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(R)-DRF053 dihydrochloride

Cat. No. 3610 1 Citation Submit a Review Datasheet / COA / SDS
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Description: Potent CK1 inhibitor; also inhibits cyclin-dependent kinases
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 (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for (R)-DRF053 dihydrochloride

(R)-DRF053 dihydrochloride is a potent casein kinase 1 (CK1) inhibitor (IC50 = 14 nM). Also an ATP-competitive cyclin-dependent kinase (cdk) inhibitor (IC50 values are 0.093 - 0.29, 0.21 and 0.82 μM for cdk2, cdk5 and cdk7, respectively). Shown to inhibit amyloid-β production in N2A-APP695 cells.

Compound Libraries for (R)-DRF053 dihydrochloride

(R)-DRF053 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for (R)-DRF053 dihydrochloride

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.

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

Solubility Data for (R)-DRF053 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 49.04 100
DMSO 49.04 100

Preparing Stock Solutions for (R)-DRF053 dihydrochloride

The following data is based on the product molecular weight 490.43. 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 2.04 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 for (R)-DRF053 dihydrochloride

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for (R)-DRF053 dihydrochloride

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

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987

If you know of a relevant reference for (R)-DRF053 dihydrochloride, please let us know.

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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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Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:

  • Cell Cycle and Mitosis
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