FIELD: chemistry.
SUBSTANCE: invention relates to amatoxins of general formula (An), where n is 2, 3, 4, 5, 6, 7, 8 or 9. Invention also relates to an antibody-drug conjugate (ADC) consisting of an antibody conjugated to amatoxin through a linker, wherein the ADC has structural formula (Ia), where Q is S; L is -(CH2)n, wherein n is integer from 1 to 6; Z is a maleimide group; and Ab is an antibody which specifically binds to Her2 or PSMA. Invention also relates to an antibody-drug conjugate (ADC), wherein the antibody specifically binds to human PSMA and contains heavy and light chain amino acid sequences and which is conjugated with HDP30.2867 compound. Invention also relates to the use of ADC for treating cancer. (HDP30.2867).
EFFECT: providing amatoxins which can be used in antibody-drug conjugates (ADC) for delivering amatoxin to a target cell, which have high plasma stability and tolerance in vivo.
16 cl, 15 tbl, 48 dwg, 22 ex
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Authors
Dates
2024-09-03—Published
2020-04-24—Filed