Pomalidomide-amido-C1-Br

• CAT Number: I017381
• CAS Number: 2351106-38-0
• Molecular Formula: C15H12BrN3O5
• Molecular Weight: 394.18
• Purity: ≥95%
• Synonyms: 2-bromo-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]acetamide
• InChI: InChI=1S/C15H12BrN3O5/c16-6-11(21)17-8-3-1-2-7-12(8)15(24)19(14(7)23)9-4-5-10(20)18-13(9)22/h1-3,9H,4-6H2,(H,17,21)(H,18,20,22)
• InChIKey: VFHGCZZAGNKHIX-UHFFFAOYSA-N
• SMILES: C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)NC(=O)CBr

Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity[1].
Pomalidomide-amido-C1-Br (Compound 6) can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (Compound 2). PROTAC B-Raf degrader 1 can effectively kill cancer cells via inducing cells apoptosis. As a B-Raf degrader, PROTAC B-Raf degrader 1 can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf[1].

Reference

[1]. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Jun;87:191-199.
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