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
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Selleck生产的Dinaciclib (SCH727965)发表文献77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 MnPLRZBweHSxc3nzJGF{e2G7 MknUNVAxKG6P NEXLSIkzPCCq MkS1bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NEDvRmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK4PVg5Pyd-MkWyPFk5QDd:L3G+
Kasumi-1 NFPYOmxCeG:ydH;zbZMhSXO|YYm= MV6xNFAhdk1? MWCyOEBp M4HQeIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NH;iTYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK4PVg5Pyd-MkWyPFk5QDd:L3G+
U937 M3HlS2Z2dmO2aX;uJGF{e2G7 M1Xpb|IwPS9zMDDuUS=> MX2zJIg> MXjicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NHnJeHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
8226 M3TMS2Z2dmO2aX;uJGF{e2G7 MmDnNk82NzFyIH7N MoXOOEBp MlPVZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? NWHhdoVXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
H929 MV\GeY5kfGmxbjDBd5NigQ>? MWiyM|UwOTBibl2= M1OyPFQhcA>? Ml;vZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
K562 MXnGeY5kfGmxbjDBd5NigQ>? MoP1NU42NzNxODDuUS=> MmTROkBp MX;icI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
BaF3/Bcr-abl MVjGeY5kfGmxbjDBd5NigQ>? MoK5NU42NzNxODDuUS=> M1HBeFYhcA>? MkT2Zoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
U937  NInZS|RHfW6ldHnvckBCe3OjeR?= Mm[5Nk8yOCCwTR?= NIPIe44{KGh? NIHGVGxjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| M3zuO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
1205Lu NEHxd2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmxNE8{OCCwTR?= M1fiblczKGh? NGK5V2NqdmirYnn0d{Bk\WyuIHfyc5d1cCCjbnSgd5Vzfmm4YXy= M3\XdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUK3NlI2Lz5{M{WyO|IzPTxxYU6=
WM1366 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrXNVAwOzBibl2= MlG2O|IhcA>? MUPpcohq[mm2czDj[YxtKGe{b4f0bEBidmRic4Xyeol3[Wx? NX\QT4hWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NlczOjVpPkKzOVI4OjJ3PD;hQi=>
RD MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPOc21pUUN3ME24MlIhdk1? MorVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Rh41 Mni0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELDT49KSzVyPUGwMlUhdk1? M2D2RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Rh18 MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPvc4dKSzVyPUGwMlUhdk1? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Rh30 MkPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG0TWM2OD17IH7N NWrpOGtlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
BT-12 MoiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPRZ5FwUUN3ME24MlUhdk1? NHzDbos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-266 NY\GdnVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHq1UHBKSzVyPUeuN{BvVQ>? Mme5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
TC-71 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e4RWlEPTB;Mz65JI5O M{HDcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-9 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPKPHQ3UUN3ME24JI5O M{TpdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-10 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTZwMzDuUS=> M4TaTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-258 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\WO3ZKSzVyPUmuPUBvVQ>? NIjLSGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
GBM2 NHrGeVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\OXGlEPTB;Nj61JI5O MmnPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NB-1643 NY\FVIJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TmeWlEPTB;Mz6zJI5O MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
NB-EBc1 M{G2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP0e4tKSzVyPUegcm0> Ml;oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-90 NXzpPZhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\VTWM2OD15LkWgcm0> NFj0dnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-136 M{[yZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO4fmZKSzVyPUmuPEBvVQ>? M4LF[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
NALM-6 M1f0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\3TWM2OD12Lk[gcm0> Ml:zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
COG-LL-317 NYTxUpJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r1PGlEPTB;Nj61JI5O NIe4flE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
RS4;11 NYTIfHdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLWTWM2OD13LkGgcm0> M13uU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
