product name K03861
Description: K03861 is an aminopyrimidine-phenyl urea, type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely. The cocrystal structure of CDK2 with the inhibitor K03861 revealed a canonical type II binding mode. K03861 competes with the binding of cyclins. The residues important for the type II inhibitors may be distant to the ATP binding pockets. The crystal structure of this complex may provide a foundation for the cyclin-competitive CDK2 inhibitors
References: ACS Chem Biol. 2015 Sep 18;10(9):2116-25.
501.50
Formula
C24H26F3N7O2
CAS No.
853299-07-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (199.4 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (29.9 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19405783
| In Vitro |
In vitro activity: K03861 is an aminopyrimidine-phenyl urea inhibitor of CDK2. The type II inhibitor CDK2 cocrystal structure of CDK2 with the inhibitor K03861 revealed a canonical type II binding mode. The type II inhibitors could compete with the binding of cyclins. The residues important for the type II inhibitors may be distant to the ATP binding pockets. The crystal structure of this complex may provide a foundation for the cyclin-competitive CDK2 inhibitors Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | ACS Chem Biol. 2015 Sep 18;10(9):2116-25. |
