1. PROTAC Protein Tyrosine Kinase/RTK Immunology/Inflammation
  2. PROTACs Molecular Glues FLT3 IKZF Family
  3. PROTAC FLT-3 degrader 5

PROTAC FLT-3 degrader 5 is a FLT3 PROTAC degrader (DC50 = 1.2 nM). PROTAC FLT-3 degrader 5 functions as a molecular glue to degrade cereblon substrates GSPT1 and IKZF1/3. PROTAC FLT-3 degrader 5 exhibits antiproliferative activity against drug-resistant acute myeloid leukemia (AML) cells and is potentially useful in AML research. (Pink: FLT3/GSPT1/IKZF1/3 ligand: (HY-169374); Blue: Thalidomide: (HY-14658); Black: linker; Thalidomide + linker: (HY-W1123823)).

For research use only. We do not sell to patients.

PROTAC FLT-3 degrader 5

PROTAC FLT-3 degrader 5 Chemical Structure

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Description

PROTAC FLT-3 degrader 5 is a FLT3 PROTAC degrader (DC50 = 1.2 nM). PROTAC FLT-3 degrader 5 functions as a molecular glue to degrade cereblon substrates GSPT1 and IKZF1/3. PROTAC FLT-3 degrader 5 exhibits antiproliferative activity against drug-resistant acute myeloid leukemia (AML) cells and is potentially useful in AML research. (Pink: FLT3/GSPT1/IKZF1/3 ligand: (HY-169374); Blue: Thalidomide: (HY-14658); Black: linker; Thalidomide + linker: (HY-W1123823))[1].

IC50 & Target[1]

Cereblon

 

IKZF1

 

IKZF3

 

In Vitro

PROTAC FLT-3 degrader 5 (Compound A2) shows antiproliferative activity against MV-4-11 FLT3-ITD, MV-4-11 FLT3-ITD-F691L, MV-4-11 FLT3-ITD-D835Y, MOLM-13 FLT3-ITD, MOLM-13 FLT3-ITD-F691L, MOLM-13-D835Y, with IC50s of 1.67, 4.74, 3.70, 3.16, 5.61, 7.55 nM, respectively, has no effect on the proliferation of FLT3 wild-type cells (IC50 > 1000)[1].
PROTAC FLT-3 degrader 5 (0-100 nM, 24 h) reduces FLT3, GSPT1, IKZF1, IKZF3 protein expression in MV-4-11 and MOLM-13 cells[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MV-4-11 cells, MOLM-13 cells
Concentration: 0 nM, 1.5 nM, 3.1 nM, 6.2 nM, 12.5 nM,25 nM, 50 nM, 100 nM
Incubation Time: 24 h
Result: Reduced FLT3, GSPT1, IKZF1, IKZF3 protein expression, degraded FLT3 protein through the proteasome-dependent fashion.
Molecular Weight

878.03

Formula

C46H59N11O7

SMILES

O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC(N(C4)CCC4CN5CCN(C(CC6)CCN6C(C=C7)=C(OC)C=C7NC8=NC(NC9CCOCC9)=C(CC)N=C8C(N)=O)CC5)=C3)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PROTAC FLT-3 degrader 5
Cat. No.:
HY-175040
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