MOLT-4 M4nzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCx[HFKSzVyPUmuN{BvVQ>? MkjsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CCRF-CEM M2iyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHTTWM2OD13Lk[gcm0> M1[yeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Kasumi-1 M2rmfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vtdmlEPTB;ND61JI5O MneyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Karpas-299 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i3WmlEPTB;Mz65JI5O NHGzSIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Ramos-RA1 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITUdZlKSzVyPUeuPUBvVQ>? NGDme4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
MIAPaCa-2 M2O5OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG5OYJ4PzJiaB?= M134TmdKPTB;MUCgcm0> M3nkdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c6Lz5{MUe2PFc4QTxxYU6=
Pa20C  NYLROpBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITQcm84OiCq NYC0fGY5T0l3ME2yNEBvVQ>? NFPDWnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe2PFc4QSd-MkG3Olg4Pzl:L3G+
ML-1 NFvyd|FCeG:ydH;zbZMhSXO|YYm= MVSxMVExODBibl2= NYW3NW9TPCCq NYD2N21xcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> M{HIVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c4Lz5{MUe2PFc4PzxxYU6=
Cytotoxicity assay NFPNTJpOTEFvTVKtOFM3 M1\yfVczKGi{cx?= NYPxOnk6UUN3MDC9JFAvODB3IN88US=> NHS0flQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NGmxNW9PS0lvSEmyPS=> MXm3NkBpenN? M1\OXWlEPTBiPTCwMlAxPSEQvF2= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MlXCUWRCNU2ELUKzNS=> MlPFO|IhcHK| M4fDZ2lEPTBiPTCwMlAxPSEQvF2= NH;MfpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NFj1Wo5UUy2HUz2x M3Th[FczKGi{cx?= NE\y[4dKSzVyIE2gNE4xODVizszN NHO1T|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NVPBXo5uSTZ5Mx?= MnvhO|IhcHK| MoL4TWM2OCB;IECuNFA2KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NFLYdJpUUy2EUj2z MV:3NkBpenN? MUTJR|UxKD1iMD6wNFUh|ryP NHrwNmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NIHRR5lOVk6JLVjPVy=> NX7XNGd1PzJiaILz NEXrT2dKSzVyIE2gNE4xODV3IN88US=> M3zafFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MmnNV2suXVRvMR?= MkjwO|IhcHK| NFLJS2dKSzVyIE2gNE4xODZizszN Ml3SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay M1z1fnUzPjZ? NVXqOXpCPzJiaILz MmnmTWM2OCB;IECuNFA3KM7:TR?= NV7HR3QxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay M4DB[HJRVUlzOEKyOi=> M{Xwd|czKGi{cx?= M1HFVWlEPTBiPTCwMlAxQSEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MVXTW|g4Og>? NFXBeoc4OiCqcoO= NFS1SHNKSzVyIE2gNE4xODl3IN88US=> NXjCVXR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MVLUOFdF MXq3NkBpenN? NV;3NpFMUUN3MDC9JFAvODFizszN NH6zTIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Apoptosis assay NFewT4tCPjd| NH3hWVkzPCCqcoO= M1HuWGVEPTBiPTCwMlAyOSEQvF2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NI[zepROS0Z5 NUPO[ohYPzJiaILz MVvJR|UxKD1iMD6wNkDPxE1? M1u0ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Function assay MkLEV4Y6 M4DzbmlEPTBiPTCwMlA4OiEQvF2= NUfKcWc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OFE5PTNpPkK2O|QyQDV|PD;hQi=>
Function assay NFv5SG9{\jl? M1vyPGlEPTBiPTCwMlAxOiEQvF2= NWO2OlJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OVE2ODVpPkK2PFUyPTB3PD;hQi=>
Function assay MXnT[lk> MVuxJIhz NFLSV3ZKSzVyIE2gNE4xODFizszN NX3WXmVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay MUXT[lk> NXzBNoN5OSCqch?= NV\0cVkzUUN3MDC9JFAvODBzIN88US=> M2\1VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay MkO4V4Y6 MUGxJIhz MoPOTWM2OCB;IECuNFAyKM7:TR?= NFrWcZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay MVzT[lk> NHjlVFAyKGi{ NWKwRVJ4UUN3MDC9JFAvODBzIN88US=> Mk\LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay MmH4V4Y6 NELDc|EyKGi{ MWDJR|UxKD1iMD6wNFMh|ryP MmLtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay MVHT[lk> NGT6XnEyKGi{ NVviUG1{UUN3MDC9JFAvODB|IN88US=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay NX7wUlByW2Z7 NYXYNZlwOSCqch?= Mn;uTWM2OCB;IECuNFA1KM7:TR?= M4j1UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay M4XhVXNnQQ>? NHS0fGUyKGi{ MkLRTWM2OCB;IECuNFA1KM7:TR?= NY\t[XJFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay NUXIS5V4W2Z7 M{H6bVExKHWP M1izemlEPTBiPTCwMlAxPCEQvF2= NH7lSIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOyPVY2QCd-MkmzNlk3PTh:L3G+
Function assay MkXGV4Y6 MoPXNUBpeg>? MmL5TWM2OCB;IECuNFAyKM7:TR?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Function assay M3nyPXNnQQ>? MknwNUBpeg>? NH7lXJNKSzVyIE2gNE4xODFizszN M33YSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|M5Lz5{OUi1N|M{QDxxYU6=
Function assay NUj4NWg2W2Z7 NWPzOZVNOSCqch?= NUXZOYNnUUN3MDC9JFAvODB|IN88US=> M2fCclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|M5Lz5{OUi1N|M{QDxxYU6=
Function assay MXnT[lk> M1LVVFEhcHJ? MVnJR|UxKD1iMD6wNFQh|ryP NIHzS4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N|M{QCd-Mkm4OVM{Ozh:L3G+
