Dinaciclib (SCH727965)

Catalog No.S2768 Synonyms: PS-095760

For research use only.

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.

Dinaciclib (SCH727965) Chemical Structure

CAS No. 779353-01-4

Selleck's Dinaciclib (SCH727965) has been cited by 96 publications

Purity & Quality Control

Choose Selective CDK Inhibitors

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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 NYLUS|Z[SXCxcITvd4l{KEG|c3H5 NYOyOY83OTByIH7N MnPQNlQhcA>? NHvFeIJqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M1XielxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mki5PFg4Lz5{NUK4PVg5PzxxYU6=
Kasumi-1 M{nnTGFxd3C2b4Ppd{BCe3OjeR?= MVyxNFAhdk1? NX;HPYhoOjRiaB?= NG[5[nNqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M1q5c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mki5PFg4Lz5{NUK4PVg5PzxxYU6=
U937 NETBSmFHfW6ldHnvckBCe3OjeR?= MnjCNk82NzFyIH7N MlXIN{Bp MmfNZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? NXrtSHp2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
8226 NV[0[XZqTnWwY4Tpc44hSXO|YYm= MV6yM|UwOTBibl2= NVHoOJppPCCq MkTjZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? NGPaUlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
H929 MULGeY5kfGmxbjDBd5NigQ>? Mn21Nk82NzFyIH7N MoLiOEBp M37QPIJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NYi0VnBQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
K562 MkD6SpVv[3Srb36gRZN{[Xl? NFzoPIYyNjVxMz:4JI5O M3jOfVYhcA>? NInzV3djdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
BaF3/Bcr-abl M2PyPGZ2dmO2aX;uJGF{e2G7 MmrCNU42NzNxODDuUS=> NIrteHI3KGh? M2q0UYJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NEPZfFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
U937  MX7GeY5kfGmxbjDBd5NigQ>? Mof4Nk8yOCCwTR?= M{HzclMhcA>? MYjicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NYLxRoFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
1205Lu NETTV4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW4NVAwOzBibl2= M2fNSVczKGh? NFKzNHVqdmirYnn0d{Bk\WyuIHfyc5d1cCCjbnSgd5Vzfmm4YXy= NIHGUpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyO|IzPSd-MkO1NlczOjV:L3G+
WM1366 NYnte3VtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHwSG5WOTBxM{Cgcm0> NUWxPYt5PzJiaB?= MVrpcohq[mm2czDj[YxtKGe{b4f0bEBidmRic4Xyeol3[Wx? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV{N{KyOUc,OjN3MkeyNlU9N2F-
RD NYPwXWNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37CUWlEPTB;OD6yJI5O MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Rh41 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjIO5p7UUN3ME2xNE42KG6P NGm4fow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Rh18 M1ftSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHewZ5RKSzVyPUGwMlUhdk1? M3q5W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Rh30 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTlibl2= MmrVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
BT-12 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnhUpBLUUN3ME24MlUhdk1? NX3YRoRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-266 MlzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTdwMzDuUS=> M1v1UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
TC-71 NW\PfZg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXzTWM2OD1|Lkmgcm0> M1vHelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-9 NHvuTVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;JTWM2OD16IH7N M2HlXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-10 NFXSOVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXpU4lKSzVyPU[uN{BvVQ>? NF;yXFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-258 NGDWNmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLrfZJKSzVyPUmuPUBvVQ>? NEH1cXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
GBM2 MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofqTWM2OD14LkWgcm0> MmW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NB-1643 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGT1d|FKSzVyPUOuN{BvVQ>? NFLsU2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
NB-EBc1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e1SWlEPTB;NzDuUS=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-90 NWnwTZVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrJTWM2OD15LkWgcm0> Ml\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CHLA-136 M2rqcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHXNmFCUUN3ME25Mlghdk1? NIX5TVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
NALM-6 NYG5d5BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuzSXNKSzVyPUSuOkBvVQ>? MlXiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
COG-LL-317 NVvtWnkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;FTWM2OD14LkWgcm0> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
RS4;11 NXHRXYVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2T5fmlEPTB;NT6xJI5O MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
