PROTAC FLT3/JAK2/BRD4 Degrader-1

PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML) . (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939) ) [1].

Product Specifications

CAS Number

[3067695-20-6]

UNSPSC

12352100

Target

Epigenetic Reader Domain; FLT3; JAK; PROTACs

Related Pathways

Epigenetics; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Smiles

CC1=C(N=C(N=C1)NC2=CC=C(C(F)=C2)N3CCN(CC3)C(CCCCCNC4=CC=C5C(C(N(C5=O)C6CCC(NC6=O)=O)=O)=C4)=O)NC7=CC=CC(NS(C(C)(C)C)(=O)=O)=C7

Molecular Formula

C44H51FN10O7S

Molecular Weight

883.00

References & Citations

[1]Xiang Q, et al. Discovery of Potent Dual PROTAC Degraders Targeting BET-Kinase To Overcome FLT3 Inhibitor Resistance. J Med Chem. 2025 Aug 28;68 (16) :17303-17322.