQW2Z7 M3;reVEhcHJ? MY\JR|UxKD1iMD6wNFQh|ryP NYDxc5VrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay MVnT[lk> M36zclExKHWP M2iyRWlEPTBiPTCwMlAxPCEQvF2= M3TOc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{K5OlU5Lz5{OUOyPVY2QDxxYU6=
Function assay NHm1VJdU\jl? NXv4R5U1OSCqch?= MmHlTWM2OCB;IECuNFAyKM7:TR?= NV33elk2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Function assay NYXSclZ5W2Z7 NFzL[HcyKGi{ NF34SWtKSzVyIE2gNE4xODFizszN M{TjNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|M5Lz5{OUi1N|M{QDxxYU6=
Function assay M{jKeHNnQQ>? MoPjNUBpeg>? NE[4foVKSzVyIE2gNE4xODNizszN MkO1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzN|goRjJ7OEWzN|M5RC:jPh?=
Function assay NGi1NmZU\jl? M{PwUFEhcHJ? NFK0WXJKSzVyIE2gNE4xODRizszN NIX1b5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N|M{QCd-Mkm4OVM{Ozh:L3G+
Antiproliferative assay MYDNU2xOOTN? NYLSO2p4PzJiaILz MnrkS2k2OCB;IECuNFA{OyEQvF2= NF;qWlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MVvNSWMy MoXXO|IhcHK| Ml[2S2k2OCB;IECuNFA{PiEQvF2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MVfNU2xOOTR? M4DxeFczKGi{cx?= MoPHS2k2OCB;IECuNFA1PSEQvF2= M4C5elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MXvDU2xQOjB3 MWe3NkBpenN? Mkf4S2k2OCB;IECuNFA3QCEQvF2= M4PWT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MX7IUFYx MnjzO|IhcHK| MWHHTVUxKD1iMD6wNFgh|ryP NIf3N2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NVTaeHZiWmGvb4O= MX[3NkBpenN? M4fkcmdKPTBiPTCwMlAxQDZizszN NF;4V4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MXTHTXNVXDF? M2nOXlczKGi{cx?= MlryS2k2OCB;IECuNFA5QCEQvF2= NWjuPZB5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay NFTMb2pWQTN5 M1vHOVczKGi{cx?= NFvaVJJIUTVyIE2gNE4xOSEQvF2= NIDYeVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MoPzRVQ{OQ>? NXXpZodEPzJiaILz NH\IT3NIUTVyIE2gNE4xOTFizszN MlW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NHfqbnZUU01z NH\nU3I4OiCqcoO= Mn3IS2k2OCB;IECuNFEyKM7:TR?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay M4XWfG1GSzJ? NVXp[VFXPzJiaILz NVXxUHRET0l3MDC9JFAvODFzIN88US=> NHn1e2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay Mn\SRVM4PQ>? NVf4bldkPzJiaILz NI\6U3NIUTVyIE2gNE4xOTFizszN MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NYLDSZJSV0OLLVHNUFM> M{fud|czKGi{cx?= M4G3fWdKPTBiPTCwMlAyOyEQvF2= MmXFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MWrCSUgzMS2PMUe= M3THTVczKGi{cx?= NGjQNItIUTVyIE2gNE4xOjFizszN M2XBflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MoPHR2hQ M4jrUFczKGi{cx?= Mn;0S2k2OCB;IECuNVYh|ryP M4O3UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Function assay NVzjeIsxVkOLLVi5Nlk> NHrlU4UxNjByNTD1US=> MV:yOEBpenN? MYTJcohq[mm2aX;uJI9nKEOGS{KtcYVlcWG2ZXSgVoIheGixc4Doc5J6dGG2aX;uJIF1KFOncjC4NFcwQDFzIHnuJIh2dWGwIF7DTU1JQTJ7IHPlcIx{KGG2IECuNFA2KHWPIHHmeIVzKDJ2IHjyd{BjgSCrbX31co9jdG:2dHnu[{BidmGueYPpdy=> NHLVWXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Function assay NH\BOpRCPjd| M1SwelAvODVidV2= M13NR|I1KGi{cx?= M{\OTWlvcGmkaYTpc44hd2ZiQ1TLNk1u\WSrYYTl[EBT[iCyaH;zdIhwenmuYYTpc44h[XRiU3XyJFgxPy96MUGgbY4hcHWvYX6gRVY4OyClZXzsd{BifCByLkC1JJVOKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91fGmwZzDhcoFtgXOrcx?= Ml;xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Apoptosis assay NV3hdI53VUWFMR?= M3O4OVAvODFidV2= NUXmPIlVOjRiaILz NUTxNmJ3UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNSWMyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIF3DUE0yKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| Mo[xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay MmOzTGw3OA>? M2HyZlAvODFidV2= NGD1[XIzPCCqcoO= MXTJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hVUOOLUGgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> M1rJT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Apoptosis assay MULNWlQuOTF? MknpNE4xOSC3TR?= M1P2SVI1KGi{cx?= MnOyTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPVkStNVEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iYz3NXWMhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? MkfFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NITpRnBOTUNz M1fwN|AvODFidV2= M1PaeFI1KGi{cx?= MXrJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2HQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[y2PWVOgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> M2f0bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Apoptosis assay MnL5UXY1NTFz NIPrOHoxNjBzIIXN Mo\6NlQhcHK| MmnCTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPVkStNVEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iTVPMMVEhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay M{XncWhNPjB? M{XHTVAvODFidV2= MXSyOEBpenN? M3fx[Wlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClLV3ZR{Bt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? NYPk[4V7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Cytotoxicity assay NVTqS2ZWXTKRUx?= NH\VTnM6PiCqcoO= Mnn6TWM2OCB;IECuNFA3KM7:TR?= NILUZ2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OESwM{c,S2iHTVLMQE9iRg>?
Function assay MWHVNm9U NUXu[GpiOSCqch?= MYnJR|UxKD1iMD6wNFch|ryP M330SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6NECvK|5EcEWPQly8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved PARP / c-Myc; 

