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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 , 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).

Product Specifications

UNSPSC

12352005

Target

Apoptosis; FLT3; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/lwy713.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C43H54N10O8

Molecular Weight

838.95

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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