2. Immunology/Inflammation Protein Tyrosine Kinase/RTK Apoptosis
  3. IRAK FLT3 Apoptosis
  4. FLT3/IRAK4-IN-1

FLT3/IRAK4-IN-1 is a selective FLT3/IRAK4 inhibitor with the remarkable activity towards FLT3-WT (IC50 = 1.95 nM), FLT3-D835Y (IC50 = 3.22 nM) and IRAK4 (IC50 = 53.72 nM). LT3/IRAK4-IN-1 has relatively low toxicity to normal bone marrow cells, can effectively promote cell apoptosis, and has the potential to overcome drug resistance. FLT3/IRAK4-IN-1 can be used for research on acute myeloid leukemia (AML).

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

FLT3/IRAK4-IN-1 Chemical Structure

FLT3/IRAK4-IN-1 Chemical Structure

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FLT3/IRAK4-IN-1 Related Antibodies

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Description

FLT3/IRAK4-IN-1 is a selective FLT3/IRAK4 inhibitor with the remarkable activity towards FLT3-WT (IC50 = 1.95 nM), FLT3-D835Y (IC50 = 3.22 nM) and IRAK4 (IC50 = 53.72 nM). LT3/IRAK4-IN-1 has relatively low toxicity to normal bone marrow cells, can effectively promote cell apoptosis, and has the potential to overcome drug resistance. FLT3/IRAK4-IN-1 can be used for research on acute myeloid leukemia (AML)[1].

In Vitro

FLT3/IRAK4-IN-1 (Compound HB-29) (1-100 nM; 72h) exhibits IC50 values of 21.84 nM, 24.48 nM, 23.24 nM, 20.11 nM, and 2.86 nM against BaF3 cells carrying FLT3-ITD, FLT3-F691L, FLT3-D835F, FLT3-D835V, and FLT3-ITD/D835Y mutations, respectively[1].
FLT3/IRAK4-IN-1 (1 μM; 24 h) induces approximately 92% apoptosis in MV-4-11 cells[1].
FLT3/IRAK4-IN-1 (1 μM; 8 h) induces apoptosis in MV-4-11 cells co-cultured with cytokines, increases SOD levels and suppresses ROS generation, indicating its potential to overcome adaptive resistance[1].
FLT3/IRAK4-IN-1 (10-1000 nM; 18 h) inhibits the FLT3 and IRAK4 signaling pathways[1].

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

FLT3/IRAK4-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: MV-4-11, Molm13, THP-1, TF-1, HS-5
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 72 h
Result: Exhibited IC50 values of 21.84 nM, 24.48 nM, 23.24 nM, 20.11 nM, 2.86 nM, 1.80 nM and 7.86 nM against BaF3 cells carrying FLT3-ITD, FLT3-F691L, FLT3-D835F, FLT3-D835V, FLT3-ITD/D835Y mutations, MV-4-11 and Molm13, respectively.
Exhibited moderate inhibitory effect against the THP-1 (IC50 = 0.43 μM).

Cell Cytotoxicity Assay[1]

Cell Line: HS-5
Concentration: 3.62 μM
Incubation Time: 0 h; 10 h; 20 h; 30 h; 40 h; 50 h; 60 h; 70 h; 80 h
Result: Exhibited a favorable safety profile in normal bone marrow cells (SI ＞ 2000), the EC50 value of HB-29 against HS-5 was 3.62 μM.

Apoptosis Analysis[1]

Cell Line: MV-4-11
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 24 h
Result: Induced 92% apoptosis at 1 μM vs. 60.7% by CA-4948.
Significantly induced apoptosis in MV-4-11 cells co-cultured with cytokines at concentrations of 1 nM.

Western Blot Analysis[1]

Cell Line: MV-4-11
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 18 h
Result: Inhibited FLT3 phosphorylation and the phos­phorylation of its downstream targets STAT5, AKT, and ERK in a dose-dependent manner.
Suppressing IRAK4 phos­phorylation and the phosphorylation of its downstream target p65.
Molecular Weight

388.44

Formula

C22H21FN6
SMILES

FC1=CC=CC(N2C=CC3=C2N=C(N=C3)NC4=CC(N[C@H]5CCNC5)=CC=C4)=C1
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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FLT3/IRAK4-IN-1 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:

FLT3/IRAK4-IN-1IRAKFLT3ApoptosisInterleukin-1 receptor associated kinaseIL-1R associated kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Antiproliferative activityCDK9Structure-activity relationshipTetrahydrothiazolopyridineInhibitorinhibitorinhibit

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