LWY713 

LWY713 is a PROTAC-class FLT3 degrader (DC₅₀=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models^[1]. LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).

DC50: 0.64 nM (FLT3)^[1]

838.95

C₄₃H₅₄N₁₀O₈

O=C1C2=CC=CC(OCC(N3CCN(C4CCN(C5=CC=C(C=C5OC)NC6=C(C(N)=O)N=C(CC)C(NC7CCOCC7)=N6)CC4)CC3)=O)=C2CN1C8C(NC(CC8)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu W et al. Discovery of LWY713 as a potent and selective FLT3 PROTAC degrader with in vivo activity against acute myeloid leukemia. Eur J Med Chem. 2023 Nov 19;264:115974.  [Content Brief]