Dinaciclib (SCH727965)

For research use only.

Catalog No.S2768 Synonyms: PS-095760

77 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 77 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 MoTZRZBweHSxc3nzJGF{e2G7 MYKxNFAhdk1? MVWyOEBp MYTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ6OUi4O{c,OjV{OEm4PFc9N2F-
Kasumi-1 NWPneG9KSXCxcITvd4l{KEG|c3H5 NXvPPZBYOTByIH7N MXOyOEBp NWDYV3V6cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NHfVUGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK4PVg5Pyd-MkWyPFk5QDd:L3G+
U937 M2DL[mZ2dmO2aX;uJGF{e2G7 M{fFPFIwPS9zMDDuUS=> M1TU[lMhcA>? NWjFNW1[[myxY3vzJIlv\HWldHnvckBw\iC[QmCtNZMh[W6mIHTve45{fHKnYX2geIFz\2W2cx?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
8226 NFfxXVBHfW6ldHnvckBCe3OjeR?= NFnPZpUzNzVxMUCgcm0> NVHHbVU3PCCq M2XpOIJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NVq1dYo2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
H929 M13GUGZ2dmO2aX;uJGF{e2G7 NX7Bbnl2Oi93L{GwJI5O NEewTYI1KGh? NYHx[nMy[myxY3vzJIlv\HWldHnvckBw\iC[QmCtNZMh[W6mIHTve45{fHKnYX2geIFz\2W2cx?= M1HEb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
K562 M3XCOmZ2dmO2aX;uJGF{e2G7 MXmxMlUwOy96IH7N NUP5dYs2PiCq NIXiR|FjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| MmnRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
BaF3/Bcr-abl MlfQSpVv[3Srb36gRZN{[Xl? NF\FR5MyNjVxMz:4JI5O NYHLOI03PiCq NHvnW2djdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| M2LycVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
U937  M{\GcGZ2dmO2aX;uJGF{e2G7 M3joSlIwOTBibl2= M2D3NFMhcA>? MY\icI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
1205Lu M2PHcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTIOHpxOTBxM{Cgcm0> MnnXO|IhcA>? M3v4cIlvcGmkaYTzJINmdGxiZ4Lve5RpKGGwZDDzeZJ3cX[jbB?= NHLUZog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyO|IzPSd-MkO1NlczOjV:L3G+
WM1366 M33VOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnZe2oyOC9|MDDuUS=> MoP4O|IhcA>? M4P4[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGGwZDDzeZJ3cX[jbB?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV{N{KyOUc,OjN3MkeyNlU9N2F-
RD MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O1[GlEPTB;OD6yJI5O MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Rh41 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13oPGlEPTB;MUCuOUBvVQ>? NFrsTnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Rh18 NVW4XpNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DsW2lEPTB;MUCuOUBvVQ>? M3PsT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Rh30 NYfGSpdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTlibl2= MnXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
BT-12 MoDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4e2UmlEPTB;OD61JI5O MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-266 NIT0W3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTdwMzDuUS=> NXTMT4s4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
TC-71 NHfJT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TsbmlEPTB;Mz65JI5O MknFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-9 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRThibl2= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-10 NG\wUGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnLXlUzUUN3ME22MlMhdk1? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-258 M2jkOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTlwOTDuUS=> MmLLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
GBM2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTZwNTDuUS=> Mn;pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NB-1643 M2XTUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LBSGlEPTB;Mz6zJI5O M3vTVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
NB-EBc1 NUCwVZFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rNNGlEPTB;NzDuUS=> NF7pV2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-90 NHPYNohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoewTWM2OD15LkWgcm0> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-136 MlrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTlwODDuUS=> MorpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NALM-6 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHNTWM2OD12Lk[gcm0> M1HCWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
COG-LL-317 M3nhUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\odJdKSzVyPU[uOUBvVQ>? NX3EeGRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
RS4;11 NEe1NIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLFTWM2OD13LkGgcm0> MmrwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
