| CAS NO: | 853299-07-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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) | |
| Other info | Chemical Name: 1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea InChi Key: PWDLXPJQFNVTNL-UHFFFAOYSA-N InChi Code: InChI=1S/C24H26F3N7O2/c1-33-10-12-34(13-11-33)15-16-2-3-18(14-20(16)24(25,26)27)31-23(35)30-17-4-6-19(7-5-17)36-21-8-9-29-22(28)32-21/h2-9,14H,10-13,15H2,1H3,(H2,28,29,32)(H2,30,31,35) SMILES Code: O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)NC3=CC=C(OC4=NC(N)=NC=C4)C=C3 |
| Synonyms | K03861; AUZ454; K-03861; AUZ 454; K 03861; AUZ-454 |
| 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: K03861 is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | ACS Chem Biol. 2015 Sep 18;10(9):2116-25. |
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