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 108 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 NVfP[|dMSXCxcITvd4l{KEG|c3H5 MXKxNFAhdk1? M1:3ZVI1KGh? M2nvbIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MkjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{OEm4PFcoRjJ3Mki5PFg4RC:jPh?=
Kasumi-1 NYThS4Q5SXCxcITvd4l{KEG|c3H5 M2j1RlExOCCwTR?= M4fqXlI1KGh? M4nadIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NF7ES2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK4PVg5Pyd-MkWyPFk5QDd:L3G+
U937 MWfGeY5kfGmxbjDBd5NigQ>? NX\USmd3Oi93L{GwJI5O MWqzJIg> MYnicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NGrCTJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
8226 MnjoSpVv[3Srb36gRZN{[Xl? MX6yM|UwOTBibl2= NEjyTGo1KGh? M1HjZoJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NXPRV5BFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
H929 MmP4SpVv[3Srb36gRZN{[Xl? MkX4Nk82NzFyIH7N NGHZOGg1KGh? Mor1Zoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? NYjub|hbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlI1PjVpPkK0N|YzPDZ3PD;hQi=>
K562 NIDudZRHfW6ldHnvckBCe3OjeR?= MnHlNU42NzNxODDuUS=> NWfs[XgxPiCq MmeyZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? M1n0W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
BaF3/Bcr-abl NEfyNFZHfW6ldHnvckBCe3OjeR?= Mly3NU42NzNxODDuUS=> MYS2JIg> M3\uboJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? M1KxbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
U937  NV7GPZlvTnWwY4Tpc44hSXO|YYm= Mkm4Nk8yOCCwTR?= MX6zJIg> NUPEVZl4[myxY3vzJIlv\HWldHnvckBw\iC[QmCtNZMh[W6mIHTve45{fHKnYX2geIFz\2W2cx?= M{j4[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
1205Lu NXrNcWlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6xNE8{OCCwTR?= NGDBT3Q4OiCq NF74UZhqdmirYnn0d{Bk\WyuIHfyc5d1cCCjbnSgd5Vzfmm4YXy= NYnCW4tyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NlczOjVpPkKzOVI4OjJ3PD;hQi=>
WM1366 MmPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPqNVAwOzBibl2= NFjYVGM4OiCq NVzJWnVUcW6qaXLpeJMh[2WubDDndo94fGhiYX7kJJN2en[rdnHs M2D5TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUK3NlI2Lz5{M{WyO|IzPTxxYU6=
RD MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHxVo5xUUN3ME24MlIhdk1? M2jJRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Rh41 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFWzRXlKSzVyPUGwMlUhdk1? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Rh18 M2L6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTFyLkWgcm0> M{LjfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
Rh30 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXix[YVpUUN3ME25JI5O NYO4XFR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
BT-12 MnnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\FNmhKSzVyPUiuOUBvVQ>? M2DjWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-266 NHvYboFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS0TWM2OD15LkOgcm0> M1HrVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
TC-71 NVvPR2ZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTPcmdCUUN3ME2zMlkhdk1? NXPSVnhjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-9 MkXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTUdVVvUUN3ME24JI5O MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-10 NGPkSGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrCTWM2OD14LkOgcm0> M{D4fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-258 M3T1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;LSYlKSzVyPUmuPUBvVQ>? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
GBM2 M{O3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW3TWM2OD14LkWgcm0> Mm\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NB-1643 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTNwMzDuUS=> NEDHZ|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
NB-EBc1 NX\MdVVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NESzNGpKSzVyPUegcm0> NGfSNJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-90 NYTxUlRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLWeZd6UUN3ME23MlUhdk1? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-136 NWjHNI9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmxPJQ{UUN3ME25Mlghdk1? MmXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
NALM-6 M4Tr[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PTOmlEPTB;ND62JI5O NX\Obnd4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
COG-LL-317 NYHuTIJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTZwNTDuUS=> Mn\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
RS4;11 M321Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\ZbGlEPTB;NT6xJI5O MmXJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