Antiproliferative assay NXn6O3p4VU:OTUGz NYq0d4pNPzJiaILz MoS4S2k2OCB;IECuNFA{OyEQvF2= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MojZUWVEOQ>? M33zR|czKGi{cx?= NYGwflN[T0l3MDC9JFAvODB|NjFOwG0> MlnCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NEPiO41OV0yPMUS= NEfDd5Q4OiCqcoO= NXiwbpNxT0l3MDC9JFAvODB2NTFOwG0> NWnMe3NCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay M2LzWGNQVE9{MEW= NXT5T25qPzJiaILz NV7mNJJlT0l3MDC9JFAvODB4ODFOwG0> M1fOU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay M3u1bWhNPjB? MUK3NkBpenN? MVTHTVUxKD1iMD6wNFgh|ryP Mmi5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MnTaVoFud3N? M2L5bFczKGi{cx?= NFHQO3RIUTVyIE2gNE4xODh4IN88US=> NIHnTZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NE\ZTllIUVOWVEG= M3;2d|czKGi{cx?= MVvHTVUxKD1iMD6wNFg5KM7:TR?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MlLiWVk{Pw>? NVfxTmR1PzJiaILz MUTHTVUxKD1iMD6wNUDPxE1? M2TrRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MkXqRVQ{OQ>? MX[3NkBpenN? MnK5S2k2OCB;IECuNFEyKM7:TR?= MkTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MoTMV2tOOQ>? MkDwO|IhcHK| MXTHTVUxKD1iMD6wNVEh|ryP MmTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NF35XYFOTUN{ Ml;QO|IhcHK| NXjJ[IV1T0l3MDC9JFAvODFzIN88US=> MlPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NFfRbXlCOzd3 MX[3NkBpenN? MnrXS2k2OCB;IECuNFEyKM7:TR?= NFPIU3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MoSzU2NKNUGPTEO= M4rlN|czKGi{cx?= MoDyS2k2OCB;IECuNFE{KM7:TR?= NHfiXFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MXXCSUgzMS2PMUe= M4fFelczKGi{cx?= MnXIS2k2OCB;IECuNFIyKM7:TR?= M3:3eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MnixR2hQ M{\T[lczKGi{cx?= MV\HTVUxKD1iMD6xOkDPxE1? NH3qe2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Function assay M4jvXm5EUS2KOUK5 MYqwMlAxPSC3TR?= NYTQSHdEOjRiaILz MoLYTY5pcWKrdHnvckBw\iCFRFuyMY1m\GmjdHXkJHJjKHCqb4PwbI9zgWyjdHnvckBifCCVZYKgPFA4NzhzMTDpckBpfW2jbjDOR2kuUDl{OTDj[YxteyCjdDCwMlAxPSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> NHPoN2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Function assay M2DTOmE3PzN? MmrGNE4xPSC3TR?= MmjyNlQhcHK| NFS5b3lKdmirYnn0bY9vKG:oIFPET|IudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IGPldkA5ODdxOEGxJIlvKGi3bXHuJGE3PzNiY3XscJMh[XRiMD6wOUB2VSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Apoptosis assay NX:0fpJqVUWFMR?= MUmwMlAyKHWP NEPwXXQzPCCqcoO= NFXNNo1KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3FR|Eh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iTVPMMVEhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? M4nSO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Apoptosis assay M2\jTWhNPjB? M1HFcFAvODFidV2= NEHHUHMzPCCqcoO= NWTBXpRSUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIF3DUE0yKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| M1KyflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Apoptosis assay NGi2VodOXjRvMUG= M4HmR|AvODFidV2= MoDHNlQhcHK| MW\JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2YND2xNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClLV3ZR{Bt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? MoXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NYHRRolCVUWFMR?= MVOwMlAyKHWP NX7kZoxmOjRiaILz MUDJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2HQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[y2PWVOgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> MmXKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay M3nvdW1XPC1zMR?= MYqwMlAyKHWP MUiyOEBpenN? NX\ad|V{UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNWlQuOTFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gUWNNNTFibHX2[Ywh[XRiMD6wNUB2VSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay NFPJVGVJVDZy Mn;SNE4xOSC3TR?= NF;VWlczPCCqcoO= M{GwNWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClLV3ZR{Bt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? MnjRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Cytotoxicity assay NI\wSYhWOk:V MXK5OkBpenN? MVPJR|UxKD1iMD6wNFYh|ryP MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDRyLze+R4hGVUKOPD;hQi=>
Function assay NXPqTo5LXTKRUx?= MY[xJIhz MoT1TWM2OCB;IECuNFA4KM7:TR?= Mm[zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh2MD:nQmNpTU2ETEyvZV4>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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. 

Cleaved PARP / c-Myc; 

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.

RNAP II (P-Ser2/P-Ser5); 

PubMed: 25289887     


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

28714472 25289887 28207834
Growth inhibition assay
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).

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.

27378523 28361959
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、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 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

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