申请人:ENZO BIOCHEM, INC.
公开号:EP0154788A2
公开(公告)日:1985-09-18
A detectable molecule of the formula
where A3 is A2 or a polymer, where A3 has at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis OH, halides, aryl, imidazoyi, carbonyl, carboxy, thiol or a residue comprising an activated carbon; -X- is selected from the group consisting of
a C1-C10 branched or unbranched alkyl or aralkyl, which may be substituted by -OH; -Y- is a direct bond to -E-, or -Y- is -E-R2- where R2 is a C1-C10 branched or unbranched alkyl; Za is chlorine, bromine or iodine; E is 0, NH or an acyclic divalent sulfur atom; Detb is a chemical moiety capable of being detected, preferably comprising biotin or a metal chelator of the formula:
or the 4-hydroxy or acyloxy derivative thereof, where R3 is C1-C4 alkyl or CH2COOM, M is the same or different and selected from the group consisting of hydrogen, a metal or non-metal cation or is C,-C,o alkyl, aryl or aralkyl; and m is an integer from 1 to the total number of modified reactive groups on A3. The detectable molecules are useful in in vitro or in vivo assays or therapy.
式中的可检测分子
其中 A3 是 A2 或聚合物,A3 具有至少一个可修饰的反应基团,该反应基团选自由氨基、羟基、顺 OH、卤化物、芳基、咪唑基、羰基、羧基、硫醇或包含活性碳的残基组成的组;-X- 选自由以下组
C1-C10支链或未支链烷基或芳烷基,可被-OH 取代;-Y- 是与-E- 的直接键,或-Y- 是-E-R2-,其中 R2 是 C1-C10 支链或未支链烷基;Za 是氯、溴或碘;E 是 0、NH 或无环二价硫原子;Detb 是可检测的化学分子,最好包括生物素或式中的金属螯合剂:
或其 4-羟基或酰氧基衍生物,其中 R3 为 C1-C4 烷基或 CH2COOM,M 相同或不同,且选自由氢、金属或非金属阳离子或 C,-C,o烷基、芳基或芳烷基组成的组;m 为 1 至 A3 上修饰反应基团总数的整数。可检测分子可用于体外或体内检测或治疗。