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89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 M2H1V2Fxd3C2b4Ppd{BCe3OjeR?= Ml3sNVAxKG6P M{DBbFI1KGh? M4f3dYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MojsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{OEm4PFcoRjJ3Mki5PFg4RC:jPh?=
Kasumi-1 M1fIbGFxd3C2b4Ppd{BCe3OjeR?= MmnFNVAxKG6P NY\EfnRiOjRiaB?= M1nVcYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M1;udVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mki5PFg4Lz5{NUK4PVg5PzxxYU6=
U937 MYjGeY5kfGmxbjDBd5NigQ>? NXv4WFZXOi93L{GwJI5O M{nm[VMhcA>? NFLQfFNjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
8226 MnTxSpVv[3Srb36gRZN{[Xl? NFzYNGgzNzVxMUCgcm0> MYe0JIg> NHfMUFFjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| NGXWVog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
H929 NHy2TZJHfW6ldHnvckBCe3OjeR?= M3S0e|IwPS9zMDDuUS=> MmfDOEBp MmXiZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MkXaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
K562 Ml7USpVv[3Srb36gRZN{[Xl? MXOxMlUwOy96IH7N MU[2JIg> MnPLZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
BaF3/Bcr-abl NGO5c5NHfW6ldHnvckBCe3OjeR?= MXSxMlUwOy96IH7N NF7Q[G03KGh? NIXob5hjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
U937  MWXGeY5kfGmxbjDBd5NigQ>? MYGyM|ExKG6P MVyzJIg> MnXuZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? NGjzRWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
1205Lu NX;NdGlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\4R|ExNzNyIH7N Mn7ZO|IhcA>? MXHpcohq[mm2czDj[YxtKGe{b4f0bEBidmRic4Xyeol3[Wx? MnP2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MkeyNlUoRjJ|NUK3NlI2RC:jPh?=
WM1366 M{n4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDSdFlMOTBxM{Cgcm0> NX7KOpExPzJiaB?= NIW5dJNqdmirYnn0d{Bk\WyuIHfyc5d1cCCjbnSgd5Vzfmm4YXy= NX7KWW1wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NlczOjVpPkKzOVI4OjJ3PD;hQi=>
RD MonHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX6TWM2OD16LkKgcm0> M1\KNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Rh41 NVj6eItkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDTTWM2OD1zMD61JI5O NHSzXJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Rh18 NI\GU3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:4dmVKSzVyPUGwMlUhdk1? NFjOPGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Rh30 NVXnUJBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHvTWM2OD17IH7N MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
BT-12 NYLZWII3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfLTWM2OD16LkWgcm0> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-266 NUDzTJc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL6TWM2OD15LkOgcm0> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
TC-71 NHrqXIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHqO|RKSzVyPUOuPUBvVQ>? M3i3c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-9 NYDySGhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3NR4NKSzVyPUigcm0> MlLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-10 M{GzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr5PYdEUUN3ME22MlMhdk1? M3LoNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-258 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HBTmlEPTB;OT65JI5O M2LsN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
GBM2 M4fPXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXW3NGR1UUN3ME22MlUhdk1? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
NB-1643 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnFVFlKSzVyPUOuN{BvVQ>? NVHO[IpmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
NB-EBc1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;GTWM2OD15IH7N M4LNZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-90 MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTdwNTDuUS=> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-136 M3nUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXWU2Z5UUN3ME25Mlghdk1? NFPrRZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
NALM-6 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlO3TWM2OD12Lk[gcm0> NFqyems9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
COG-LL-317 NV7Qb4FNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTZwNTDuUS=> M3HQO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
RS4;11 NVXVSXNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTVwMTDuUS=> M3vPOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
