然而Ki的测定需要先测定该酶特定条件下的Km,然后在某种抑制剂浓度、不同底物浓度下进行双倒数作图,得到表观Km(即Kmapp)后再根据Kmapp=Km(1+[I]/Ki)得到Ki,不过在竞争性抑制剂情况下,固定酶的浓度,IC50与Ki满足Cheng-Prusoff方程[3](注:此方程不适用于tight-binding型抑制剂,对于这种抑制剂其IC50与酶浓度相关...
误差可以很大。IC50是半数抑制浓度，如名所言，就是酶活性被抑制一半的时候所需化合物的浓度，用于评价...
Ki和IC50的关系
cyp酶抑制试验中低溶解度抑制剂表观ic50偏高问题的解决方案研究 热度: BiochemicalPharmacology,Vol.22,pp.3099-3108.PergamonPress,1973.PrintedinGreatBritain. RELATIONSHIPBETWEENTHEINHIBITIONCONSTANT (&)ANDTHECONCENTRATION OFINHIBITORWHICH CAUSES50PERCENTINHIBITION(Iso)OFANENZYMATIC ...
Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor with IC50 value of 2 nM; 6 fold and > 100 fold selectivity over VEGFR2(IC50=12 nM) and c-Kit/PDGFR_beta_(IC50=451/217 nM), respectively. 纯度 >98% 储存/保存方法 Store at -20℃ for one year(Powder);Store at...
IC50 & Target:2 nM (CSF1R), 12 nM (VEGFR2), 451 nM (c-Kit) and 217 nM (PDGFRβ)[1] 热销产品:Mosunetuzumab|DSPE-PEG 2000|Ribociclib|Canagliflozin|Orlistat|Mitapivat|Abiraterone|Napabucasin|SBI-115|Sodium 2-oxobutanoate Trending products:Recombinant Proteins|Bioactive Screening Libraries|Nat...
Measuring Bioactivity: KI, IC50 and EC50Which quantity permits a characterisation of the performance of a bioactive molecule? How can a test be created so as to detect the effect of a molecule on a given target? Are there any general rules...
IC50 和目标:Ki:0.37 nM (PSMA)[1]。体外Vipivotide tetraxetan (PSMA-617) 表现出至少 72 小时的高辐射稳定性。高抑制效力(平衡解离常数 Ki=2.34±2.94 nM 对 LNCaP;Ki=0.37±0.21 nM 酶促测定)和高效内化到 LNCaP 细胞中展示了[1]。体内:68Ga 标记的 Vipivotide tetraxetan (PSMA-617) 1 小时后 (...
泽布替尼作为新一代BTKi,具有优良的药代动力学特性,对BTK靶点能形成持久且精准的抑制作用,保证了高于IC50的持续暴露覆盖率。在FL中,T细胞标志物IL-2可诱导酪氨酸激酶(ITK)的表达,与良好的预后和更长的生存期有关。由于脱靶效应,...
An Intuitive Look at the Relationship of K[sub i] and IC[sub 50]: A More General Use for the Dixon Plot. Burlingham, B.T., and Widlanski, T.S. (2003). An Intuitive Look at the Relationship of Ki and IC50: A More General Use for the Dixon Plot. J... Burlingham,Benjamin,T.,...