MOLT-4 M3nNPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LWfmlEPTB;OT6zJI5O MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CCRF-CEM MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTVwNjDuUS=> MlK0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Kasumi-1 NWDKVZZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTRwNTDuUS=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Karpas-299 MkPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTXWm9DUUN3ME2zMlkhdk1? M4n2elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Ramos-RA1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTdwOTDuUS=> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
MIAPaCa-2 M3XmWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfpTZU4OiCq MWLHTVUxRTFyIH7N MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd4OEe3PUc,OjF5Nki3O|k9N2F-
Pa20C  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoWwO|IhcA>? M3vUR2dKPTB;MkCgcm0> Ml7mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5Nki3O|koRjJzN{[4O|c6RC:jPh?=
ML-1 NYHDd2ZsSXCxcITvd4l{KEG|c3H5 NF;FbncyNTFyMECgcm0> MYq0JIg> MnP6bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd4OEe3O{c,OjF5Nki3O|c9N2F-
Cytotoxicity assay M3LjUW1FSS2PQj20N|Y> MXq3NkBpenN? NHr4N5FKSzVyIE2gNE4xODVizszN NX;vWWtQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MVrOR2kuUDl{OR?= M1XOXVczKGi{cx?= MnzaTWM2OCB;IECuNFA2KM7:TR?= NHfldo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay MkLVUWRCNU2ELUKzNS=> NHPXcIw4OiCqcoO= MX7JR|UxKD1iMD6wNFUh|ryP M1ux[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay M1jRWXNMNUWVLUG= MVm3NkBpenN? NX6yfnlvUUN3MDC9JFAvODB3IN88US=> M4np[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay NWPid2tFSTZ5Mx?= MV23NkBpenN? NWLBXYVpUUN3MDC9JFAvODB3IN88US=> NVfnPYIyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay M1i4bXNMNUKULUO= NYDQVFZlPzJiaILz M{LDSGlEPTBiPTCwMlAxPSEQvF2= NUnwXW5TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MV\NUm5INUiRUx?= M4raeFczKGi{cx?= NHXWdmxKSzVyIE2gNE4xODV3IN88US=> NH;CWYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay M3nrcHNMNVWWLUG= NYXwUpVKPzJiaILz NXPxS|dkUUN3MDC9JFAvODB4IN88US=> MlHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay NWTrUlRiXTJ4Nh?= MoTnO|IhcHK| MWfJR|UxKD1iMD6wNFYh|ryP M{\sclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay NG\JcphTWE2LMUiyNlY> NV\McVdqPzJiaILz MmTaTWM2OCB;IECuNFA6KM7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay M3e2eXNYQDd{ MoXnO|IhcHK| NEfsPHhKSzVyIE2gNE4xODl3IN88US=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MnnWWFQ4TA>? M4nUTVczKGi{cx?= NIDt[m5KSzVyIE2gNE4xOSEQvF2= NHj5WGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Apoptosis assay M3i3eGE3PzN? MmHyNlQhcHK| NGW4fVRGSzVyIE2gNE4xOTFizszN M4joVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay M13tdm1ETjd? M1;YcFczKGi{cx?= NGDIN5RKSzVyIE2gNE4xOiEQvF2= Mni0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Function assay NVXadGhvW2Z7 MYLJR|UxKD1iMD6wO|Ih|ryP NWjU[YhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OFE5PTNpPkK2O|QyQDV|PD;hQi=>
Function assay NEfhdlJ{\jl? NH;RSWRKSzVyIE2gNE4xODJizszN MoDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NUG1NFUoRjJ4OEWxOVA2RC:jPh?=
Function assay NFP6XIJU\jl? M33M[lEhcHJ? NYr4WXJkUUN3MDC9JFAvODBzIN88US=> MlriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay MoXTV4Y6 NHHiUXcyKGi{ MXnJR|UxKD1iMD6wNFEh|ryP NIDnO3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay MWnT[lk> NFrrRYsyKGi{ NX70bHJ5UUN3MDC9JFAvODBzIN88US=> M4PKT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay M2XOV3NnQQ>? M2rNWlEhcHJ? MXXJR|UxKD1iMD6wNFEh|ryP Mk\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M{fyUnNnQQ>? MYWxJIhz MnW5TWM2OCB;IECuNFA{KM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay MnzpV4Y6 M{XmW|EhcHJ? MUfJR|UxKD1iMD6wNFMh|ryP NFS1PZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay NVPBcW1CW2Z7 MYSxJIhz NYLKN4NbUUN3MDC9JFAvODB2IN88US=> M2jzflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay NH6yXm9U\jl? MYWxJIhz Mn3YTWM2OCB;IECuNFA1KM7:TR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay M1\jUXNnQQ>? NWO3[3p{OTBidV2= MVjJR|UxKD1iMD6wNFQh|ryP NVe1N|BHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzNlk3PThpPkK5N|I6PjV6PD;hQi=>
Function assay NF\PbnRU\jl? M37HU|EhcHJ? MVLJR|UxKD1iMD6wNFEh|ryP NYLsZpZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Function assay MVPT[lk> MnLrNUBpeg>? MlfOTWM2OCB;IECuNFAyKM7:TR?= NVHtOFdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Function assay NGDsOnVU\jl? MX:xJIhz NELybIpKSzVyIE2gNE4xODNizszN M1XRWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|M5Lz5{OUi1N|M{QDxxYU6=
