Name: Dinaciclib (SCH727965)
Brand: Selleck Chemicals
SKU: S2768
Rating: 5 (96 reviews)

Dinaciclib (SCH727965) Chemical Structure

CAS No. 779353-01-4

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

Purity & Quality Control

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CDK Signaling Pathway Map

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 p27^Kip1 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>?

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 ; 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 TopCoun^TM. (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)

References

[4] Fu W, et al. Mol Cancer Ther. 2011, 10(6), 1018-1027.

+ Expand

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. Click to purchase: PEG300	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
Storage	2 years	-80°C	in solvent
Smiles	CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCCC4CCO

Download Dinaciclib (SCH727965) SDF

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:μL Number of animals:

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

Dilution Calculator Molecular Weight Calculator

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

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