(R)-CR8

Pricing Availability Delivery Time Qty
Cat.No. 3605 - (R)-CR8 | C24H29N7O.3HCl | CAS No. 294646-77-8
Description: Dual cdk1/cdk5 inhibitor; also inhibits CK1
Chemical Name: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine trihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (6)
Literature

Biological Activity

Inhibitor of cyclin-dependent kinase (cdk) and casein kinase 1 (CK1) (IC50 values are 130, 130 and 600 nM for cdk1/cyclin B, cdk5/p35 (cdk5/p25) and CK1, respectively).

Compound Libraries

(R)-CR8 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 540.92
Formula C24H29N7O.3HCl
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 294646-77-8
PubChem ID 90488866
InChI Key ORYSYXHQFOWNDK-RGFWRHHQSA-N
Smiles CC(C)N2C1=NC(N[C@H](CC)CO)=NC(NCC3=CC=C(C4=NC=CC=C4)C=C3)=C1N=C2.Cl.Cl.Cl

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.09 100
water 54.09 100

Preparing Stock Solutions

The following data is based on the product molecular weight 540.92. Batch specific molecular weights may vary from batch to batch due to solvent 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 1.85 mL 9.24 mL 18.49 mL
5 mM 0.37 mL 1.85 mL 3.7 mL
10 mM 0.18 mL 0.92 mL 1.85 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 5229 PMID: 18698753


If you know of a relevant reference for (R)-CR8, please let us know.

View Related Products by Product Action

View all Cyclin-Dependent Protein Kinase Inhibitors

Keywords: cdk1 cdk5 inhibitors inhibits CK1 cyclin-dependent kinases casein kinase 1 Cyclin-dependent Kinase

6 Citations for (R)-CR8

Citations are publications that use Tocris products. Selected citations for (R)-CR8 include:

Wu et al (2012) Delayed expression of cell cycle proteins contributes to astroglial scar formation and chronic inflammation after rat spinal cord contusion. J Neuroinflammation 9 169 PMID: 22784881

Malonia et al (2015) F-box protein FBXO31 directs degradation of MDM2 to facilitate p53-mediated growth arrest following genotoxic stress. Microvasc Res 112 8632 PMID: 26124108

Wu et al (2014) Spinal cord injury causes brain inflammation associated with cognitive and affective changes: role of cell cycle pathways. J Neurosci 34 10989 PMID: 25122899

Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046 PMID: 24740004

Wu et al (2013) Cell cycle activation contributes to increased neuronal activity in the posterior thalamic nucleus and associated chronic hyperesthesia after rat spinal cord contusion. Neurotherapeutics 10 520 PMID: 23775067

Wu et al (2013) TrkB.T1 contributes to neuropathic pain after spinal cord injury through regulation of cell cycle pathways. J Neurosci 33 12447 PMID: 23884949


Do you know of a great paper that uses (R)-CR8 from Tocris? If so please let us know.

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Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for (R)-CR8

Protocols

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