(R)-CR8

Name: ( R )-CR8
Brand: Tocris Bioscience
SKU: 3605

Tocris Bioscience, part of Bio-Techne | Catalog # 3605

Citations (12)

COA / SDS

Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue

Key Product Details

Description:	Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue
Chemical Name:	(2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	540.92

View Full Technical Details for (R)-CR8

Technical Data
Citations

Biological Activity for (R)-CR8

(R)-CR8 is a cyclin dependent kinase (cdk) inhibitor (reported IC₅₀ values are 0.036 - 0.07, 0.09 - 0.8, 0.13 - 0.68, 0.18 - 1 and >1 μM for cdk2, cdk1, cdk5, cdk9 and cdk7, respectively). Also inhibits casein kinase 1 (CK1; IC₅₀ = 0.6 μM). Acts as molecular glue; forms a complex between CDK12-cyclin K and the CUL4 adapter protein DDB1 resulting in ubiquination and degradation of cyclin K.

Compound Libraries for (R)-CR8

(R)-CR8 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)-CR8

M. Wt	540.92
Formula	C₂₄H₂₉N₇O.3HCl
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	1786438-30-9
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.

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

Solubility for (R)-CR8

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

Preparing Stock Solutions for (R)-CR8

The following data is based on the product molecular weight 540.92.

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.

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	3.70 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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References for (R)-CR8

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

Jorda How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 2018 PMID: 30234987
Słabicki The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K. Nature 2020 PMID: 32494016
Oumata Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 2008 PMID: 18698753