Dinaciclib
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.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 779353-01-4
- Formula: C21H28N6O2
- Molecular Weight:396.49
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Dinaciclib
More- Nat Commun. 2024 Mar 13;15(1):2265. [Abstract]
- Nat Commun. 2021 Nov 16;12(1):6607. [Abstract]
- Mol Cell. 2020 May 21;78(4):624-640.e7. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Pharm Sin B. 2022 Mar;12(3):1390-1405. [Abstract]
- J Exp Clin Cancer Res. 2023 Aug 21;42(1):214. [Abstract]
- Sci Adv. 2023 Jan 6;9(1):eade1694. [Abstract]
- Sci Adv. 2022 Sep 16;8(37):eabp9005. [Abstract]
- J Control Release. 2024 May:369:309-324. [Abstract]
- Cell Death Dis. 2024 May 20;15(5):345. [Abstract]
- Cell Death Dis. 2021 Apr 30;12(5):427. [Abstract]
- Cancer Lett. 2024 Aug 10:597:217074. [Abstract]
- J Neuroinflammation. 2025 Oct 28;22(1):246. [Abstract]
- Clin Cancer Res. 2024 Sep 13;30(18):4179-4189. [Abstract]
- Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5. [Abstract]
- Int J Biol Macromol. 2026 Mar:350:150992. [Abstract]
- Cell Genom. 2026 May 17.
- Cell Rep. 2021 Jul 20;36(3):109394. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Med Chem. 2025 Nov 27;68(22):24326-24357. [Abstract]
- J Med Chem. 2022 Jul 14;65(13):8881-8896. [Abstract]
- J Med Chem. 2021 Aug 12;64(15):10981-10996. [Abstract]
- J Med Chem. 2019 May 9;62(9):4606-4623. [Abstract]
- Eur J Med Chem. 2021 Apr 15:216:113309. [Abstract]
- Eur J Med Chem. 2018 Oct 5:158:896-916. [Abstract]
- Biochem Pharmacol. 2026 Sep;251(Pt 1):118099. [Abstract]
- Mol Ther Nucleic Acids. 2025 Dec 15.
- Biochem Pharmacol. 2024 Jun 7:116348. [Abstract]
- Cell Rep Methods. 2023 Feb 21;3(2):100411. [Abstract]
- Mol Cancer Ther. 2020 Feb;19(2):627-636. [Abstract]
- Int J Mol Sci. 2022 Feb 24;23(5):2493. [Abstract]
- Sci Rep. 2024 May 8;14(1):10582. [Abstract]
- Sci Rep. 2021 Mar 8;11(1):5374. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Mol Oncol. 2025 Apr;19(4):1265-1280. [Abstract]
- Mol Oncol. 2023 Dec;17(12):2507-2525. [Abstract]
- J Virol. 2025 Nov 26:e0065725. [Abstract]
- J Biol Chem. 2024 Jan;300(1):105501. [Abstract]
- Cell Cycle. 2022 May;21(10):1103-1119. [Abstract]
- Invest New Drugs. 2020 Oct;38(5):1272-1281. [Abstract]
- Glycobiology. 2024 Dec 10;34(12):cwae081. [Abstract]
- 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. 2023 May 30:2023.05.28.542643. [Abstract]
- bioRxiv. 2023 Jan 2:2023.01.01.522436. [Abstract]
- University of London. 2021 Oct 13.
- Patent. US20210085619A1.
- bioRxiv. 2020 Apr.
- Harvard University. 2019 May.
- Patent. US20180263995A1.
-
Bio/Physico-chemical Assay
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RT-PCR
-
Bio/Physico-chemical Assay
-
IP
-
Gel Electrophoresis
Biological Activity
|
CDK2 1 nM (IC50) |
CDK5 1 nM (IC50) |
CDK1 3 nM (IC50) |
CDK9 4 nM (IC50) |
|
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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 779353-01-4
-
Appearance Solid
-
Molecular Weight 396.49
-
Formula 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
-
Synonyms
SCH 727965
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (56)
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Journal Impact Factor
-
Most Recent
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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.
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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.
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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
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
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
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 -
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Cell Rep
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 -
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Biochem Pharmacol
2024 Jun 7:116348. PMID: 38852642 -
Cell Rep Methods
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).
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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
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
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 -
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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 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: 20% HP-β-CD in Saline
Solubility: 10 mg/mL (25.22 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
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.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |