Cat. No.: HY-175610

PROTAC FLT3/JAK2/BRD4 Degrader-1

PROTAC FLT3/JAK2/BRD4 Degrader-1 is a FLT3/JAK2/BRD4 PROTAC degrader with DC₅₀ values of 5.23, 0.68, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces cereblon- and proteasome-dependent degradation of FLT3, JAK2, and BRD4 via the ubiquitin-proteasome system. PROTAC FLT3/JAK2/BRD4 Degrader-1 is used in studies related to FLT3 inhibitor-resistant leukemia and acute myeloid leukemia.
(Pink: FLT3 and BRD4 and JAK2 ligand (HY-175611); Blue: Cereblon ligand (HY-W087383); Black: linker).

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

CAS No.: 3067695-20-6
Formula: C₄₄H₅₁FN₁₀O₇S
Molecular Weight:883.00

Storage:

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

Data Sheet (270 KB)

PROTAC FLT3/JAK2/BRD4 Degrader-1 Chemical Structure

CAS No.: 3067695-20-6

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Use of MCE Products

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

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

Biological Activity

Description

PROTAC FLT3/JAK2/BRD4 Degrader-1 is a FLT3/JAK2/BRD4 PROTAC degrader with DC₅₀ values of 5.23, 0.68, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces cereblon- and proteasome-dependent degradation of FLT3, JAK2, and BRD4 via the ubiquitin-proteasome system. PROTAC FLT3/JAK2/BRD4 Degrader-1 is used in studies related to FLT3 inhibitor-resistant leukemia and acute myeloid leukemia^[1]. (Pink: FLT3 and BRD4 and JAK2 ligand (HY-175611); Blue: Cereblon ligand (HY-W087383); Black: linker).

IC₅₀ & Target

^[1]

JAK2

0.678 nM (DC₅₀)

BRD4

1.17 nM (DC₅₀)

BRD2

11.97 nM (DC₅₀)

BRD3

24.46 nM (DC₅₀)

Cereblon

All PROTACs Isoforms :

All JAK Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	DC₅₀	5.23 nM	Degradation of FLT3 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation. Degradation of FLT3 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation.	40764262
MV4-11	DC₅₀	0.68 nM	Degradation of JAK2 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation. Degradation of JAK2 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation.	40764262
MV4-11	DC₅₀	1.17 nM	Degradation of BRD4 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation. Degradation of BRD4 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation.	40764262
MV4-11	DC₅₀	11.97 nM	Degradation of BRD2 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation. Degradation of BRD2 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation.	40764262
MV4-11	DC₅₀	24.46 nM	Degradation of BRD3 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation. Degradation of BRD3 protein in human MV4;11 acute myeloid leukemia cells measured via Western blotting after 24 h incubation.	40764262
MV4-11	IC₅₀	0.79 nM	Antiproliferative activity against human MV4;11 acute myeloid leukemia cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay. Antiproliferative activity against human MV4;11 acute myeloid leukemia cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay.	40764262
BaF3	IC₅₀	35.64 nM	Antiproliferative activity against FLT3-ITD-D835Y mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay. Antiproliferative activity against FLT3-ITD-D835Y mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay.	40764262
BaF3	IC₅₀	24.34 nM	Antiproliferative activity against FLT3-ITD-F691L mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay. Antiproliferative activity against FLT3-ITD-F691L mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay.	40764262
BaF3	IC₅₀	43.71 nM	Antiproliferative activity against FLT3-ITD-N676D mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay. Antiproliferative activity against FLT3-ITD-N676D mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay.	40764262
BaF3	IC₅₀	6.63 nM	Antiproliferative activity against FLT3-ITD-D835V mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay. Antiproliferative activity against FLT3-ITD-D835V mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay.	40764262
BaF3	IC₅₀	8.80 nM	Antiproliferative activity against FLT3-ITD-Y842C mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay. Antiproliferative activity against FLT3-ITD-Y842C mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay.	40764262
BaF3	IC₅₀	28.62 nM	Antiproliferative activity against FLT3-ITD mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay. Antiproliferative activity against FLT3-ITD mutant-transformed Ba/F3 cells assessed as reduction in cell viability incubated for 96 hrs by CCK8 assay.	40764262

In Vitro

PROTAC FLT3/JAK2/BRD4 Degrader-1 (compound 13e) (96 h) potently inhibits the proliferation of MV4;11 acute myeloid leukemia cells with an IC₅₀ of 0.79 nM, while exhibiting extremely low cytotoxicity against normal HEK293 and HUVEC cells. It also potently suppresses the proliferation of Ba/F3 cells transformed with FLT3 mutations, with IC₅₀ values ranging from 6.63 nM to 43.71 nM, indicating its potential to overcome resistance to FLT3 inhibitors^[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1.6 nM-2 μM; 48 h) significantly induces apoptosis in MV4;11 acute myeloid leukemia cells at low micromolar concentrations and modulates key apoptosis-related proteins^[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1.6 nM-2 μM; 1-24 h) rapidly degrades FLT3, JAK2 and BRD4 proteins in a dose- and time-dependent manner in MV4;11 cells, with DC₅₀ values of 5.23, 0.68 and 1.17 nM, respectively^[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 cells
Concentration:

1.6, 8 nM, 0.04, 0.2, 1, 2 μM
Incubation Time:

1, 2, 4, 6, 8, 16, 24 h
Result:

Induced the degradation of FLT3, JAK2, BRD4, as well as BRD2 and BRD3 proteins in a highly concentration-dependent manner.
Significantly degraded BRD4 within 4 h, and almost completely degraded FLT3, JAK2, and BRD4 between 8 and 24 h.

Apoptosis Analysis^[1]

Cell Line:

MV4;11 cells
Concentration:

1, 10, 100, 1000 nM
Incubation Time:

48 h
Result:

Induced over 70% of cells to undergo apoptosis at extremely low concentrations (10 nM).

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	CL
Rat^[1]	10 mg/kg	i.p.	5.90 h	0.08 h	3793 ng/mL	1863 ng·h/mL	1887 ng·h/mL	1.62 mL/min/kg

In Vivo

PROTAC FLT3/JAK2/BRD4 Degrader-1 (compound 13e) (10 mg/kg; i.p.; once daily; for 21 consecutive days) exhibits potent antitumor activity and favorable safety profiles in the NOD SCID mouse leukemia xenograft model established via subcutaneous injection of MV4;11 cells^[1].

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

Animal Model:

NOD SCID (female, 4 weeks old, subcutaneous implantation of 3 × 10⁶ MV4;11 cells)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; once daily; 21 days
Result:

Achieved a tumor growth inhibition (TGI) of 62%.
Showed no significant weight loss during the study.

Chemical Information

CAS No. 3067695-20-6
Molecular Weight 883.00
Formula C₄₄H₅₁FN₁₀O₇S
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
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]. Xiang Q, et al. Discovery of Potent Dual PROTAC Degraders Targeting BET-Kinase To Overcome FLT3 Inhibitor Resistance. Journal of medicinal chemistry. 2025 Aug 28;68(16):17303-17322. [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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PROTAC FLT3/JAK2/BRD4 Degrader-1

All PROTACs Isoforms

All JAK Isoforms

All Epigenetic Reader Domain Isoforms