2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs FLT3 Apoptosis
  4. PROTAC FLT-3 degrader 4

PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor).

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PROTAC FLT-3 degrader 4 Chemical Structure

PROTAC FLT-3 degrader 4 Chemical Structure

CAS No. : 2956722-48-6

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PROTAC FLT-3 degrader 4 Related Antibodies

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Description

PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor)[1].

IC50 & Target[1]

Cereblon

 

In Vitro

PROTAC FLT-3 degrader 4 (compound A20) shows antiproliferative activities against MV4-11 and MOLM-13 cells (IC50 of 39.9 nM and 169.9 nM, respectively)[1].
PROTAC FLT-3 degrader 4 (0.25-100 nM; 24 h) demonstrates a substantial reduction in FLT3-ITD protein levels in MV4-11 and MOLM-13 cells[1].
PROTAC FLT-3 degrader 4 (20 nM; 12 h) inhibits FLT3-ITD phosphorylation and its downstream signal mediators including STAT5, S6K, and ERK in MV4-11 and MOLM-13 cells[1].
PROTAC FLT-3 degrader 4 (20 nM; 12 h) dose-dependently induces cycle arrest in the G1 phase. PROTAC FLT-3 degrader 4 also dose-dependently induces the apoptosis of MV4-11 and MOLM-13 cells[1].

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

PROTAC FLT-3 degrader 4 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 0.25 nM, 0.5 nM, 1 nM, 5 nM, 10 nM, 20 nM, 50 nM, 80 nM, 100 nM
Incubation Time: 24 h
Result: Showed potent FLT3-ITD degradation activity with DC50 values of 7.4 nM and 20.1 nM for MV4-11 and MOLM-13 cells, respectively.

Apoptosis Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 1 nM, 5 nM, 50 nM
Incubation Time: 24 h
Result: Blocked AML cell cycle in G1 phase and induced apoptosis.
In Vivo

PROTAC FLT-3 degrader 4 (compound A20; 1.235-10 mg/kg; po; daily; for 2 weeks) significantly inhibits tumor growth at 1.25 mg/kg. Tumor regression is observed at 5 mg/kg (TGI = 97.5%), and complete regression is observed at 10 mg/kg[1].
Pharmacokinetic Parameters of PROTAC FLT-3 degrader 4 in Sprague-Dawley rats[1].
1.19

parameter iv (1 mg/kg) po (10 mg/kg)
AUC0-t (h·ng/mL) 2768.1 14705.3
Cmax (ng/mL) - 1117.5
Tmax (h) - 6.2
T1/2 (h) 6.5 3.8
Vss (L/kg) 3.5 5.7
CL (mL/min/kg) 5.5 11.2
F (%) - 53

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

Animal Model: Four week old male nu/nu mice injected with MV4-11 cells[1]
Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration: po; daily; for 2 weeks
Result: Significantly inhibited tumor growth at 1.25 mg/kg.
Molecular Weight

736.79

Formula

C39H41FN8O6
CAS No.
SMILES

O=C1NC2=CC=C(C=C2/C1=C/C3=C(C(NC(CN4CCN(CC4)CC5CCN(CC5)C6=CC=C7C(N(C(C7=C6)=O)C8CCC(NC8=O)=O)=O)=O)=CN3)C)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC FLT-3 degrader 4 Related Classifications

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Help & FAQs
  • 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.

Keywords:

PROTAC FLT-3 degrader 42956722-48-6PROTACsFLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3antiproliferative activitiesPROTAC FLT-3 degradercycle arrestSTAT5S6KERKInhibitorinhibitorinhibit

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