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 102 publications

Purity & Quality Control

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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 MXHBdI9xfG:|aYOgRZN{[Xl? MXKxNFAhdk1? NX3GcmZoOjRiaB?= NE[wfoZqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ6OUi4O{c,OjV{OEm4PFc9N2F-
Kasumi-1 MmDuRZBweHSxc3nzJGF{e2G7 MWexNFAhdk1? MWCyOEBp M4rUSYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NYOzOGxFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPFk5QDdpPkK1Nlg6QDh5PD;hQi=>
U937 MUPGeY5kfGmxbjDBd5NigQ>? M1\lTlIwPS9zMDDuUS=> M{ewc|MhcA>? M3XycoJtd2OtczDpcoR2[3Srb36gc4YhYEKSLUHzJIFv\CCmb4fud5Rz\WGvIIThdodmfHN? NFXFS5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
8226 M{TGNmZ2dmO2aX;uJGF{e2G7 MmjKNk82NzFyIH7N MoHIOEBp NWjSeVZm[myxY3vzJIlv\HWldHnvckBw\iC[QmCtNZMh[W6mIHTve45{fHKnYX2geIFz\2W2cx?= M{XuWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
H929 NUTyNpozTnWwY4Tpc44hSXO|YYm= NWT2VpB6Oi93L{GwJI5O NE\EN4Y1KGh? MkP4Zoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MkS2OUc,OjR|NkK0OlU9N2F-
K562 M{LRO2Z2dmO2aX;uJGF{e2G7 NYn4U|lKOS53L{OvPEBvVQ>? MWS2JIg> MmTSZoxw[2u|IHnu[JVkfGmxbjDv[kBZSlBvMYOgZY5lKGSxd37zeJJm[W1idHHy[4V1ew>? M3XNOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[yOFY2Lz5{NEO2NlQ3PTxxYU6=
BaF3/Bcr-abl NW\iXGhiTnWwY4Tpc44hSXO|YYm= NUfkVFB[OS53L{OvPEBvVQ>? MoHZOkBp NFH3O|BjdG:la4OgbY5lfWO2aX;uJI9nKFiEUD2xd{BidmRiZH;3cpN1emWjbTD0ZZJo\XS| MknDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkK0OlUoRjJ2M{[yOFY2RC:jPh?=
U937  NIHwbotHfW6ldHnvckBCe3OjeR?= NYrqZXYzOi9zMDDuUS=> NEHEepo{KGh? MWnicI9kc3NiaX7keYN1cW:wIH;mJHhDWC1zczDhcoQh\G:5boP0doVidSC2YYLn[ZR{ NETGNFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2NlQ3PSd-MkSzOlI1PjV:L3G+
1205Lu MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnlV5oyOC9|MDDuUS=> NWDySm56PzJiaB?= Mn\1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W6mIIP1dpZqfmGu MmnGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MkeyNlUoRjJ|NUK3NlI2RC:jPh?=
WM1366 MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4T1[FExNzNyIH7N MYO3NkBp M3znc4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGwZDDzeZJ3cX[jbB?= M1XXbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUK3NlI2Lz5{M{WyO|IzPTxxYU6=
RD NXTBTIFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;I[mVKSzVyPUiuNkBvVQ>? NI\yTmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Rh41 NFvMeYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LoOGlEPTB;MUCuOUBvVQ>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
Rh18 M33B[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4qyNWlEPTB;MUCuOUBvVQ>? NXrCenl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Rh30 MkS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m3VWlEPTB;OTDuUS=> NYT6XnhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
BT-12 MkS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j5TWlEPTB;OD61JI5O NYO0WJlMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-266 NWLFWIN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HwW2lEPTB;Nz6zJI5O MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
TC-71 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD4e2xIUUN3ME2zMlkhdk1? NWDJNmJIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-9 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jWZWlEPTB;ODDuUS=> NYTO[ZZSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
CHLA-10 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTZwMzDuUS=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
CHLA-258 MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTlwOTDuUS=> M120VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
GBM2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\mTWM2OD14LkWgcm0> NVv0Z5NRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
NB-1643 M{njVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fVWWlEPTB;Mz6zJI5O NUS2enVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
NB-EBc1 M3nDWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DCSGlEPTB;NzDuUS=> NFn0e3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
CHLA-90 M4TKT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfvbW5KSzVyPUeuOUBvVQ>? M4XHdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
CHLA-136 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nkNGlEPTB;OT64JI5O MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjNzNUK0NEc,OjJ|MUWyOFA9N2F-
NALM-6 M13DeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS0TWM2OD12Lk[gcm0> NYrCeWQ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
COG-LL-317 NGLJV|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HsW2lEPTB;Nj61JI5O NVywbo1qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
RS4;11 NYraPVU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonJTWM2OD13LkGgcm0> M2\VTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{G1NlQxLz5{MkOxOVI1ODxxYU6=
MOLT-4 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTlwMzDuUS=> MkTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
CCRF-CEM MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHpXW1KSzVyPUWuOkBvVQ>? MnzKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
Kasumi-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTRwNTDuUS=> NGTlVlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOxOVI1OCd-MkKzNVUzPDB:L3G+
Karpas-299 M3z4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITibldKSzVyPUOuPUBvVQ>? NVPWendIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNVUzPDBpPkKyN|E2OjRyPD;hQi=>
Ramos-RA1 MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXneHZKSzVyPUeuPUBvVQ>? Moq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MUWyOFAoRjJ{M{G1NlQxRC:jPh?=
MIAPaCa-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi3NkBp MX\HTVUxRTFyIH7N M2nQcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c6Lz5{MUe2PFc4QTxxYU6=
Pa20C  MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjmTWluPzJiaB?= MmPmS2k2OD1{MDDuUS=> M{Li[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{[4O|c6Lz5{MUe2PFc4QTxxYU6=
ML-1 MkLpRZBweHSxc3nzJGF{e2G7 NITkNVUyNTFyMECgcm0> M3fOPFQhcA>? MkmxbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NWTuN|l1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3Olg4PzdpPkKxO|Y5Pzd5PD;hQi=>
Cytotoxicity assay MULNSGEuVUJvNEO2 MUO3NkBpenN? MWHJR|UxKD1iMD6wNFUh|ryP MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MUHOR2kuUDl{OR?= M2TvUFczKGi{cx?= M{Lx[GlEPTBiPTCwMlAxPSEQvF2= M3ezWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Cytotoxicity assay M{PSVG1FSS2PQj2yN|E> MoL0O|IhcHK| NVTwcmZrUUN3MDC9JFAvODB3IN88US=> NUm1[GNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MlvPV2suTVNvMR?= M2nHdlczKGi{cx?= MUPJR|UxKD1iMD6wNFUh|ryP NWP2PWg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay Mn;BRVY4Ow>? NYTKbllOPzJiaILz NF\KeIlKSzVyIE2gNE4xODVizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NYm4dnZNW0tvQmKtNy=> NXjneJVMPzJiaILz MoDaTWM2OCB;IECuNFA2KM7:TR?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay Mm\sUW5PTy2KT2O= MYi3NkBpenN? Mn7wTWM2OCB;IECuNFA2PSEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NF76NWxUUy2XVD2x NEDUdGw4OiCqcoO= NHr0TllKSzVyIE2gNE4xODZizszN MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay MWjVNlY3 MVi3NkBpenN? NY\DWHRMUUN3MDC9JFAvODB4IN88US=> NICwPVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay M4rnOXJRVUlzOEKyOi=> NFzpXok4OiCqcoO= NVv3cGRpUUN3MDC9JFAvODB7IN88US=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Cytotoxicity assay NUnlVIVyW1d6N{K= MWi3NkBpenN? MlXuTWM2OCB;IECuNFA6PSEQvF2= NX;ldZVyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NFA6OjVpPkKzOlAxQTJ3PD;hQi=>