Function assay M2j0[XNnQQ>? M1T1OFEhcHJ? MkWyTWM2OCB;IECuNFA1KM7:TR?= NVfhV2N3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Antiproliferative assay MlOxUW9NVTF| NIHFZ2U4OiCqcoO= MUfHTVUxKD1iMD6wNFM{KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay M3vlUm1GSzF? NYKwdmFEPzJiaILz NHTN[WtIUTVyIE2gNE4xODN4IN88US=> NInFdmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NGnyU|hOV0yPMUS= MoDLO|IhcHK| MYfHTVUxKD1iMD6wNFQ2KM7:TR?= M{j2eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay M2H2WGNQVE9{MEW= M4n5OlczKGi{cx?= MoXqS2k2OCB;IECuNFA3QCEQvF2= NXP2W|B6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay M2TPdmhNPjB? MUe3NkBpenN? M4\iPGdKPTBiPTCwMlAxQCEQvF2= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NH;IcmRT[W2xcx?= MkXPO|IhcHK| M4PMdmdKPTBiPTCwMlAxQDZizszN MljRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NUfNRZQ6T0mVVGSx NF\5OYU4OiCqcoO= NWn2RpFWT0l3MDC9JFAvODB6ODFOwG0> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NUD0XVlrXTl|Nx?= MoXyO|IhcHK| NXj3cotrT0l3MDC9JFAvODFizszN NFf5V4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MX\BOFMy MoHqO|IhcHK| NHvkTopIUTVyIE2gNE4xOTFizszN NWHNe|V[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay M2PudXNMVTF? Mo[5O|IhcHK| M2jKVGdKPTBiPTCwMlAyOSEQvF2= NGD4NlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay M3PtSG1GSzJ? M4PxdlczKGi{cx?= MUfHTVUxKD1iMD6wNVEh|ryP M{XtdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MXXBN|c2 MkDrO|IhcHK| MVfHTVUxKD1iMD6wNVEh|ryP MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NHvuT3VQS0lvQV3MNy=> NV\vb2tZPzJiaILz NGjKOGVIUTVyIE2gNE4xOTNizszN MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NVTmOnc1SkVqMjmtUVE4 MX23NkBpenN? NV7FfplpT0l3MDC9JFAvODJzIN88US=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NYrOOFZ1S0iR MX:3NkBpenN? M4WzcWdKPTBiPTCwMlE3KM7:TR?= NXnPdYxlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Function assay MXrOR2kuUDl{OR?= MVewMlAxPSC3TR?= NG\wXFkzPCCqcoO= M4[wSGlvcGmkaYTpc44hd2ZiQ1TLNk1u\WSrYYTl[EBT[iCyaH;zdIhwenmuYYTpc44h[XRiU3XyJFgxPy96MUGgbY4hcHWvYX6gUmNKNUh7MkmgZ4VtdHNiYYSgNE4xODVidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ M{S3VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Function assay MnfaRVY4Ow>? NIKy[m8xNjB3IIXN NGPnfnEzPCCqcoO= NIrjRXlKdmirYnn0bY9vKG:oIFPET|IudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IGPldkA5ODdxOEGxJIlvKGi3bXHuJGE3PzNiY3XscJMh[XRiMD6wOUB2VSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= MmHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Apoptosis assay MnjqUWVEOQ>? MXuwMlAyKHWP MkPvNlQhcHK| M4DIUmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTVXDNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCPQ1ytNUBt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? Ml7iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NU\3fZBDUEx4MB?= NHj5SY0xNjBzIIXN NW\sR2lrOjRiaILz NFzzOFBKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iTVPMMVEhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? MkXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay MnfiUXY1NTFz NILKWGsxNjBzIIXN NYXkRXg3OjRiaILz M1XHdmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHOtUXlEKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| NWHhfpUxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay MYfNSWMy MWOwMlAyKHWP MmXZNlQhcHK| NH21eWpKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3FR|Eh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iYz3NXWMhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? NUO2PZU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay NUPvc2prVVZ2LUGx NYe5VJV7OC5yMTD1US=> MXWyOEBpenN? NXe2R25KUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNWlQuOTFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gUWNNNTFibHX2[Ywh[XRiMD6wNUB2VSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= NFLIRWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Apoptosis assay NWDVS4MxUEx4MB?= MlXiNE4xOSC3TR?= MoO1NlQhcHK| M4[5dWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClLV3ZR{Bt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Cytotoxicity assay Mm[0WVJQWw>? MY[5OkBpenN? MYLJR|UxKD1iMD6wNFYh|ryP M2fqd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6NECvK|5EcEWPQly8M4E,
Function assay M4TKVXUzV1N? MWKxJIhz MYHJR|UxKD1iMD6wNFch|ryP MWW8ZUB1[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
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
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]
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  • 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]
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  • 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.

  • * Indicates a Required Field

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

CDK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID