cBu-Cit-GAL-02-221  (Synonyms: cBu-Cit-PROTAC BRD4 Degrader-5)

cBu-Cit-GAL-02-221 is a PROTAC that degrades BRD4 by association with cBu-Cit. cBu-Cit-GAL-02-221 can effectively inhibit BRD4 in HER2 positive and negative breast cancer cell lines. cBu-Cit-GAL-02-221 has a single bond and can be conjugated to an ADC antibody to form a PAC^[1].

1628.31

C₇₉H₉₉ClN₁₆O₁₆S₂

2417369-73-2

CC1=C(C)SC(N2C3=NN=C2C)=C1C(C4=CC=C(C=C4)Cl)=N[C@H]3CC(NCCOCCOCCOCC(N[C@H](C(N5C[C@@H](C[C@H]5C(NCC(C=C6)=CC=C6C7=C(C)N=CS7)=O)OCNC(OCC8=CC=C(NC([C@@H](NC(C9(C(NCCCCCN%10C(C=CC%10=O)=O)=O)CCC9)=O)CCCNC(N)=O)=O)C=C8)=O)=O)C(C)(C)C)=O)=O

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• [1]. Peter S Dragovich, et al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties. J Med Chem. 2021 Mar 11;64(5):2534-2575.  [Content Brief]