MOLT-4 MmjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTlwMzDuUS=> NV7nVG9bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CCRF-CEM M1fiV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzW[XBKSzVyPUWuOkBvVQ>? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Kasumi-1 NXr0UWhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPnbnpQUUN3ME20MlUhdk1? MmO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Karpas-299 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTNwOTDuUS=> NInTN3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Ramos-RA1 NYi5cm9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX2NYZKSzVyPUeuPUBvVQ>? MlSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
MIAPaCa-2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H5SFczKGh? Mn7US2k2OD1zMDDuUS=> MlXYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5Nki3O|koRjJzN{[4O|c6RC:jPh?=
Pa20C  Ml;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfWcWt3PzJiaB?= NVTRNWdYT0l3ME2yNEBvVQ>? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd4OEe3PUc,OjF5Nki3O|k9N2F-
ML-1 NIntXIVCeG:ydH;zbZMhSXO|YYm= NGrVOm4yNTFyMECgcm0> M4XwbVQhcA>? M2fBc4lv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 M2HIS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c4Lz5{MUe2PFc4PzxxYU6=
Cytotoxicity assay Mlj6UWRCNU2ELUSzOi=> NHfpNWk4OiCqcoO= MkXZTWM2OCB;IECuNFA2KM7:TR?= NUPaWIhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay NF22NodPS0lvSEmyPS=> Mm\4O|IhcHK| NWnxRo15UUN3MDC9JFAvODB3IN88US=> NWSzWW14RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay M4rjO21FSS2PQj2yN|E> NETyOYI4OiCqcoO= MlfvTWM2OCB;IECuNFA2KM7:TR?= M3;rUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay Ml7HV2suTVNvMR?= NV36RoJ7PzJiaILz NGHyWW1KSzVyIE2gNE4xODVizszN M3T0[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay NFOyOIxCPjd| NXvUNVNOPzJiaILz M4nqZ2lEPTBiPTCwMlAxPSEQvF2= MnLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Cytotoxicity assay MYPTT{1DWi1| NWeyVGEzPzJiaILz M3G0S2lEPTBiPTCwMlAxPSEQvF2= NFHDNFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NYS3cIx4VU6QRz3IU3M> NXLY[ItsPzJiaILz NWPvbYpsUUN3MDC9JFAvODB3NTFOwG0> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MWHTT{1WXC1z Mln3O|IhcHK| NV3BPYNKUUN3MDC9JFAvODB4IN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NXnlW|R6XTJ4Nh?= MonwO|IhcHK| MUDJR|UxKD1iMD6wNFYh|ryP M322b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay M1;SR3JRVUlzOEKyOi=> NF\hNFE4OiCqcoO= MkjrTWM2OCB;IECuNFA6KM7:TR?= M4rJXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay NEj1eWZUXzh5Mh?= MlfUO|IhcHK| Mmf0TWM2OCB;IECuNFA6PSEQvF2= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NFTsR|dVPDeG MUS3NkBpenN? NWTyW2Z7UUN3MDC9JFAvODFizszN NGfVeFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Apoptosis assay NUf2[3FZSTZ5Mx?= MmPZNlQhcHK| MojNSWM2OCB;IECuNFEyKM7:TR?= NEnsemg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay NUmyVZVrVUOINx?= NEfYNYQ4OiCqcoO= MXjJR|UxKD1iMD6wNkDPxE1? MlXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Function assay MojKV4Y6 NGr1Z2lKSzVyIE2gNE4xPzJizszN MmfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5NEG4OVMoRjJ4N{SxPFU{RC:jPh?=
Function assay M2DKbJNnQQ>? MmfvTWM2OCB;IECuNFAzKM7:TR?= M1HCZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEWxOVA2Lz5{Nki1NVUxPTxxYU6=
Function assay MXrT[lk> NHq5SmYyKGi{ NVnwdWJ1UUN3MDC9JFAvODBzIN88US=> MlPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay M4[y[nNnQQ>? MVSxJIhz NGPPSHhKSzVyIE2gNE4xODFizszN M16yXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay Ml2wV4Y6 MoCzNUBpeg>? MU\JR|UxKD1iMD6wNFEh|ryP NYXqcplsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay NVnEd2FHW2Z7 MWOxJIhz MX7JR|UxKD1iMD6wNFEh|ryP NIDRSpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay M3P1OXNnQQ>? NEjJU3oyKGi{ M3O1VGlEPTBiPTCwMlAxOyEQvF2= NU[wWHV3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay NELnfZVU\jl? MYCxJIhz MnvTTWM2OCB;IECuNFA{KM7:TR?= NGDkelg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay M4\aUnNnQQ>? MmPiNUBpeg>? MkjWTWM2OCB;IECuNFA1KM7:TR?= M1zXXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay NIrKVWtU\jl? Mn73NUBpeg>? NG\Bc4RKSzVyIE2gNE4xODRizszN NV;FWWlPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay Mn3wV4Y6 M2i2ZlExKHWP MnzaTWM2OCB;IECuNFA1KM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN{OU[1PEc,Ojl|Mkm2OVg9N2F-