PubMed: 25289887     


Immunoblot analysis of A2780 cells during the 5 hr time-course treatment of Dinaciclib (100 nM).

Mcl-1 / Bcl-2 / Bcl-xl / Bax / Bak / PUMA / Noxa; 

PubMed: 28714472     


H196 cells treated with doxorubicin for the indicated times were assessed by immunoblot analysis. 

RNAP II (P-Ser2/P-Ser5); 

PubMed: 25289887     


Immunoblot analysis of A2780 cells during the 5 hr time-course treatment of Dinaciclib (100 nM).

Survivin; 

PubMed: 28207834     


Western blot analysis was performed in cells treated with dinaciclib (25 nM) or vehicle for the indicated time. The levels of Mcl-1, Bcl-xL and survivin were evaluated in BHP7-13, WRO82-1 and 8505C cells.

25289887 28714472 28207834
Growth inhibition assay
Cell viability; 

PubMed: 28361959     


(a-c) The number of cells after dinaciclib treatment. Cell number in 49 fields (7 × 7) was calculated and shown in the graph (n = 4). (a) Total cell number. **p < 0.01 vs control. (b) Number of OCT4 positive cells. **p < 0.01 vs control. (c) Number of OCT4 negative cells. n.s., not significant. (d) The percentage of OCT4 positive cells. **p < 0.01 vs control. *p < 0.05 vs 6 nM.

Cell viability; 

PubMed: 27378523     


(a) Six typical NB cell lines were treated with increasing concentrations of dinaciclib for 48 hrs. Cell viability was then measured by the Cell Counting Kit-8 (CCK-8) assay. P-values < 0.01 (**) or P < 0.001 (***) (Student's t-test, two-tailed) were indicated. (b) The IC50 values of dinaciclib on each cell line listed were calculated based on the data in (a).

28361959 27378523
Immunofluorescence
cyclin B1 / α-tubulin / Aurora A; 

PubMed: 28207834     


(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.

OCT4; 

PubMed: 28361959     


Representative images of OCT4 positive cells (red). Nuclei were stained with Hoechst (blue). Scale bars = 200 μm.

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]
- 合并

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]
- 合并
  • 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]
- 合并
  • 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
    (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
储存条件 粉状
溶于溶剂
别名 PS-095760

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID