(R)-CR8
Tocris Bioscience, part of Bio-Techne | Catalog # 3605
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
Product Description
(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.Product Specifications
Molecular Weight
540.92
Formula
C24H29N7O.3HCl
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
(2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for (R)-CR8
For research use only
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