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Cat. No.: HY-158325

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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).

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

CAS No.: 2956722-48-6
Formula: C₃₉H₄₁FN₈O₆
Molecular Weight:736.79

Storage:

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

Data Sheet (270 KB)

PROTAC FLT-3 degrader 4 Chemical Structure

CAS No.: 2956722-48-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Cereblon

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	31.3 nM Compound: A20	Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD D835Y mutant incubated for 48 hrs by CCK8 assay Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD D835Y mutant incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
BaF3	IC₅₀	45.1 nM Compound: A20	Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD D835V mutant incubated for 48 hrs by CCK8 assay Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD D835V mutant incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
BaF3	IC₅₀	46.7 nM Compound: A20	Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD Y842H mutant incubated for 48 hrs by CCK8 assay Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD Y842H mutant incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
BaF3	IC₅₀	66.2 nM Compound: A20	Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD F691L mutant incubated for 48 hrs by CCK8 assay Antiproliferative activity against mouse Ba/F3 cells expressing FLT3-ITD F691L mutant incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
HL-60	IC₅₀	>40000 nM Compound: A20	Antiproliferative activity against human HL-60 cells expressing wild-type FLT3 incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells expressing wild-type FLT3 incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MOLM-13	IC₅₀	147.4 nM Compound: A20	Antiproliferative activity against Sunitinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against Sunitinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MOLM-13	IC₅₀	169.9 nM Compound: A20	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MOLM-13	IC₅₀	483.6 nM Compound: A20	Antiproliferative activity against Quizartinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against Quizartinib-resistant human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
MV4-11	IC₅₀	39.9 nM Compound: A20	Antiproliferative activity against human MV4-11 cells expressing FLT3-ITD mutant incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells expressing FLT3-ITD mutant incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
THP-1	IC₅₀	15117.5 nM Compound: A20	Antiproliferative activity against human THP-1 cells expressing wild-type FLT3 incubated for 48 hrs by CCK8 assay Antiproliferative activity against human THP-1 cells expressing wild-type FLT3 incubated for 48 hrs by CCK8 assay	[PMID: 38655686]
U-937	IC₅₀	>40000 nM Compound: A20	Antiproliferative activity against human U-937 cells expressing wild-type FLT3 incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-937 cells expressing wild-type FLT3 incubated for 48 hrs by CCK8 assay	[PMID: 38655686]

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.

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].

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.

Chemical Information

CAS No. 2956722-48-6
Molecular Weight 736.79
Formula C₃₉H₄₁FN₈O₆
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Junwei Wang, et al. Discovery of a Novel Orally Bioavailable FLT3-PROTAC Degrader for Efficient Treatment of Acute Myeloid Leukemia and Overcoming Resistance of FLT3 Inhibitors. J Med Chem. 2024 May 9;67(9):7197-7223. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC FLT-3 degrader 4

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC FLT-3 degrader 4 Related Classifications

HY-158325 Related Classifications