Dinaciclib (SCH727965)

For research use only.

Catalog No.S2768 Synonyms: PS-095760

89 publications

Dinaciclib (SCH727965) Chemical Structure

CAS No. 779353-01-4

Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.

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Selleck's Dinaciclib (SCH727965) has been cited by 89 publications

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.
Targets
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
In vitro

Dinaciclib is also a potent DNA replication inhibitor that blocks thymidine (dThd) DNA incorporation in A2780 cells with IC50 of 4 nM. Dinaciclib strongly suppresses phosphorylation of Rb on Ser 807/811 at concentrations >6.25 nM, which is in agreement with the observation that 4 nM concentrations are required for 50% inhibition of dThd DNA incorporation in the same cell model. Significantly, complete suppression of Rb phosphorylation is correlated with the onset of apoptosis, as indicated by the appearance of the p85 PARP cleavage product in cells exposed to >6.25 nM Dinaciclib. Dinaciclib is active against a broad spectrum of human tumor cell lines. [1] Addition of Dinaciclib during hydroxyurea exposure also suppresses accumulation of γ-H2AX, in a dose-dependent manner. [2] Dinaciclib inhibits melanoma cell proliferation, and drives melanoma cells into massive apoptosis. [3] Dinaciclib induces the apoptosis of several osteosarcoma cell lines including those resistant to doxorubicin and dasatinib. Dinaciclib attenuates the phosphorylation of RNAP II at serine 2 and the phosphorylation of the CDK inhibitor p27Kip1 at threonine 187. Reductions in phosphorylation activity occurrs at 12 - 40 nM Dinaciclib (4 to 16 hours post-Dinaciclib addition). Dinaciclib also reduces the phosphorylation of Rb at serine 807/811. Dinaciclib induces the apoptosis of mock- and p53-depleted U2OS cells to a similar extent. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CA46 MmriRZBweHSxc3nzJGF{e2G7 MWixNFAhdk1? NYHuc|M6OjRiaB?= NV21Sm5bcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NX\RZ5RwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPFk5QDdpPkK1Nlg6QDh5PD;hQi=>
Kasumi-1 Ml\DRZBweHSxc3nzJGF{e2G7 NXLp[|FTOTByIH7N NFXPepozPCCq MYHpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ6OUi4O{c,OjV{OEm4PFc9N2F-
U937 NETnbYRHfW6ldHnvckBCe3OjeR?= MXyyM|UwOTBibl2= NFvGbYc{KGh? MmS2Zoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MkfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
8226 M3\XUmZ2dmO2aX;uJGF{e2G7 NVXlcoh1Oi93L{GwJI5O NX3UOnl{PCCq MWDicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ MnTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
H929 NEToVIFHfW6ldHnvckBCe3OjeR?= M2HVOVIwPS9zMDDuUS=> NHLySJI1KGh? Ml:wZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? NVTwS4N4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
K562 M3ztc2Z2dmO2aX;uJGF{e2G7 MXGxMlUwOy96IH7N MX62JIg> MY\icI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
BaF3/Bcr-abl Mnv3SpVv[3Srb36gRZN{[Xl? Mm[zNU42NzNxODDuUS=> MmSzOkBp M3frToJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NVrLeY5kRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
U937  MmHYSpVv[3Srb36gRZN{[Xl? NUO5XYRUOi9zMDDuUS=> M{jSS|MhcA>? M4DadYJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NInRc5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
1205Lu MoXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHRNVAwOzBibl2= M{OxRlczKGh? M1XVe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGwZDDzeZJ3cX[jbB?= NEXST2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyO|IzPSd-MkO1NlczOjV:L3G+
WM1366 MlmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPtU|EyOC9|MDDuUS=> MYe3NkBp MVPpcohq[mm2czDj[YxtKGe{b4f0bEBidmRic4Xyeol3[Wx? NF7pZ|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyO|IzPSd-MkO1NlczOjV:L3G+
RD NWn6UWJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjrRYNKSzVyPUiuNkBvVQ>? NUWzRlRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Rh41 M2P0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HU[2lEPTB;MUCuOUBvVQ>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Rh18 NHvYS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7yVoo{UUN3ME2xNE42KG6P NVixc2p4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Rh30 MlzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTlibl2= NW\mdoF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
BT-12 M3:yS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRThwNTDuUS=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-266 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TTcWlEPTB;Nz6zJI5O MkjSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
TC-71 NYPPfYsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTNwOTDuUS=> NHi1[FY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-9 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmO4TWM2OD16IH7N M1LiNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-10 M2nPZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXJTWM2OD14LkOgcm0> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-258 NY[3SZhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkW0TWM2OD17Lkmgcm0> NWjqVVMyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
