PROTAC FLT3/CHK1 Degrader-1
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML) . (Pink: FLT3/CHK1 ligand (HY-178869), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238) ) [1].
Product Specifications
UNSPSC
12352005
Target
Akt; Checkpoint Kinase (Chk) ; c-Myc; ERK; FLT3; PROTACs; STAT
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Field of Research
Cancer
Smiles
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=C(N4CC(CN[C@H]5CC[C@@H](NC6=NC(NC7=CC=C(OCC(C)(O)C)C=C7)=NC=C6C(F)(F)F)CC5)C4)C(F)=C3)=O
Molecular Formula
C38H42F4N8O6
Molecular Weight
782.78
References & Citations
[1]Lian X, et al. Development of Dual FLT3 and CHK1 PROTACs for the Treatment of AML. J Med Chem. 2025 Oct 23;68 (20) :21939-21961.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon; Chk1
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