L1BC8

L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments. (Pink: BRD4 ligand ; Blue: VHL ligand (HY-125845) ; Black: linker (HY-171663) ).

Product Specifications

CAS Number

2417370-68-2

UNSPSC

12352005

Target

Drug-Linker Conjugates for ADC; Epigenetic Reader Domain; PROTACs

Related Pathways

Antibody-drug Conjugate/ADC Related; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Purity

99.20

Smiles

O=C(OCC1=CC=C(NC([C@@H](NC(C2(CCC2)C(NCCCCCN3C(C=CC3=O)=O)=O)=O)CCCNC(N)=O)=O)C=C1)NC4=CC(CCOCC(N[C@@H](C(C)(C)C)C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)=O)=CC(OCCNC(C8=C(CS(=O)(C)=O)C=C(C(N(C9=NC=C(F)C=C9F)C%10)=C8)C%11=CN(C)C(C%12=C%11C%10=CN%12)=O)=O)=C4

Molecular Formula

C86H98F2N16O18S2

Molecular Weight

1745.92

References & Citations

[1]Dragovich PS, et al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64 (5) :2576-2607.