Function assay MYnT[lk> NGrkNG4yKGi{ M13uZWlEPTBiPTCwMlAxOSEQvF2= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Function assay MULT[lk> NW\WWItnOSCqch?= MYfJR|UxKD1iMD6wNFEh|ryP NWPGSnJnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Function assay MYfT[lk> M3y1SFEhcHJ? MWnJR|UxKD1iMD6wNFMh|ryP NW\UT3lDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Function assay NXe0ZWUxW2Z7 M{XXZVEhcHJ? NYTOSHR1UUN3MDC9JFAvODB2IN88US=> NUHhUplsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Antiproliferative assay Mn3aUW9NVTF| MYq3NkBpenN? MUjHTVUxKD1iMD6wNFM{KM7:TR?= M2e5clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NHnPR4pOTUNz NX3TVndGPzJiaILz NYW2OGZTT0l3MDC9JFAvODB|NjFOwG0> NXf6O|BPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay MVfNU2xOOTR? NXHxWVhLPzJiaILz NWXSZ5hMT0l3MDC9JFAvODB2NTFOwG0> MoTyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MnTWR29NVzJyNR?= M3TuXVczKGi{cx?= MVrHTVUxKD1iMD6wNFY5KM7:TR?= NHPDPWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MWTIUFYx NHj1eZM4OiCqcoO= M3uzVWdKPTBiPTCwMlAxQCEQvF2= NVjZWos1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay NGiyZlJT[W2xcx?= MV[3NkBpenN? M1\ZNGdKPTBiPTCwMlAxQDZizszN NYHTb5ZrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay NYT6WGozT0mVVGSx MoXrO|IhcHK| NVnNPIM4T0l3MDC9JFAvODB6ODFOwG0> MnvrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay M{f3[nU6Ozd? NG\oR5E4OiCqcoO= M1HoNWdKPTBiPTCwMlAyKM7:TR?= NWTUcXhGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay MXLBOFMy NIjieHM4OiCqcoO= NGjifYFIUTVyIE2gNE4xOTFizszN NGTuO5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MYTTT20y NIHwUIo4OiCqcoO= NYDDe3NwT0l3MDC9JFAvODFzIN88US=> MoHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MlfJUWVEOg>? NF:0SIU4OiCqcoO= MVjHTVUxKD1iMD6wNVEh|ryP NEf3Wog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay MonyRVM4PQ>? NHf1cHk4OiCqcoO= M4jrZ2dKPTBiPTCwMlAyOSEQvF2= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MnLyU2NKNUGPTEO= M17FV|czKGi{cx?= MlTaS2k2OCB;IECuNFE{KM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NFjYWlJDTSh{KT3NNVc> NHXrfI04OiCqcoO= MW\HTVUxKD1iMD6wNlEh|ryP MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NFKwUpNEUE9? MkTkO|IhcHK| MlHvS2k2OCB;IECuNVYh|ryP NXXYVoNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Function assay NFjJU2NPS0lvSEmyPS=> NIG1SFYxNjByNTD1US=> MoTvNlQhcHK| NGjqdoxKdmirYnn0bY9vKG:oIFPET|IudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IGPldkA5ODdxOEGxJIlvKGi3bXHuJG5EUS2KOUK5JINmdGy|IHH0JFAvODB3IIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? NH;5WpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Function assay M2jJVGE3PzN? Mmj5NE4xPSC3TR?= NUnjcGhqOjRiaILz Mom1TY5pcWKrdHnvckBw\iCFRFuyMY1m\GmjdHXkJHJjKHCqb4PwbI9zgWyjdHnvckBifCCVZYKgPFA4NzhzMTDpckBpfW2jbjDBOlc{KGOnbHzzJIF1KDBwMEWgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| NYX4VZZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Apoptosis assay M4f0em1GSzF? MnO4NE4xOSC3TR?= MX:yOEBpenN? MnvYTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPRVOxJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKE2FTD2xJIxmfmWuIHH0JFAvODFidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Apoptosis assay NEfHNpNJVDZy M1[4NlAvODFidV2= NE\CdHgzPCCqcoO= MYjJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hVUOOLUGgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> NXXZTldsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay MVTNWlQuOTF? M{ftNFAvODFidV2= MnnONlQhcHK| M2\xfmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHOtUXlEKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| MoW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay NGLTT4NOTUNz NFyySXoxNjBzIIXN NX3kOGpuOjRiaILz NEjvbW9KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3FR|Eh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iYz3NXWMhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? NF:3WoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Apoptosis assay M1vlO21XPC1zMR?= Mn;hNE4xOSC3TR?= M4CyN|I1KGi{cx?= M4mzfGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIF3DUE0yKGyndnXsJIF1KDBwMEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| NVvLXoNTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay NHXZeGFJVDZy NYDsWWlZOC5yMTD1US=> MnHPNlQhcHK| MorPTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGNvTWnDJIxmfmWuIHH0JFAvODFidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ NIW1flg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Cytotoxicity assay M{W3SnUzV1N? MmjEPVYhcHK| MXvJR|UxKD1iMD6wNFYh|ryP Mly1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh2MD:nQmNpTU2ETEyvZV4>
Function assay MYrVNm9U M{LsbFEhcHJ? MX;JR|UxKD1iMD6wNFch|ryP NGnhOXE9[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.
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.

Solubility (25°C)

In vitro

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

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 LLC 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 2022-08-01)

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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