GBM2 NX[4XG1yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInsVHhKSzVyPU[uOUBvVQ>? Mn32QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NB-1643 M1XiN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTNwMzDuUS=> M3yxSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
NB-EBc1 NYTpXoZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTdibl2= NIm2WJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-90 M2Dy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml6yTWM2OD15LkWgcm0> M{\CTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-136 NETZcIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXzXnRwUUN3ME25Mlghdk1? NEDLVGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
NALM-6 NHnYVYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4iwS2lEPTB;ND62JI5O NHGwUnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
COG-LL-317 MoXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTZwNTDuUS=> NVXxbplKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
RS4;11 NXzEXI1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S3PGlEPTB;NT6xJI5O MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
MOLT-4 NYHLNpRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nRPGlEPTB;OT6zJI5O NFT1fVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CCRF-CEM NVHyZZFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jNVWlEPTB;NT62JI5O NVvWbIhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Kasumi-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XXVmlEPTB;ND61JI5O NVLaOmpMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Karpas-299 MnvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvhTWM2OD1|Lkmgcm0> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Ramos-RA1 NF62PYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfKZlJ3UUN3ME23Mlkhdk1? NHj4OG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
MIAPaCa-2 MojTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjTSXlCPzJiaB?= MoqxS2k2OD1zMDDuUS=> NFfVO489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe2PFc4QSd-MkG3Olg4Pzl:L3G+
Pa20C  NF3Wc5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nwblczKGh? M3\td2dKPTB;MkCgcm0> NF;RUHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe2PFc4QSd-MkG3Olg4Pzl:L3G+
ML-1 M1nxcmFxd3C2b4Ppd{BCe3OjeR?= NVu3OpVyOS1zMECwJI5O M1XrNVQhcA>? MmjpbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd4OEe3O{c,OjF5Nki3O|c9N2F-
Cytotoxicity assay MlPYUWRCNU2ELUSzOi=> NFHMNVk4OiCqcoO= NX;TWWhHUUN3MDC9JFAvODB3IN88US=> NV7rbmU4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MXfOR2kuUDl{OR?= M3jHXlczKGi{cx?= M4nCUWlEPTBiPTCwMlAxPSEQvF2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MV3NSGEuVUJvMkOx NInQ[Fc4OiCqcoO= M2nOPGlEPTBiPTCwMlAxPSEQvF2= NE[5U2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay MkLkV2suTVNvMR?= NFH3d3A4OiCqcoO= MVfJR|UxKD1iMD6wNFUh|ryP NFLZZlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NUjmOZF2STZ5Mx?= NXSzNItZPzJiaILz NELhZlNKSzVyIE2gNE4xODVizszN MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MknrV2suSlJvMx?= MlS3O|IhcHK| MnP0TWM2OCB;IECuNFA2KM7:TR?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NHm2XWlOVk6JLVjPVy=> MWq3NkBpenN? MkToTWM2OCB;IECuNFA2PSEQvF2= MnXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay M3;5cXNMNVWWLUG= NXjGPXA4PzJiaILz NGP5e3FKSzVyIE2gNE4xODZizszN Mni1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay MYrVNlY3 NFjxWII4OiCqcoO= MkLNTWM2OCB;IECuNFA3KM7:TR?= NX;EfWk4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MUDSVG1KOTh{Mk[= NWj3UVlGPzJiaILz NHXwVoZKSzVyIE2gNE4xODlizszN MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay Mn;PV3c5PzJ? MUi3NkBpenN? NUnqTYtDUUN3MDC9JFAvODB7NTFOwG0> NEnnZnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay MWrUOFdF NH;od|k4OiCqcoO= NUTXU|l[UUN3MDC9JFAvODFizszN NG\RWpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Apoptosis assay NHeySHhCPjd| MXWyOEBpenN? M2XrbGVEPTBiPTCwMlAyOSEQvF2= NWfFSINXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NXzweplOVUOINx?= NFHSfWI4OiCqcoO= Mkj4TWM2OCB;IECuNFIh|ryP MmjGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Function assay MVfT[lk> MXzJR|UxKD1iMD6wO|Ih|ryP M3n1O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{SxPFU{Lz5{Nke0NVg2OzxxYU6=
Function assay NWXmfndJe2Z7 NGnLZ5RKSzVyIE2gNE4xODJizszN MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh3MUWwOUc,OjZ6NUG1NFU9N2F-
Function assay NFjNeZNU\jl? MWSxJIhz NXfGU2xKUUN3MDC9JFAvODBzIN88US=> MlzxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M{O0fnNnQQ>? M3nTV|EhcHJ? MkTBTWM2OCB;IECuNFAyKM7:TR?= NX;TPXhxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay M{XCdHNnQQ>? MnizNUBpeg>? M1;mTmlEPTBiPTCwMlAxOSEQvF2= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay NGnRS3pU\jl? MV2xJIhz M1OwN2lEPTBiPTCwMlAxOSEQvF2= MmDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay NVXIbZBtW2Z7 M13DdVEhcHJ? MX7JR|UxKD1iMD6wNFMh|ryP M3PFdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay M4PoTnNnQQ>? NFTreYIyKGi{ M2DKcWlEPTBiPTCwMlAxOyEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay NGmxWlVU\jl? Mor2NUBpeg>? Mor3TWM2OCB;IECuNFA1KM7:TR?= NVL0eJJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay M3;qSXNnQQ>? MY[xJIhz NYXablU6UUN3MDC9JFAvODB2IN88US=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay M1fZSnNnQQ>? NFPM[IwyOCC3TR?= NF[1eYRKSzVyIE2gNE4xODRizszN NWP6UmFlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzNlk3PThpPkK5N|I6PjV6PD;hQi=>