MOLT-4 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHq1VnlKSzVyPUmuN{BvVQ>? NUjmcG43RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CCRF-CEM MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTVwNjDuUS=> M3\VSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Kasumi-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\TUGlEPTB;ND61JI5O M2rEelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Karpas-299 NYXiRZB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DzNGlEPTB;Mz65JI5O NVLzTlJURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Ramos-RA1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLITWM2OD15Lkmgcm0> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
MIAPaCa-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\TT2c4OiCq NFjmOm1IUTVyPUGwJI5O M2rYclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c6Lz5{MUe2PFc4QTxxYU6=
Pa20C  NWD0bXpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrJVVc4OiCq NF3UZo5IUTVyPUKwJI5O MnzBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5Nki3O|koRjJzN{[4O|c6RC:jPh?=
ML-1 M3vE[2Fxd3C2b4Ppd{BCe3OjeR?= MnLPNU0yODByIH7N NETKNIs1KGh? M2D5[olv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 NH3leWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe2PFc4Pyd-MkG3Olg4Pzd:L3G+
Cytotoxicity assay NFm5copOTEFvTVKtOFM3 MUO3NkBpenN? MWTJR|UxKD1iMD6wNFUh|ryP NVHOXo11RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NUGyTXN5VkOLLVi5Nlk> NVz1NWJVPzJiaILz MYPJR|UxKD1iMD6wNFUh|ryP MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay M3Tvcm1FSS2PQj2yN|E> MX[3NkBpenN? M2jOXWlEPTBiPTCwMlAxPSEQvF2= NWHGfHFKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay M1P1fXNMNUWVLUG= NIfaR204OiCqcoO= MX3JR|UxKD1iMD6wNFUh|ryP M1zIcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay M2[xS2E3PzN? M{mxSlczKGi{cx?= NXHafohOUUN3MDC9JFAvODB3IN88US=> NWToU5gxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MVfTT{1DWi1| MYK3NkBpenN? M4XPVmlEPTBiPTCwMlAxPSEQvF2= M{HsVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay NIThcnpOVk6JLVjPVy=> NYnkfYtMPzJiaILz NGrxVm5KSzVyIE2gNE4xODV3IN88US=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MoDYV2suXVRvMR?= MlmwO|IhcHK| M3u1OGlEPTBiPTCwMlAxPiEQvF2= MnzTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay NITzZlVWOjZ4 M2HlUFczKGi{cx?= NGrhdWxKSzVyIE2gNE4xODZizszN NFTp[m09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay MkXLVnBOUTF6MkK2 NYjGcGtiPzJiaILz MVrJR|UxKD1iMD6wNFkh|ryP NXT3eYtpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NGXmVoxUXzh5Mh?= NFq4e484OiCqcoO= MnPiTWM2OCB;IECuNFA6PSEQvF2= MoK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay M{\LXnQ1P0R? MYK3NkBpenN? MoTmTWM2OCB;IECuNFEh|ryP MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Apoptosis assay NHzod2lCPjd| M{jTU|I1KGi{cx?= NGq2XmRGSzVyIE2gNE4xOTFizszN M4XjdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MmTSUWNHPw>? MVu3NkBpenN? NGr0OFNKSzVyIE2gNE4xOiEQvF2= MnfsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Function assay MWTT[lk> MnfOTWM2OCB;IECuNFczKM7:TR?= NGrhN|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke0NVg2Oyd-Mk[3OFE5PTN:L3G+
Function assay Mkf6d4Y6 M3jiNWlEPTBiPTCwMlAxOiEQvF2= MkL4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NUG1NFUoRjJ4OEWxOVA2RC:jPh?=
Function assay M37WN3NnQQ>? MkGyNUBpeg>? M4HLcGlEPTBiPTCwMlAxOSEQvF2= NXPrXVlFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay NIXpW3NU\jl? MXyxJIhz NGHGS4JKSzVyIE2gNE4xODFizszN MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay MUXT[lk> NYH4e|ZpOSCqch?= NYrhUY53UUN3MDC9JFAvODBzIN88US=> MmLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M1XlWnNnQQ>? MnvTNUBpeg>? M2rpb2lEPTBiPTCwMlAxOSEQvF2= NUjKS5BoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay NITQbWJU\jl? NHvkT|QyKGi{ MUPJR|UxKD1iMD6wNFMh|ryP Mlu5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M3vMZXNnQQ>? M4HmTFEhcHJ? NYrQVGRMUUN3MDC9JFAvODB|IN88US=> MkDPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M3rsV3NnQQ>? NHzQc44yKGi{ MoDWTWM2OCB;IECuNFA1KM7:TR?= NVrReWI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay MkDYV4Y6 MWWxJIhz MV\JR|UxKD1iMD6wNFQh|ryP NXPLfplURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay MknlV4Y6 M{LhVlExKHWP NH\FfIVKSzVyIE2gNE4xODRizszN MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN{OU[1PEc,Ojl|Mkm2OVg9N2F-
Function assay NHvhRZlU\jl? NInEbVUyKGi{ Mlz1TWM2OCB;IECuNFAyKM7:TR?= MnPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzN|goRjJ7OEWzN|M5RC:jPh?=
Function assay NUfRUIc3W2Z7 M2H5PVEhcHJ? NFrQRnNKSzVyIE2gNE4xODFizszN MlLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzN|goRjJ7OEWzN|M5RC:jPh?=
