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.
- Formula: C22H21FN6
- Molecular Weight:388.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:MV-4-11, Molm13, THP-1, TF-1, HS-5
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Concentration:1 nM, 10 nM, 100 nM
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Incubation Time:72 h
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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).
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Cell Line:HS-5
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Concentration:3.62 μM
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Incubation Time:0 h; 10 h; 20 h; 30 h; 40 h; 50 h; 60 h; 70 h; 80 h
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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.
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Cell Line:MV-4-11
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Concentration:1 nM, 10 nM, 100 nM
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Incubation Time:24 h
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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.
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Cell Line:MV-4-11
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Concentration:1 nM, 10 nM, 100 nM
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Incubation Time:18 h
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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.
Chemical Information
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Molecular Weight 388.44
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Formula C22H21FN6
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SMILES
FC1=CC=CC(N2C=CC3=C2N=C(N=C3)NC4=CC(N[C@H]5CCNC5)=CC=C4)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FLT3/IRAK4-IN-1 Related Classifications
HY-176735 Related Classifications
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