MOLT-4 M4O3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTlwMzDuUS=> NHz5eXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CCRF-CEM NHXoTHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv6WG9bUUN3ME21MlYhdk1? MmPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Kasumi-1 MnnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLa[FlRUUN3ME20MlUhdk1? MlrNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Karpas-299 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHTbVBkUUN3ME2zMlkhdk1? NELGcII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Ramos-RA1 MnXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fa[WlEPTB;Nz65JI5O NHjxcVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
MIAPaCa-2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXMVYpoPzJiaB?= M3XXXGdKPTB;MUCgcm0> MortQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5Nki3O|koRjJzN{[4O|c6RC:jPh?=
Pa20C  NFHGenVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPMO|IhcA>? M323O2dKPTB;MkCgcm0> NX7ZWYt5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3Olg4PzlpPkKxO|Y5Pzd7PD;hQi=>
ML-1 NFvBNnJCeG:ydH;zbZMhSXO|YYm= NF:yO3oyNTFyMECgcm0> MlL4OEBp NWH4b5JucW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NGnkdGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe2PFc4Pyd-MkG3Olg4Pzd:L3G+
Cytotoxicity assay Mm\MUWRCNU2ELUSzOi=> MYi3NkBpenN? NVnIb21TUUN3MDC9JFAvODB3IN88US=> MoG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay M2Ljd25EUS2KOUK5 NWTCPHlwPzJiaILz NFHqfpVKSzVyIE2gNE4xODVizszN NI\WTFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay M1u5Tm1FSS2PQj2yN|E> M1rofFczKGi{cx?= M2rZN2lEPTBiPTCwMlAxPSEQvF2= NEHiTVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay MVHTT{1GWy1z MorFO|IhcHK| MXTJR|UxKD1iMD6wNFUh|ryP NHrjd4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NGL0eHlCPjd| MXW3NkBpenN? NH[ycXpKSzVyIE2gNE4xODVizszN NWixcJZDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MVHTT{1DWi1| MkHrO|IhcHK| Mlr3TWM2OCB;IECuNFA2KM7:TR?= MmnaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay MlXMUW5PTy2KT2O= NH7sc2Y4OiCqcoO= NH7t[GVKSzVyIE2gNE4xODV3IN88US=> M3LnO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MYXTT{1WXC1z MlXqO|IhcHK| NXzqc2tpUUN3MDC9JFAvODB4IN88US=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MlPKWVI3Pg>? M{HLTFczKGi{cx?= NYPCfZlpUUN3MDC9JFAvODB4IN88US=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MUPSVG1KOTh{Mk[= MY[3NkBpenN? NXTJXHlRUUN3MDC9JFAvODB7IN88US=> NXX6PZBCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MW\TW|g4Og>? NH\YXnY4OiCqcoO= MV\JR|UxKD1iMD6wNFk2KM7:TR?= M{jhXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay MoPHWFQ4TA>? NHH6clg4OiCqcoO= MY\JR|UxKD1iMD6wNUDPxE1? NEjyfXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Apoptosis assay MUnBOlc{ MYSyOEBpenN? MlTISWM2OCB;IECuNFEyKM7:TR?= M3z2NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay NGXROFROS0Z5 MnrNO|IhcHK| MmLlTWM2OCB;IECuNFIh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Function assay M2TZZ3NnQQ>? NX3G[mRXUUN3MDC9JFAvODd{IN88US=> NFzzTmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke0NVg2Oyd-Mk[3OFE5PTN:L3G+
Function assay NXrtco5xe2Z7 NF;YN|RKSzVyIE2gNE4xODJizszN MmjkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NUG1NFUoRjJ4OEWxOVA2RC:jPh?=
Function assay M{\kcnNnQQ>? NFvFSZkyKGi{ M4nCdGlEPTBiPTCwMlAxOSEQvF2= M1KyclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay MkHtV4Y6 NHvMUGkyKGi{ M3Lu[2lEPTBiPTCwMlAxOSEQvF2= NGCzWmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay Mki3V4Y6 NE\CfGUyKGi{ Ml7UTWM2OCB;IECuNFAyKM7:TR?= MnjCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M2fzNnNnQQ>? MYixJIhz Mkm3TWM2OCB;IECuNFAyKM7:TR?= MnvSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay NXnzNIRjW2Z7 M3P2UFEhcHJ? M2fFPWlEPTBiPTCwMlAxOyEQvF2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay NUnoZpVvW2Z7 NVTteXJsOSCqch?= M2\pWmlEPTBiPTCwMlAxOyEQvF2= NXXFb2pDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay MnSxV4Y6 NGK0eWoyKGi{ NFXNZ21KSzVyIE2gNE4xODRizszN NHnkXW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay NXPXdJM2W2Z7 NEjpb|QyKGi{ NEPTZnpKSzVyIE2gNE4xODRizszN MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Function assay NX3uUlJSW2Z7 M2q1W|ExKHWP NHjPOlBKSzVyIE2gNE4xODRizszN NWjxWlNlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzNlk3PThpPkK5N|I6PjV6PD;hQi=>
Function assay MWrT[lk> NHPFOZoyKGi{ NVr0[Yo4UUN3MDC9JFAvODBzIN88US=> M4TwUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|M5Lz5{OUi1N|M{QDxxYU6=
Function assay MkHIV4Y6 NGfiR4YyKGi{ MkO1TWM2OCB;IECuNFAyKM7:TR?= NHWzR4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N|M{QCd-Mkm4OVM{Ozh:L3G+
Function assay NHPyNXJU\jl? NUTpOpl5OSCqch?= NUPYR5MyUUN3MDC9JFAvODB|IN88US=> MkDuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzN|goRjJ7OEWzN|M5RC:jPh?=