Function assay MnjoV4Y6 NFPvW|QyKGi{ NGHIS|JKSzVyIE2gNE4xODNizszN MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Function assay MXnT[lk> NGjYcVQyKGi{ NYqxc2lvUUN3MDC9JFAvODB2IN88US=> MkjHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzN|goRjJ7OEWzN|M5RC:jPh?=
Antiproliferative assay MYPNU2xOOTN? NXXFZ5JHPzJiaILz M{T2PWdKPTBiPTCwMlAxOzNizszN M2HwPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MoriUWVEOQ>? Ml;nO|IhcHK| NETjPFlIUTVyIE2gNE4xODN4IN88US=> NY\GNZJxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay MoH1UW9NVTF2 MYq3NkBpenN? MVrHTVUxKD1iMD6wNFQ2KM7:TR?= M1:1N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay M{nsVmNQVE9{MEW= NIrpVnk4OiCqcoO= MoO1S2k2OCB;IECuNFA3QCEQvF2= NGftOmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MonxTGw3OA>? NU\XVYpJPzJiaILz NWP2Nmh{T0l3MDC9JFAvODB6IN88US=> M4W5N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MYDSZY1wew>? MXe3NkBpenN? Ml;VS2k2OCB;IECuNFA5PiEQvF2= NFjYRnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MlTBS2lUXFRz NXvSfVhFPzJiaILz MoOyS2k2OCB;IECuNFA5QCEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NW[yTGMyXTl|Nx?= M3u4SVczKGi{cx?= MVjHTVUxKD1iMD6wNUDPxE1? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NUTpUGdnSTR|MR?= MXO3NkBpenN? M4L0WGdKPTBiPTCwMlAyOSEQvF2= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MXLTT20y NHu5TYs4OiCqcoO= MlXnS2k2OCB;IECuNFEyKM7:TR?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MUfNSWMz Mmm4O|IhcHK| MlOxS2k2OCB;IECuNFEyKM7:TR?= M4S3UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NV[zUmNmSTN5NR?= NUjudI0zPzJiaILz NEXEZY5IUTVyIE2gNE4xOTFizszN MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MkmzU2NKNUGPTEO= NFHhc|M4OiCqcoO= NUDWbIlwT0l3MDC9JFAvODF|IN88US=> NW\XbYcxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay Mnf2RmUpOilvTUG3 NEXObm44OiCqcoO= NWLuc5VnT0l3MDC9JFAvODJzIN88US=> NUL2NHp6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay NGPlWpVEUE9? NHzDems4OiCqcoO= NXv1Rmh4T0l3MDC9JFAvOTZizszN M17Ce|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Function assay MonQUmNKNUh7Mkm= MlXZNE4xODVidV2= MnP4NlQhcHK| NVjhRXg3UW6qaXLpeIlwdiCxZjDDSGszNW2nZHnheIVlKFKkIIDoc5NxcG:{eXzheIlwdiCjdDDT[ZIhQDB5L{ixNUBqdiCqdX3hckBPS0lvSEmyPUBk\WyuczDheEAxNjByNTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? M1zoPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Function assay NGrTR2hCPjd| M2TGelAvODVidV2= Mlr5NlQhcHK| M4fBdWlvcGmkaYTpc44hd2ZiQ1TLNk1u\WSrYYTl[EBT[iCyaH;zdIhwenmuYYTpc44h[XRiU3XyJFgxPy96MUGgbY4hcHWvYX6gRVY4OyClZXzsd{BifCByLkC1JJVOKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91fGmwZzDhcoFtgXOrcx?= NWnxZ2QzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Apoptosis assay NILWPGtOTUNz NX3jc4FwOC5yMTD1US=> M3jUN|I1KGi{cx?= MXXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2HQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hVUOOLUGgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> MkH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NVXsV3FrUEx4MB?= NGnXVIIxNjBzIIXN Mlu0NlQhcHK| MVfJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hVUOOLUGgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> MmrCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NWjuVFhpVVZ2LUGx M1S3cVAvODFidV2= MkX0NlQhcHK| M{TEW2lv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHOtUXlEKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay MXjNSWMy MlzyNE4xOSC3TR?= NUDofFN6OjRiaILz NHfDWIhKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3FR|Eh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iYz3NXWMhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? NHjBelI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Apoptosis assay MoTsUXY1NTFz MV2wMlAyKHWP NETM[5ozPCCqcoO= NH\XUJJKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3WOE0yOSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDNR2wuOSCuZY\lcEBifCByLkCxJJVOKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91fGmwZzDhcoFtgXOrcx?= NUOyNpZuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay MULIUFYx M{G4[lAvODFidV2= NGjzZoIzPCCqcoO= MXfJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[y2PWVOgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Cytotoxicity assay MkTqWVJQWw>? NGXzNZY6PiCqcoO= MonxTWM2OCB;IECuNFA3KM7:TR?= NGLTfXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OESwM{c,S2iHTVLMQE9iRg>?
Function assay NXO2W5AzXTKRUx?= MVqxJIhz NGPwclFKSzVyIE2gNE4xODdizszN MoDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh2MD:nQmNpTU2ETEyvZV4>

... 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、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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID