(R)-DRF053 dihydrochloride

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Cat.No. 3610 - (R)-DRF053 dihydrochloride | C23H27N7O.2HCl | CAS No. 1241675-76-2
Description: Dual CK1/cdk inhibitor
Chemical Name: 2-[[9-(1-Methylethyl)-6-[[3-(2-pyridinyl)phenyl]amino]-9H-purin-2-yl]amino]-1-butanol dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

Potent, ATP-competitive inhibitor of cyclin-dependent kinase (cdk) and casein kinase 1 (CK1) (IC50 values are 220, 80 and 14 nM for cdk1/cyclin B, cdk5/p25 and CK1 respectively). Selective over GSK-3 αβ (IC50= 4.1 μM). Also shown to inhibit amyloid-β production in N2A-APP695 cells.

Compound Libraries

(R)-DRF053 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 490.43
Formula C23H27N7O.2HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1241675-76-2
PubChem ID 71433624
InChI Key BQPRBNGSDBTKAK-ZEECNFPPSA-N
Smiles CC(C)N2C1=NC(N[C@H](CC)CO)=NC(NC3=CC(C4=NC=CC=C4)=CC=C3)=C1N=C2.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 49.04 100
water 49.04 100

Preparing Stock Solutions

The following data is based on the product molecular weight 490.43. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.04 mL 10.2 mL 20.39 mL
5 mM 0.41 mL 2.04 mL 4.08 mL
10 mM 0.2 mL 1.02 mL 2.04 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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

Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 522


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View all Casein Kinase 1 Inhibitors

Keywords: (R)-DRF053 dihydrochloride, (R)-DRF053 dihydrochloride supplier, casein, cyclin-dependent, kinases, cyclin, cdk5, cdk1, CK1, p25, dual, specificity, inhibits, inhibitors, Casein, Kinase, 1, Cyclin-dependent, 3610, Tocris Bioscience

1 Citation for (R)-DRF053 dihydrochloride

Citations are publications that use Tocris products. Selected citations for (R)-DRF053 dihydrochloride include:

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


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Literature in this Area

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