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K03861(AUZ 454)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
K03861(AUZ 454)图片
CAS NO:853299-07-7
规格:≥98%
包装与价格:
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

产品介绍
理化性质和储存条件
Molecular Weight (MW)501.50
FormulaC24H26F3N7O2
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

实验参考方法
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.