Cytotoxicity assay MnfjWFQ4TA>? MXu3NkBpenN? MoXGTWM2OCB;IECuNFEh|ryP MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Apoptosis assay MlviRVY4Ow>? NX\kZ2h4OjRiaILz NX[zUWYxTUN3MDC9JFAvODFzIN88US=> NGfwNY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFkzPSd-MkO2NFA6OjV:L3G+
Cytotoxicity assay MXzNR2Y4 NYS4VmY5PzJiaILz M2\MZmlEPTBiPTCwMlAzKM7:TR?= M3jOZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkCwPVI2Lz5{M{[wNFkzPTxxYU6=
Function assay MXjT[lk> MnvpTWM2OCB;IECuNFczKM7:TR?= NV6xVVVDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OFE5PTNpPkK2O|QyQDV|PD;hQi=>
Function assay NG\ZXnZ{\jl? M2LM[2lEPTBiPTCwMlAxOiEQvF2= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh3MUWwOUc,OjZ6NUG1NFU9N2F-
Function assay MV\T[lk> M{TYV|EhcHJ? NXTnTYV7UUN3MDC9JFAvODBzIN88US=> NYnE[m5PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Function assay NH;sT3ZU\jl? MY[xJIhz NFHOUWZKSzVyIE2gNE4xODFizszN M3Li[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay M{LP[XNnQQ>? Ml3MNUBpeg>? NY\xS5RTUUN3MDC9JFAvODBzIN88US=> M1nPdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay NX7mWpozW2Z7 NHu1PVEyKGi{ MmTxTWM2OCB;IECuNFAyKM7:TR?= Mo[zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Function assay NGnIbI5U\jl? M{HoZlEhcHJ? Mn\QTWM2OCB;IECuNFA{KM7:TR?= M{\MSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
Function assay M2\TTHNnQQ>? NHvvTpgyKGi{ NGHYNplKSzVyIE2gNE4xODNizszN NIXZeVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay MkLSV4Y6 MVyxJIhz MYjJR|UxKD1iMD6wNFQh|ryP NHvtdJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay NVzJR5g3W2Z7 M3z3RVEhcHJ? NViwbplbUUN3MDC9JFAvODB2IN88US=> NGS5VYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Function assay M{W2T3NnQQ>? NV34[XlyOTBidV2= MnyxTWM2OCB;IECuNFA1KM7:TR?= MoLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl|Mkm2OVgoRjJ7M{K5OlU5RC:jPh?=
Function assay M3LpZXNnQQ>? NVfkU4lROSCqch?= MnizTWM2OCB;IECuNFAyKM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{OzPEc,Ojl6NUOzN|g9N2F-
Function assay NIHKU2dU\jl? M1TDTVEhcHJ? NUDLfodxUUN3MDC9JFAvODBzIN88US=> NV7ScHBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Function assay MWXT[lk> NXOwfpdQOSCqch?= M123dGlEPTBiPTCwMlAxOyEQvF2= NYLNcVNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{OzhpPkK5PFU{OzN6PD;hQi=>
Function assay MlXhV4Y6 Mlu2NUBpeg>? NFPFUpVKSzVyIE2gNE4xODRizszN NI\l[FI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N|M{QCd-Mkm4OVM{Ozh:L3G+
Antiproliferative assay NG[4[WJOV0yPMUO= MW[3NkBpenN? NUnscIIxT0l3MDC9JFAvODB|MzFOwG0> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MnHTUWVEOQ>? M1nPN|czKGi{cx?= NGTCUm1IUTVyIE2gNE4xODN4IN88US=> M{f6d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NF\3OlhOV0yPMUS= MoHiO|IhcHK| MmmxS2k2OCB;IECuNFA1PSEQvF2= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NIrQ[WhEV0yRMkC1 M{jpPVczKGi{cx?= M{PVbmdKPTBiPTCwMlAxPjhizszN NUHVelNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay M2fyeGhNPjB? NHS3OIY4OiCqcoO= NVLJT5F4T0l3MDC9JFAvODB6IN88US=> NUnEcIxKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay MV3SZY1wew>? NUjsSHA3PzJiaILz MkPCS2k2OCB;IECuNFA5PiEQvF2= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay MV\HTXNVXDF? MoH2O|IhcHK| MmS1S2k2OCB;IECuNFA5QCEQvF2= NEfDPI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Antiproliferative assay M2LofXU6Ozd? MlrOO|IhcHK| NWnpV45vT0l3MDC9JFAvODFizszN MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ3M{O0Okc,OzB{NUOzOFY9N2F-
