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Description: Potent and selective inhibitor of CDK2, CDK5, CDK1 and CDK9
Alternative Names: SCH 727965
Chemical Name: (2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol
Purity: ≥98% (HPLC)

Biological Activity for Dinaciclib

Dinaciclib is a potent and selective inhibitor of CDK2, CDK5, CDK1 and CDK9 activity in vitro (IC50 values are 1, 1, 3 and 4 nM, respectively). The compound inhibits DNA replication by blocking thymidine DNA incorporation in A2780 cells (IC50 = 4 nM). Dinaciclib induces regression of established solid tumors in mouse models and shows antiviral activity against SARS-CoV-2 in vitro (Vero E6, IC50 = 0.127 μM; A549-ACE2, IC50 = 0.032 μM).

Compound Libraries for Dinaciclib

Dinaciclib is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for Dinaciclib

M. Wt 396.5
Formula C21H28N6O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 779353-01-4
PubChem ID 46926350
Smiles [O-][N+]1=CC=CC(CNC(N2N=C3)=CC(N4[C@@H](CCCC4)CCO)=NC2=C3CC)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Dinaciclib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 39.65 100
ethanol 7.93 20

Preparing Stock Solutions for Dinaciclib

The following data is based on the product molecular weight 396.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.52 mL 12.61 mL 25.22 mL
5 mM 0.5 mL 2.52 mL 5.04 mL
10 mM 0.25 mL 1.26 mL 2.52 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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References for Dinaciclib

References are publications that support the biological activity of the product.

Parry et al (2010) Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol.Cancer Ther. 9 2344 PMID: 20663931

Bouhaddou et al (2020) The global phosphorylation landscape of SARS-CoV-2 infection. Cell 182 685 PMID: 32645325

If you know of a relevant reference for Dinaciclib, please let us know.

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Citations for Dinaciclib

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