Name | K03861 |
Synonyms | KO3861 K03861 K0-3861 AUZ 454 CS-2904 K0 3861 AUZ 454 (K03861) 1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea Urea, N-[4-[(2-amino-4-pyrimidinyl)oxy]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]- |
CAS | 853299-07-7 |
Molecular Formula | C24H26F3N7O2 |
Molar Mass | 501.5 |
Solubility | DMSO: ≥ 33 mg/mL |
Storage Condition | -20℃ |
In vitro study | K03861 inhibits CDK2 activity by competitively binding activated cyclins. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.994 ml | 9.97 ml | 19.94 ml |
5 mM | 0.399 ml | 1.994 ml | 3.988 ml |
10 mM | 0.199 ml | 0.997 ml | 1.994 ml |
5 mM | 0.04 ml | 0.199 ml | 0.399 ml |
biological activity | K03861 (AUZ 454,AUZ454) is a type II CDK2 inhibitor that acts on CDK2(WT), the Kd of CDK2(C118L),CDK2(A144C), and CDK2(C118L/A144C) are 50 nM,18.6 nM,15.4 nM, and 9.7 nM, respectively. |
Target | Value |
CDK2(C118L/A144C) (Cell-free assay) | 9.7 nM(Kd) |
CDK2(A144C) (Cell-free assay) | 15.4 nM(Kd) |
CDK2(C118L) (Cell-free assay) | 18.6 nM(Kd) |
CDK2(WT) (Cell-free assay) | 50 nM(Kd) |