Function assay NXO2WGo4W2Z7 NHjPe2YyKGi{ NIPi[lhKSzVyIE2gNE4xODFizszN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Function assay MmG1V4Y6 NEHDd4UyKGi{ M4\ieGlEPTBiPTCwMlAxOSEQvF2= NIXHd|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N|M{QCd-Mkm4OVM{Ozh:L3G+
Function assay MknyV4Y6 M3rTVlEhcHJ? MY\JR|UxKD1iMD6wNFMh|ryP M{LzZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|M5Lz5{OUi1N|M{QDxxYU6=
Function assay NFjqXlJU\jl? M2rmOlEhcHJ? NV3XbpgyUUN3MDC9JFAvODB2IN88US=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Antiproliferative assay MWjNU2xOOTN? M4jXWlczKGi{cx?= NUj3NYxlT0l3MDC9JFAvODB|MzFOwG0> MkPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MlfzUWVEOQ>? MnXRO|IhcHK| MVTHTVUxKD1iMD6wNFM3KM7:TR?= M3fUbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay Ml;BUW9NVTF2 NWfqOYZ6PzJiaILz MYLHTVUxKD1iMD6wNFQ2KM7:TR?= NIT4PGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MlHXR29NVzJyNR?= NH24NXU4OiCqcoO= MoTNS2k2OCB;IECuNFA3QCEQvF2= MojiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NIPxZYlJVDZy NEn6ZWw4OiCqcoO= NWnoUIMxT0l3MDC9JFAvODB6IN88US=> MnHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NFjxZolT[W2xcx?= NGrvdIM4OiCqcoO= Mme3S2k2OCB;IECuNFA5PiEQvF2= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NE\JcIRIUVOWVEG= M1jUT|czKGi{cx?= M1vKUGdKPTBiPTCwMlAxQDhizszN NFToOXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NH;S[pRWQTN5 M17ZVlczKGi{cx?= MVTHTVUxKD1iMD6wNUDPxE1? MnXIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay M2DwZWE1OzF? Moj6O|IhcHK| M1;VT2dKPTBiPTCwMlAyOSEQvF2= NEfsRnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay Mn7PV2tOOQ>? NFj5V4U4OiCqcoO= NIPpNY5IUTVyIE2gNE4xOTFizszN Mkn1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay Mn3lUWVEOg>? MX:3NkBpenN? M4rWd2dKPTBiPTCwMlAyOSEQvF2= NYfzcoVURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay MWnBN|c2 MlLZO|IhcHK| NHXIOVZIUTVyIE2gNE4xOTFizszN MknZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NVrldXd5V0OLLVHNUFM> NHvxNWU4OiCqcoO= M1nvUWdKPTBiPTCwMlAyOyEQvF2= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MmTzRmUpOilvTUG3 M3jrOVczKGi{cx?= NUH6WWl6T0l3MDC9JFAvODJzIN88US=> Mor6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay M3XCO2NJVw>? NYXE[plYPzJiaILz NXLLXWpGT0l3MDC9JFAvOTZizszN NIG3SXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Function assay NUTtfW9MVkOLLVi5Nlk> NUL3fGRNOC5yMEWgeW0> NY\JR4lTOjRiaILz M1TJPWlvcGmkaYTpc44hd2ZiQ1TLNk1u\WSrYYTl[EBT[iCyaH;zdIhwenmuYYTpc44h[XRiU3XyJFgxPy96MUGgbY4hcHWvYX6gUmNKNUh7MkmgZ4VtdHNiYYSgNE4xODVidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ MmnPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Function assay NWn1bW0zSTZ5Mx?= MWmwMlA2KHWP MXWyOEBpenN? NEjBOI5KdmirYnn0bY9vKG:oIFPET|IudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IGPldkA5ODdxOEGxJIlvKGi3bXHuJGE3PzNiY3XscJMh[XRiMD6wOUB2VSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= NYjPN41ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Apoptosis assay NUn5bWFUVUWFMR?= MVmwMlAyKHWP NX;CUY9vOjRiaILz M1rhUGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTVXDNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCPQ1ytNUBt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay NWTpU5ZHUEx4MB?= MUOwMlAyKHWP NXOxNGYyOjRiaILz NGjsW|ZKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iTVPMMVEhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? MnT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NXzKR3FDVVZ2LUGx MUewMlAyKHWP MXmyOEBpenN? MVXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2YND2xNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClLV3ZR{Bt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? MoHnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NYDMfXFDVUWFMR?= MVuwMlAyKHWP NHTJcY4zPCCqcoO= MkXaTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPRVOxJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGNvTWnDJIxmfmWuIHH0JFAvODFidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ NFnSfXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Apoptosis assay MkLqUXY1NTFz NYL2ZZh5OC5yMTD1US=> NHLZUGQzPCCqcoO= NGP4eIRKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3WOE0yOSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDNR2wuOSCuZY\lcEBifCByLkCxJJVOKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91fGmwZzDhcoFtgXOrcx?= NHq5fGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Apoptosis assay NGjnVJVJVDZy NUnkTlliOC5yMTD1US=> MUCyOEBpenN? NGLKOJFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iYz3NXWMhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? NF;jcYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Cytotoxicity assay NXXafmdPXTKRUx?= Mn7SPVYhcHK| NHTUXW9KSzVyIE2gNE4xODZizszN MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDRyLze+R4hGVUKOPD;hQi=>
Function assay NGPMWIZWOk:V NF\UeGoyKGi{ MXvJR|UxKD1iMD6wNFch|ryP MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDRyLze+R4hGVUKOPD;hQi=>