Function assay MWXT[lk> M4jzdVEhcHJ? NGX0VmVKSzVyIE2gNE4xODRizszN MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Antiproliferative assay MV;NU2xOOTN? MW[3NkBpenN? MVTHTVUxKD1iMD6wNFM{KM7:TR?= MkCzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MoXoUWVEOQ>? M2joelczKGi{cx?= M33NWGdKPTBiPTCwMlAxOzZizszN NEfidYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NUnvSVlnVU:OTUG0 M3zNTVczKGi{cx?= NGHOfYxIUTVyIE2gNE4xODR3IN88US=> Mk\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay M{nnNWNQVE9{MEW= NYXxZooyPzJiaILz M4n5fWdKPTBiPTCwMlAxPjhizszN M4G5S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay M{fu[GhNPjB? NWrOWXNXPzJiaILz Mnv4S2k2OCB;IECuNFA5KM7:TR?= M4\pTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NGm3TpdT[W2xcx?= NETzfno4OiCqcoO= MWfHTVUxKD1iMD6wNFg3KM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay M2LCR2dKW1SWMR?= M3KwfVczKGi{cx?= MnjMS2k2OCB;IECuNFA5QCEQvF2= M{LLWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay Ml3FWVk{Pw>? M4L0WVczKGi{cx?= MnHrS2k2OCB;IECuNFEh|ryP NHXhOpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay NGPGSIFCPDNz M13KZVczKGi{cx?= MkPuS2k2OCB;IECuNFEyKM7:TR?= MlTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay NVTDOm1PW0uPMR?= NUTifZh2PzJiaILz NXfaNG9oT0l3MDC9JFAvODFzIN88US=> NGS3cHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MXzNSWMz NFzxZmU4OiCqcoO= M{fKSmdKPTBiPTCwMlAyOSEQvF2= M3;XeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MWDBN|c2 MljkO|IhcHK| MULHTVUxKD1iMD6wNVEh|ryP M4DZNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MYfPR2kuSU2OMx?= MWC3NkBpenN? MVfHTVUxKD1iMD6wNVMh|ryP M2XWT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MVrCSUgzMS2PMUe= NHHWd204OiCqcoO= NWP4TGduT0l3MDC9JFAvODJzIN88US=> NGjHOFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay M2joSWNJVw>? M1jUcVczKGi{cx?= M3ThN2dKPTBiPTCwMlE3KM7:TR?= NYW4PJZ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Function assay NGm3[lJPS0lvSEmyPS=> NEX5TW8xNjByNTD1US=> NHT6fVkzPCCqcoO= NVjabFkzUW6qaXLpeIlwdiCxZjDDSGszNW2nZHnheIVlKFKkIIDoc5NxcG:{eXzheIlwdiCjdDDT[ZIhQDB5L{ixNUBqdiCqdX3hckBPS0lvSEmyPUBk\WyuczDheEAxNjByNTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? NUTkWlFyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Function assay NFfZZmpCPjd| NVnqPGZ2OC5yNTD1US=> M{TpXFI1KGi{cx?= MY\Jcohq[mm2aX;uJI9nKEOGS{KtcYVlcWG2ZXSgVoIheGixc4Doc5J6dGG2aX;uJIF1KFOncjC4NFcwQDFzIHnuJIh2dWGwIFG2O|Mh[2WubIOgZZQhOC5yNTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? M3;wWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Apoptosis assay NIfyO4hOTUNz NV2xRo5tOC5yMTD1US=> NW\FeVFwOjRiaILz MlniTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPRVOxJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKE2FTD2xJIxmfmWuIHH0JFAvODFidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ M4nvRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Apoptosis assay MWXIUFYx MWewMlAyKHWP NVnleVVEOjRiaILz M1TPWGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCPQ1ytNUBt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? NUG4dZI6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay MVrNWlQuOTF? NI[4RoUxNjBzIIXN M2S3OlI1KGi{cx?= M365SGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHOtUXlEKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay MWfNSWMy NGCwOm4xNjBzIIXN MWeyOEBpenN? NHz0bVBKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3FR|Eh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iYz3NXWMhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay NUfLbJRYVVZ2LUGx MV6wMlAyKHWP NHPSVJczPCCqcoO= MnKxTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPVkStNVEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iTVPMMVEhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay MojCTGw3OA>? NIHK[4QxNjBzIIXN M3mxeVI1KGi{cx?= MmfTTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGNvTWnDJIxmfmWuIHH0JFAvODFidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ NFvjOlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Cytotoxicity assay M4T0e3UzV1N? NGnK[2I6PiCqcoO= MW\JR|UxKD1iMD6wNFYh|ryP NUf0UY5pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i0NE8oRkOqRV3CUFww[T5?
Function assay M2S2fnUzV1N? MorzNUBpeg>? MmCwTWM2OCB;IECuNFA4KM7:TR?= NEDFdJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OESwM{c,S2iHTVLMQE9iRg>?
Assay
Methods Test Index PMID
Western blot Mcl-1 / Bcl-2 / Bcl-xl / Bax / Bak / PUMA / Noxa ; Cleaved PARP / c-Myc ; Survivin ; RNAP II (P-Ser2/P-Ser5) 28714472 25289887 28207834
Growth inhibition assay Cell viability ; Cell viability 27378523 28361959
Immunofluorescence cyclin B1 / α-tubulin / Aurora A ; OCT4 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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

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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.

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