2. PROTAC Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling Epigenetics
  3. PROTACs FLT3 JAK Epigenetic Reader Domain
  4. PROTAC FLT3/JAK2/BRD4 Degrader-1

PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)).

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

PROTAC FLT3/JAK2/BRD4 Degrader-1

PROTAC FLT3/JAK2/BRD4 Degrader-1 Chemical Structure

CAS No. : 3067695-20-6

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PROTAC FLT3/JAK2/BRD4 Degrader-1 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939))[1].

IC50 & Target[1]

Cereblon

 

BRD4

1.17 nM (DC50)

JAK2

0.678 nM (DC50)

FLT3

5.23 nM (DC50)

In Vitro

PROTAC FLT3/JAK2/BRD4 Degrader-1 (Compound 13e) degrades FLT3, JAK2, and BRD4 in MV4;11 cells with DC50 values of 5.23, 0.678, and 1.17 nM, respectively[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1 μM, 8 h) induces cereblon- and proteasome-dependent degradation via the ubiquitin-proteasome system (UPS) of FLT3, JAK2, and BRD4 in MV4;11 cells[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (0.00001-1000 nM, 96 h) potently inhibits MV4;11 cell proliferation with an IC50 of 0.79 nM[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (96 h) exhibits potent anti-proliferative activity against FLT3 mutant-transformed Ba/F3 cells, including FLT3-ITD-D835Y (IC50 = 35.64 nM), FLT3-ITD-F691L (IC50 = 24.34 nM ), FLT3-ITD-N676D (IC50 = 43.71 nM ), FLT3-ITD-D835V (IC50 = 6.63 nM ), FLT3-ITD-Y842C (IC50 = 8.80 nM), and FLT3-ITD (IC50 = 28.62 nM )[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1-1000 nM, 48 h) induces over 70% apoptosis in MV4;11 cells[1].

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

PROTAC FLT3/JAK2/BRD4 Degrader-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV4;11 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 48 h
Result: Induced over 70% apoptosis in MV4;11 cells.
Suppressed activated apoptotic proteins PARP, Caspase 9, Caspase 3.
Upregulated Cleaved-caspase 3.
In Vivo

PROTAC FLT3/JAK2/BRD4 Degrader-1 (Compound 13e) (10 mg/kg, i.p., once daily, 21 days) demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice[1].

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

Animal Model: MV4;11 cells (3 × 106) were subcutaneously implanted into the right flanks of four-week-old female nonobese diabetic severe combined immune-deficiency (NOD SCID) mice to establish the MV4;11 xenograft model[1]
Dosage: 10 mg/kg
Administration: i.p., once daily, 21 days
Result: Achieved a tumor growth inhibition (TGI) rate of 62% at a dose of 10 mg/kg in the MV4;11 xenograft model.
Showed no significant changes in body weight.
Molecular Weight

883.00

Formula

C44H51FN10O7S
CAS No.
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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC FLT3/JAK2/BRD4 Degrader-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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 FLT3/JAK2/BRD4 Degrader-13067695-20-6PROTACsFLT3JAKEpigenetic Reader DomainCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Janus kinaseacute myeloid leukemia (AML)PROTACJAK2BRD4MV4;11 cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC FLT3/JAK2/BRD4 Degrader-1
Cat. No.:
HY-175610
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.