... 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
In vivo Dinaciclib i.p. administration at 8, 16, 32, and 48 mg/kg daily for 10 days results in tumor inhibition by 70%, 70%, 89%, and 96%, respectively. Dinaciclib MED (minimum effective dose) appears to be <8 mg/kg. Dinaciclib is well tolerated, and the maximum body weight loss in the highest dosage group is 5%. Dinaciclib has dose-dependent antitumor activity in vivo, and that nearly complete inhibition of tumor growth occurs at a dose level below the MTD (maximum tolerated dose). Dinaciclib has a short plasma half-life in mouse. [1]

Protocol

Kinase Assay:[1]
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Cyclin/CDK kinase assay:

Recombinant cyclin/CDK holoenzymes are purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes are typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 1 mM DTT, and 0.1 mM sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2-μM substrate solution (a biotinylated peptide derived from histone H1) are mixed and combined with 10 μL of diluted Dinaciclib. The reaction is started by the addition of 50 μL of 2 μM ATP and 0.1 μCi of 33P-ATP. Kinase reactions are incubated for 1 hour at room temperature and are stopped by the addition of 0.1% Triton X-100, 1 mM ATP, 5 mM EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads are captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads are washed twice with 2 M NaCl and twice with 2 M NaCl containing 1% phosphoric acid. The signal is then assayed using a TopCount 96-well liquid scintillation counter.
Cell Research:[1]
- Collapse
  • Cell lines: A2780 cells
  • Concentrations: 0 μM -5 μM
  • Incubation Time: 24 hours
  • Method: A2780 cells are maintained in DMEM plus 10% fetal bovine serum and passaged twice weekly by detaching the monolayer with trypsin-EDTA. One hundred microliters of A2780 cells (5 × 103 cells) are added per well to a 96-well Cytostar-T plate and incubated for 16 hours to 24 hours at 37 °C. Dinaciclib is serially diluted in complete media plus 2% 14C-labeled dThd. Media are removed from the Cytostar T plate; 200 μL of various Dinaciclib dilutions are added in quadruplicate; and the cells are incubated for 24 hours at 37 °C. Accumulated incorporation of radiolabel is assayed using scintillation proximity and measured on a TopCounTM.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Nude mice bearing A2780 tumors
  • Dosages: 8 mg/kg, 16 mg/kg, 32 mg/kg, and 48 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 26 mg/mL warmed (65.57 mM)
Ethanol 8 mg/mL warmed (20.17 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 396.49
Formula

C21H28N6O2

CAS No. 779353-01-4
Storage powder
in solvent
Synonyms PS-095760
Smiles CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCCC4CCO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

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

  • Answer:

    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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID