製品番号: HY-10492

Dinaciclib

(別名: SCH 727965)

56 Cited Publications

カスタマーレビュー

Based on 56 publication(s) in Google Scholar

Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC₅₀s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.

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純度: 99.80%
CAS 番号: 779353-01-4
分子式: C₂₁H₂₈N₆O₂
分子量:396.49

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Dinaciclib 構造式

CAS 番号: 779353-01-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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製品説明

Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC₅₀s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively^[1].

IC₅₀ & Target^[1]

CDK2

1 nM (IC₅₀)

CDK5

1 nM (IC₅₀)

CDK1

3 nM (IC₅₀)

CDK9

4 nM (IC₅₀)

CDK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	28.11 nM Compound: 1; SCH727965; MK-7965	Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
A-375	GI₅₀	0.011 μM Compound: 7; SCH727965	Antiproliferative activity against human A375 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human A375 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
A-431	GI₅₀	0.011 μM Compound: 7; SCH727965	Antiproliferative activity against human A431 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human A431 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
A549	CC₅₀	>100 μM Compound: 10; SCH 727965	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 33539089]
A549	GI₅₀	0.006 μM Compound: Dinaciclib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 36054949]
A673	EC₅₀	0.011 μM Compound: dinaciclib	Induction of apoptosis in human A673 cells assessed as caspase-3 activation after 24 hrs by luminescence assay Induction of apoptosis in human A673 cells assessed as caspase-3 activation after 24 hrs by luminescence assay	[PMID: 23600925]
A673	IC₅₀	<0.005 μM Compound: dinaciclib	Cytotoxicity against human A673 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human A673 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
BT-474	GI₅₀	0.01 μM Compound: Dinaciclib	Antiproliferative activity against trastuzumab-sensitive HER2-positive human BT-474 cells by Cell Titer Glo assay Antiproliferative activity against trastuzumab-sensitive HER2-positive human BT-474 cells by Cell Titer Glo assay	[PMID: 38061230]
BT-549	IC₅₀	>10 μM Compound: dinaciclib	Cytotoxicity against human BT549 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human BT549 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
BT-549	IC₅₀	10.43 nM Compound: 1; SCH727965; MK-7965	Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
CCRF-CEM	IC₅₀	0.007 μM Compound: SCH727965	Antiproliferative activity against human CEM cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human CEM cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
CHO	GI₅₀	0.16 μM Compound: 7; SCH727965	Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
COLO 205	GI₅₀	0.0068 μM Compound: 7; SCH727965	Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
DB	GI₅₀	0.014 μM Compound: DIN	Antiproliferative activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis Antiproliferative activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis	[PMID: 35749742]
G-361	IC₅₀	0.016 μM Compound: SCH727965	Antiproliferative activity against human G361 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human G361 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
GISTT1	GI₅₀	0.0088 μM Compound: 7; SCH727965	Antiproliferative activity against human GISTT1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human GISTT1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
HCT-116	GI₅₀	0.009 μM Compound: Dinaciclib	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 36054949]
HCT-116	IC₅₀	0.007 μM Compound: SCH727965	Antiproliferative activity against human HCT116 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
HEK-293T	IC₅₀	0.023 μM Compound: Dinaciclib	Antiproliferative activity against human HEK293T cells assessed as cell growth inhibition incubated for 48 hrs Antiproliferative activity against human HEK293T cells assessed as cell growth inhibition incubated for 48 hrs	[PMID: 35143203]
HeLa	IC₅₀	0.013 μM Compound: SCH727965	Antiproliferative activity against human HeLa cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HeLa cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
HL-60	GI₅₀	0.008 μM Compound: 7; SCH727965	Antiproliferative activity against human HL60 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human HL60 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
HOS-TE85	IC₅₀	0.0055 μM Compound: dinaciclib	Cytotoxicity against human MNNG-HOS cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human MNNG-HOS cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
HT	GI₅₀	0.019 μM Compound: SCH727965	Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
HT	IC₅₀	0.019 μM Compound: SCH727965	Antiproliferative activity against human HT cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HT cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
JeKo-1	IC₅₀	0.014 μM Compound: SCH727965	Antiproliferative activity against human JeKo1 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human JeKo1 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
JIMT-1	GI₅₀	0.023 μM Compound: Dinaciclib	Antiproliferative activity against trastuzumab-resistant HER2-positive human JIMT-1 cells by Cell Titer Glo assay Antiproliferative activity against trastuzumab-resistant HER2-positive human JIMT-1 cells by Cell Titer Glo assay	[PMID: 38061230]
K562	IC₅₀	0.011 μM Compound: SCH727965	Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
K562	IC₅₀	0.013 μM Compound: Dinaciclib	Antiproliferative activity against human K562 cells assessed as cell death measured after 72 hrs by resazurin dye based assay Antiproliferative activity against human K562 cells assessed as cell death measured after 72 hrs by resazurin dye based assay	[PMID: 34288692]
Maver1	IC₅₀	0.017 μM Compound: SCH727965	Antiproliferative activity against human Maver1 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human Maver1 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
MCF7	GI₅₀	0.012 μM Compound: Dinaciclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 36054949]
MCF7	IC₅₀	0.006 μM Compound: SCH727965	Antiproliferative activity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
MCF7	IC₅₀	0.02 μM Compound: dinaciclib	Cytotoxicity against human MCF7 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human MCF7 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
MDA-MB-231	IC₅₀	<0.005 μM Compound: dinaciclib	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
MDA-MB-231	IC₅₀	13.4 nM Compound: 1; SCH727965; MK-7965	Inhibition of cell viability in human MDA-MB-231 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human MDA-MB-231 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
MDA-MB-436	IC₅₀	<0.005 μM Compound: dinaciclib	Cytotoxicity against human MDA-MB-436 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human MDA-MB-436 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
MDA-MB-468	IC₅₀	11.85 nM Compound: 1; SCH727965; MK-7965	Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
MM1.S	IC₅₀	3.63 nM Compound: 1; SCH727965; MK-7965	Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
MOLM-13	GI₅₀	0.0033 μM Compound: 7; SCH727965	Antiproliferative activity against human MOLM13 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MOLM13 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MOLM-14	GI₅₀	0.0045 μM Compound: 7; SCH727965	Antiproliferative activity against human MOLM14 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MOLM14 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MV4-11	IC₅₀	0.007 μM Compound: Dinaciclib	Antiproliferative activity against human MV4-11 cells assessed as cell death measured after 72 hrs by resazurin dye based assay Antiproliferative activity against human MV4-11 cells assessed as cell death measured after 72 hrs by resazurin dye based assay	[PMID: 34288692]
NCI-H929	IC₅₀	<0.005 μM Compound: dinaciclib	Cytotoxicity against human NCI-H929 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human NCI-H929 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
NU-DUL-1	GI₅₀	0.01 μM Compound: DIN	Antiproliferative activity against human NU-DUL-1 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis Antiproliferative activity against human NU-DUL-1 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis	[PMID: 35749742]
OCI-AML-3	GI₅₀	0.013 μM Compound: 7; SCH727965	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
OCI-LY19	GI₅₀	0.02 μM Compound: DIN	Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis	[PMID: 35749742]
OCI-Ly7	IC₅₀	0.002 μM Compound: SCH727965	Antiproliferative activity against human OCI-LY7 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human OCI-LY7 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
Raji	IC₅₀	0.025 μM Compound: SCH727965	Antiproliferative activity against human Raji cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human Raji cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
Ramos	GI₅₀	0.0086 μM Compound: 7; SCH727965	Antiproliferative activity against human Ramos cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human Ramos cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
Ramos	IC₅₀	0.015 μM Compound: SCH727965	Antiproliferative activity against human Ramos cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human Ramos cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
RPMI-8226	IC₅₀	0.009 μM Compound: SCH727965	Antiproliferative activity against human RPMI8226 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human RPMI8226 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
Sf9	IC₅₀	0.002 μM Compound: SCH727965	Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	0.002 μM Compound: SCH-727965	Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP	[PMID: 26851505]
Sf9	IC₅₀	0.015 μM Compound: SCH727965	Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3 Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3	[PMID: 30943029]
Sf9	IC₅₀	0.067 μM Compound: SCH727965	Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g	[PMID: 30943029]
Sf9	IC₅₀	0.072 μM Compound: Dinaciclib	Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP	[PMID: 26741853]
Sf9	IC₅₀	0.072 μM Compound: SCH727965	Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	0.115 μM Compound: SCH727965	Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	0.17 μM Compound: SCH727965	Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2 Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2	[PMID: 30943029]
Sf9	IC₅₀	1 nM Compound: 11; SCH727965	Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	1 nM Compound: 11; SCH727965	Inhibition of recombinant CDK2/cyclin A (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis Inhibition of recombinant CDK2/cyclin A (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	1 nM Compound: 11; SCH727965	Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	1 nM Compound: 11; SCH727965	Inhibition of recombinant CDK5/p25 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis Inhibition of recombinant CDK5/p25 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	1 nM Compound: 3; SCH 727965	Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method	[PMID: 30978559]
Sf9	IC₅₀	1 nM Compound: 3; SCH 727965	Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method	[PMID: 30978559]
Sf9	IC₅₀	1 nM Compound: MK7965; SCH727965	Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method	[PMID: 30543440]
Sf9	IC₅₀	1 nM Compound: MK7965; SCH727965	Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method	[PMID: 30543440]
Sf9	IC₅₀	3 nM Compound: 11; SCH727965	Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	3 nM Compound: 11; SCH727965	Inhibition of recombinant CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis Inhibition of recombinant CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	3 nM Compound: 3; SCH 727965	Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method	[PMID: 30978559]
Sf9	IC₅₀	3 nM Compound: MK7965; SCH727965	Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method	[PMID: 30543440]
Sf9	IC₅₀	4 nM Compound: 11; SCH727965	Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	4 nM Compound: 11; SCH727965	Inhibition of recombinant CDK9/cyclin T (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis Inhibition of recombinant CDK9/cyclin T (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis	[PMID: 27171036]
Sf9	IC₅₀	4 nM Compound: 3; SCH 727965	Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method	[PMID: 30978559]
Sf9	IC₅₀	4 nM Compound: MK7965; SCH727965	Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method	[PMID: 30543440]
SK-BR-3	IC₅₀	<0.005 μM Compound: dinaciclib	Cytotoxicity against human SK-BR-3 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human SK-BR-3 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
SK-ES1	IC₅₀	<0.005 μM Compound: dinaciclib	Cytotoxicity against human SK-ES-1 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human SK-ES-1 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
SKM-1	GI₅₀	0.011 μM Compound: 7; SCH727965	Antiproliferative activity against human SKM1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human SKM1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
SK-N-BE(2)-M17	GI₅₀	0.021 μM Compound: 7; SCH727965	Antiproliferative activity against human BE(2)-M17 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human BE(2)-M17 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
SK-UT-1	IC₅₀	0.006 μM Compound: dinaciclib	Cytotoxicity against human SK-UT-1 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human SK-UT-1 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
SUD4	GI₅₀	0.009 μM Compound: DIN	Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis	[PMID: 35749742]
SUD4	IC₅₀	0.01 μM Compound: SCH727965	Antiproliferative activity against human SUDHL4 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human SUDHL4 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
SW480	GI₅₀	0.008 μM Compound: Dinaciclib	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 36054949]
SW872	IC₅₀	0.0095 μM Compound: dinaciclib	Cytotoxicity against human SW872 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human SW872 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
T47D	IC₅₀	0.01 μM Compound: dinaciclib	Cytotoxicity against human T47D cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human T47D cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
T-cell	IC₅₀	4 nM Compound: 16; SCH-727965	Inhibition of CDK9/Cyclin T (unknown origin) Inhibition of CDK9/Cyclin T (unknown origin)	[PMID: 35485642]
THP-1	IC₅₀	0.007 μM Compound: SCH727965	Antiproliferative activity against human THP1 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human THP1 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
TMD8	IC₅₀	0.017 μM Compound: SCH727965	Antiproliferative activity against human TMD8 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human TMD8 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
U-266	IC₅₀	0.006 μM Compound: dinaciclib	Cytotoxicity against human U266 cells after 72 hrs by resazurin/resorufin-based fluorescence assay Cytotoxicity against human U266 cells after 72 hrs by resazurin/resorufin-based fluorescence assay	[PMID: 23600925]
U2932	GI₅₀	0.011 μM Compound: DIN	Antiproliferative activity against human U2932 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis Antiproliferative activity against human U2932 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis	[PMID: 35749742]
U2932	IC₅₀	0.011 μM Compound: SCH727965	Antiproliferative activity against human U2932 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human U2932 cells assessed as growth inhibition measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
U2OS	IC₅₀	6 nM Compound: 27	Cytotoxicity against human U2OS cells assessed as growth inhibition after 96 hrs by SRB assay Cytotoxicity against human U2OS cells assessed as growth inhibition after 96 hrs by SRB assay	[PMID: 27746890]
U2OS	IC₅₀	7 nM Compound: 27	Inhibition of 17AAG-induced HSF1-mediated HSP72 expression in human U2OS cells preincubated for 1 hr followed by 17AAG addition measured after 18 hrs by ELISA Inhibition of 17AAG-induced HSF1-mediated HSP72 expression in human U2OS cells preincubated for 1 hr followed by 17AAG addition measured after 18 hrs by ELISA	[PMID: 27746890]
U-937	GI₅₀	0.01 μM Compound: 7; SCH727965	Antiproliferative activity against human U937 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human U937 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]

体外実験

Dinaciclib (SCH 727965) is a potent DNA replication inhibitor that blocks thymidine (dThd) DNA incorporation in A2780 cells with an IC₅₀ of 4 nM. Dinaciclib (100 nM) inhibits phosphorylation of the retinoblastoma (Rb) tumor suppressor protein and induces accumulation of the p85 PARP caspase cleavage product^[1]. In vitro cell growth of pancreatic cancer cells is inhibited by Dinaciclib (SCH727965) in a dose-dependent manner. Upon incubation with Dinaciclib for 72 h, the GI50s are approximately 10 and 20 nM for MIAPaCa-2 and Pa20C cells, respectively. These results are consistent with studies of Dinaciclib in other cancer cell lines. In soft agar assays, 5 to 10 nM of Dinaciclib significantly reduces colony formation and anchorage independent growth of MIAPaCa-2 cells. Moreover, in vitro cell migration of Pa20C and MIAPaCa-2 cells is significantly reduced by Dinaciclib-concentrations starting from 2-5 nM, as demonstrated using BD FluoroChrom, modified Boyden Chamber and wound healing assays^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Dinaciclib (8, 16, 32, and 48 mg/kg, i.p.) results in tumor inhibition by 70%, 70%, 89%, and 96%, respectively; Dinaciclib (SCH 727965) is well tolerated, and the maximum body weight loss in the highest dosage group is 5%. Dinaciclib has a short plasma half-life in mouse. A dose of 5 mg/kg Dinaciclib given i.p. in mice is associated with a plasma half-life of ~0.25 hour^[1]. Treatment with Dinaciclib (SCH727965) given as twice weekly i.p. doses of 40 mg/kg for 4 weeks causes significant tumor growth inhibition (TGI) in 10/10 (100%) of low-passage subcutaneous pancreatic xenografts tested^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 779353-01-4
性状 Solid
分子量 396.49
分子式 C₂₁H₂₈N₆O₂
Color Off-white to yellow
SMILES

OCC[C@H]1N(CCCC1)C2=NC3=C(C=NN3C(NCC4=C[N+]([O-])=CC=C4)=C2)CC
別名

SCH 727965
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (56)

All Gel ElectrophoresisBio/Physico-chemical AssayRT-PCRIPCell Proliferation/Viability AssayWB

Sort by:

Journal Impact Factor

Nat Commun

High-resolution cryo-EM of the human CDK-activating kinase for structure-based drug design. [Abstract]

2024 Mar 13;15(1):2265. PMID: 38480681
Nat Commun

Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation. [Abstract]

2021 Nov 16;12(1):6607. PMID: 34785661
Mol Cell

Discovery of Widespread Host Protein Interactions with the Pre-replicated Genome of CHIKV Using VIR-CLASP. [Abstract]

2020 May 21;78(4):624-640.e7. PMID: 32380061

Dinaciclib purchased from MedChemExpress. Usage Cited in: Mol Cell. 2020 May 21;78(4):624-640.e7. [Abstract]

SDS-PAGE and silver stain (top), agarose gel (bottom) that of CLASP with pretreatment of cells with Dinaciclib for 4 hr.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Acta Pharm Sin B

Inhibition of the CDK9-cyclin T1 protein-protein interaction as a new approach against triple-negative breast cancer. [Abstract]

2022 Mar;12(3):1390-1405. PMID: 35530158

Dinaciclib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Mar;12(3):1390-1405. [Abstract]

Inhibition of the CDK9-cyclin T1 PPI by 1-20(Dinaciclib, 30 min) as measured using the AlphaScreen assay.

Dinaciclib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Mar;12(3):1390-1405. [Abstract]

Mcl-1 mRNA levels by compounds (3 mmol/L) in MDA-MB-231 cells as measured by qPCR assay after 24-48 h.

Dinaciclib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Mar;12(3):1390-1405. [Abstract]

20(Dinaciclib) inhibits CDK9ecyclin T1 activity in a dose-dependent manner.

Dinaciclib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Mar;12(3):1390-1405. [Abstract]

Inhibition effect of 1 or 20(Dinaciclib) on the binding ability of CDK9 to c-Myc and Mcl-1 promoter in MDA-MB-231 cells by ChIP-qPCR. Indicated concentrations of 1 or 20 treated with cells for 4 h. Then cells were collected to perform ChIP-qPCR.
J Exp Clin Cancer Res

MYC up-regulation confers vulnerability to dual inhibition of CDK12 and CDK13 in high-risk Group 3 medulloblastoma. [Abstract]

2023 Aug 21;42(1):214. PMID: 37599362
Sci Adv

Antagonistic effect of cyclin-dependent kinases and a calcium-dependent phosphatase on polyglutamine-expanded androgen receptor toxic gain of function. [Abstract]

2023 Jan 6;9(1):eade1694. PMID: 36608116
Sci Adv

Targeting OXPHOS de novo purine synthesis as the nexus of FLT3 inhibitor-mediated synergistic antileukemic actions. [Abstract]

2022 Sep 16;8(37):eabp9005. PMID: 36112677
J Control Release

Nanodrug modified with engineered cell membrane targets CDKs to activate aPD-L1 immunotherapy against liver metastasis of immune-desert colon cancer. [Abstract]

2024 May:369:309-324. PMID: 38554771
Cell Death Dis

CDK9 inhibition as an effective therapy for small cell lung cancer. [Abstract]

2024 May 20;15(5):345. PMID: 38769311
Cell Death Dis

The role of E26 transformation-specific variant transcription factor 5 in colorectal cancer cell proliferation and cell cycle progression. [Abstract]

2021 Apr 30;12(5):427. PMID: 33931578
Cancer Lett

FOXK2 amplification promotes breast cancer development and chemoresistance. [Abstract]

2024 Aug 10:597:217074. PMID: 38901667
J Neuroinflammation

STAT3 S727 phosphorylation drives pathogenic Th17 differentiation and neuroinflammation in autoimmune disease. [Abstract]

2025 Oct 28;22(1):246. PMID: 41152886
Clin Cancer Res

CDK9 inhibition by dinaciclib is a therapeutic vulnerability in epithelioid hemangioendothelioma. [Abstract]

2024 Sep 13;30(18):4179-4189. PMID: 39052240
Cell Chem Biol

Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. [Abstract]

2018 Feb 15;25(2):135-142.e5. PMID: 29276047
Int J Biol Macromol

Unveiling the mechanistic link between peroxiredoxin inhibition and ferroptosis-like cell death induced by Dinaciclib in Entamoeba histolytica. [Abstract]

2026 Mar:350:150992. PMID: 41713546
Cell Genom

2026 May 17.
Cell Rep

Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. [Abstract]

2021 Jul 20;36(3):109394. PMID: 34289372
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
J Med Chem

Fluorocyclopropyl-Containing Tacrine Derivatives as Potent and Selective Dual CDK2/CDK9 Inhibitors for the Treatment of Colorectal Cancer. [Abstract]

2025 Nov 27;68(22):24326-24357. PMID: 41239996
J Med Chem

3,5,7-Substituted Pyrazolo[4,3- d]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders. [Abstract]

2022 Jul 14;65(13):8881-8896. PMID: 35749742
J Med Chem

3 H-Pyrazolo[4,3- f]quinoline-Based Kinase Inhibitors Inhibit the Proliferation of Acute Myeloid Leukemia Cells In Vivo. [Abstract]

2021 Aug 12;64(15):10981-10996. PMID: 34288692
J Med Chem

3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. [Abstract]

2019 May 9;62(9):4606-4623. PMID: 30943029
Eur J Med Chem

Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure. [Abstract]

2021 Apr 15:216:113309. PMID: 33711765
Eur J Med Chem

Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor. [Abstract]

2018 Oct 5:158:896-916. PMID: 30253346
Biochem Pharmacol

Butein suppresses pancreatic cancer progression by downregulating CDK2 and disrupting CDK2/CyclinA2 interaction. [Abstract]

2026 Sep;251(Pt 1):118099. PMID: 42178048
Mol Ther Nucleic Acids

2025 Dec 15.
Biochem Pharmacol

Insight into the structure, function and the tumor suppression effect of gasdermin E. [Abstract]

2024 Aug:226:116348. PMID: 38852642
Cell Rep Methods

A hybrid deep forest-based method for predicting synergistic drug combinations. [Abstract]

2023 Feb 21;3(2):100411. PMID: 36936075
Mol Cancer Ther

Rational Combination Therapy for Melanoma with Dinaciclib by Targeting BAK-Dependent Cell Death. [Abstract]

2020 Feb;19(2):627-636. PMID: 31744894

Dinaciclib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2020 Feb;19(2):627-636. [Abstract]

Human melanoma cells were treated with Dinaciclib at the indicated doses for 72 hours. After 72-hours incubation, cell viability is assessed by the CellTiter-Glo 2.0 assay. Relative growth to vehicle control is shown.

Dinaciclib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2020 Feb;19(2):627-636. [Abstract]

A2058 melanoma cells are treated with 50 nM Dinaciclib for 3 or 6 hours. Whole cell lysates are subjected to Western blotting (left).
Int J Mol Sci

Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]

2022 Feb 24;23(5):2493. PMID: 35269635
Sci Rep

Selective but not pan-CDK inhibition abrogates 5-FU-driven tissue factor upregulation in colon cancer. [Abstract]

2024 May 8;14(1):10582. PMID: 38719932
Sci Rep

Pre-therapeutic efficacy of the CDK inhibitor dinaciclib in medulloblastoma cells. [Abstract]

2021 Mar 8;11(1):5374. PMID: 33686114
Cancers (Basel)

Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]

2022 Mar 19;14(6):1575. PMID: 35326726
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
Mol Oncol

The CDK12-BRCA1 signaling axis mediates dinaciclib-associated radiosensitivity through p53-mediated cellular senescence. [Abstract]

2025 Apr;19(4):1265-1280. PMID: 39626031
Mol Oncol

Dinaciclib synergizes with BH3 mimetics targeting BCL-2 and BCL-XL in multiple myeloma cell lines partially-dependent on MCL-1 and in plasma cells from patients. [Abstract]

2023 Dec;17(12):2507-2525. PMID: 37704591
J Virol

FMDV 3A cooperates with PDCD10 to promote FMDV replication by inhibiting VISA-mediated innate immunity. [Abstract]

2025 Nov 26:e0065725. PMID: 41296880
J Biol Chem

The reversible inhibitor SR-4835 binds Cdk12/Cyclin K in a non-canonical G-loop conformation. [Abstract]

2024 Jan;300(1):105501. PMID: 38016516
Cell Cycle

Synthetic lethality of cyclin-dependent kinase inhibitor Dinaciclib with VHL-deficiency allows for selective targeting of clear cell renal cell carcinoma. [Abstract]

2022 May;21(10):1103-1119. PMID: 35240916
Invest New Drugs

Discovery of a novel and highly selective CDK9 kinase inhibitor (JSH-009) with potent antitumor efficacy in preclinical acute myeloid leukemia models. [Abstract]

2020 Oct;38(5):1272-1281. PMID: 31872348
Glycobiology

Compromised CDK12 activity causes dependency on the high activity of O-GlcNAc transferase. [Abstract]

2024 Dec 10;34(12):cwae081. PMID: 39361894
bioRxiv

2026 Mar 26.
Charles University

2026.
Res Sq

2025 Dec 18.
Technical University of Dresden

2025.
University of California, Irvine

2024.
Research Square Preprint

2024 Nov 06.
University of Cologne

2024.
bioRxiv

FOXK2 amplification and overexpression promotes breast cancer development and chemoresistance. [Abstract]

2023 May 30:2023.05.28.542643. PMID: 37398114
bioRxiv

Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells Selectively. [Abstract]

2023 Jan 2:2023.01.01.522436. PMID: 36711980
University of London

2021 Oct 13.
Patent

US20210085619A1.
bioRxiv

2020 Apr.
Harvard University

2019 May.
Patent

US20180263995A1.

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (126.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5221 mL

12.6107 mL

25.2213 mL

5 mM

0.5044 mL

2.5221 mL

5.0443 mL

10 mM

0.2522 mL

1.2611 mL

2.5221 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.31 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 20% HP-β-CD in Saline

Solubility: 10 mg/mL (25.22 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Kinase Assay^[1]

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 (SCH 727965). 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. Dose-response curves are generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC₅₀ values are derived by nonlinear regression analysis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

A2780 cells are plated onto tissue culture dishes and propagated with the appropriate growth media. Growing cultures are exposed to increasing concentrations of Dinaciclib (0.75, 1.5, 3.15, 6.25, 12.5, 25, and 500 nM) or a vehicle control, typically for 7 days. After removing the medium, cells are fixed with 50% methanol/50% acetone for 5 minutes and stained with 0.2% crystal violet in 2% ethanol for 5 minutes. Following staining, cells are washed with 5 to 10 mL of water. Stained cells are solubilized in 1% deoxycholic acid, and the absorbance of the resulting solution is measured at 600 nm using a SOFTmax PRO 4.3 plate reader. Absorbance of Dinaciclib-treated samples is plotted as a percent of that of a vehicle-treated control, and data are reported as an IC₅₀ value relative to these controls. For suspension cell lines, assessments of cell viability are obtained using the alamarBlue Cell Viability Assay kit^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
For tumor implantation, specific cell lines are grown in vitro, washed once with PBS, and resuspended in 50% Matrigel in PBS to a final concentration of 4×10⁷ to 5×10⁷ cells per milliliter. Nude mice are injected with 0.1 mL of this suspension s.c. in the flank region. Tumor length (L), width (W), and height (H) are measured by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L×W×H)/2. When the tumor volume reaches 100 mm³, the animals are randomized to treatment groups (10 mice/group) and treated i.p. with either Dinaciclib (8, 16, 32, and 48 mg/kg daily, i.p.) or individual chemotherapeutic agents according to the dosing schedule indicated in table and figure legends. Tumor volumes and body weights are measured during and after the treatment periods.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[1]. Parry D, et al. Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53. [Content Brief]

[2]. Feldmann G, et al. Cyclin-dependent kinase inhibitor Dinaciclib (SCH727965) inhibits pancreatic cancer growth and progression in murine xenograft models. Cancer Biol Ther. 2011 Oct 1;12(7):598-609. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5221 mL	12.6107 mL	25.2213 mL	63.0533 mL
	5 mM	0.5044 mL	2.5221 mL	5.0443 mL	12.6107 mL
	10 mM	0.2522 mL	1.2611 mL	2.5221 mL	6.3053 mL
	15 mM	0.1681 mL	0.8407 mL	1.6814 mL	4.2036 mL
	20 mM	0.1261 mL	0.6305 mL	1.2611 mL	3.1527 mL
	25 mM	0.1009 mL	0.5044 mL	1.0089 mL	2.5221 mL
	30 mM	0.0841 mL	0.4204 mL	0.8407 mL	2.1018 mL
	40 mM	0.0631 mL	0.3153 mL	0.6305 mL	1.5763 mL
	50 mM	0.0504 mL	0.2522 mL	0.5044 mL	1.2611 mL
	60 mM	0.0420 mL	0.2102 mL	0.4204 mL	1.0509 mL
	80 mM	0.0315 mL	0.1576 mL	0.3153 mL	0.7882 mL
	100 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6305 mL

Keywords

Dinaciclib

56 Cited Publications

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Dinaciclib

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MedChemExpress（MCE）の使用を引用している文献 Dinaciclib

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Publications (56)

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Complete Stock Solution Preparation Table

Dinaciclib 関連分類

HY-10492 関連分類