Antiproliferative assay NF7Yd5dCPDNz NFy5PHg4OiCqcoO= NInZZnFIUTVyIE2gNE4xOTFizszN NUHMNJFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Antiproliferative assay MYfTT20y Mn\jO|IhcHK| NVHKe5hLT0l3MDC9JFAvODFzIN88US=> MnrUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Antiproliferative assay MYDNSWMz M4L0WlczKGi{cx?= NEfoSWRIUTVyIE2gNE4xOTFizszN M4[2ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay MX\BN|c2 NFu1fGs4OiCqcoO= MX3HTVUxKD1iMD6wNVEh|ryP M{nyZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NGi1SpVQS0lvQV3MNy=> NFvqNYU4OiCqcoO= MoL4S2k2OCB;IECuNFE{KM7:TR?= M{DXO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NEe1[|dDTSh{KT3NNVc> MkT3O|IhcHK| MYnHTVUxKD1iMD6wNlEh|ryP M{K5ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Antiproliferative assay NX7JfGp{S0iR NHiwOVQ4OiCqcoO= NUOxSJVpT0l3MDC9JFAvOTZizszN NW\DN3U2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Function assay NH7mN2lPS0lvSEmyPS=> NGnSWIwxNjByNTD1US=> MYSyOEBpenN? NVHlemFUUW6qaXLpeIlwdiCxZjDDSGszNW2nZHnheIVlKFKkIIDoc5NxcG:{eXzheIlwdiCjdDDT[ZIhQDB5L{ixNUBqdiCqdX3hckBPS0lvSEmyPUBk\WyuczDheEAxNjByNTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? Mme3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MEC5NlUoRjJ|NkCwPVI2RC:jPh?=
Function assay M1nybGE3PzN? MVywMlA2KHWP M3;lPFI1KGi{cx?= Mmf1TY5pcWKrdHnvckBw\iCFRFuyMY1m\GmjdHXkJHJjKHCqb4PwbI9zgWyjdHnvckBifCCVZYKgPFA4NzhzMTDpckBpfW2jbjDBOlc{KGOnbHzzJIF1KDBwMEWgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZyMEmyOUc,OjN4MEC5NlU9N2F-
Apoptosis assay NU\lVWRyVUWFMR?= NXrFSWRiOC5yMTD1US=> MmXFNlQhcHK| MXfJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2HQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hVUOOLUGgcIV3\WxiYYSgNE4xOSC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> M4fwVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkWzN|Q3Lz5|MEK1N|M1PjxxYU6=
Apoptosis assay M2n2XGhNPjB? MYKwMlAyKHWP NGnvNHkzPCCqcoO= NEnoU3lKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iTVPMMVEhdGW4ZXygZZQhOC5yMTD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? Mnf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NUOzOFYoRjNyMkWzN|Q3RC:jPh?=
Apoptosis assay Ml3NUXY1NTFz M3TRdFAvODFidV2= MoXlNlQhcHK| NFnu[pFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3WOE0yOSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDjMW1[SyCuZY\lcEBifCByLkCxJJVOKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91fGmwZzDhcoFtgXOrcx?= NGLZN|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Apoptosis assay NEHaXWFOTUNz NYLiWoo5OC5yMTD1US=> MViyOEBpenN? M2Owc2lv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTVXDNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClLV3ZR{Bt\X[nbDDheEAxNjBzIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0eIlv\yCjbnHsfZNqew>? NXX1RmlXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay Mn7OUXY1NTFz M3\XTFAvODFidV2= M3LoWlI1KGi{cx?= NG\BN3lKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3WOE0yOSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDNR2wuOSCuZY\lcEBifCByLkCxJJVOKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91fGmwZzDhcoFtgXOrcx?= NYD6[od{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOVM{PDZpPkOwNlU{OzR4PD;hQi=>
Apoptosis assay NV36S|dTUEx4MB?= Mnn0NE4xOSC3TR?= M{Lm[FI1KGi{cx?= MnzITY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGNvTWnDJIxmfmWuIHH0JFAvODFidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ NFjCbW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK1N|M1Pid-M{CyOVM{PDZ:L3G+
Cytotoxicity assay NGTTWZFWOk:V MWC5OkBpenN? NHqyWmlKSzVyIE2gNE4xODZizszN MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDRyLze+R4hGVUKOPD;hQi=>
Function assay M{LwXnUzV1N? MkHPNUBpeg>? NYLXflA1UUN3MDC9JFAvODB5IN88US=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDRyLze+R4hGVUKOPD;hQi=>
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

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

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 2022-01-17)

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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