HSB401
HSB401 is an orally active FLT3 inhibitor (IC50: 28, 5, 72, 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, FLT3-ITD, respectively). HSB401 downregulates FLT3 signaling and induces cell cycle arrest and apoptosis. HSB401 spares c-KIT inhibition, thereby reducing the risk of myelosuppression. HSB401 significantly suppresses tumor growth in the MV4-11 xenograft mouse model. HSB401 can be used for the research of acute myeloid leukemia.
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- No. CAS: 3022265-51-3
- Fòrmula: C26H28FN5O
- Peso molecular:445.53
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
HSB401 exhibits the GI50 value of 0.772 μM in K562 cells and 0.027 μM in MV4-11 cells[1].
HSB401 (20-500 nM, 2 h) inhibits FLT3 and its downstream signaling pathways in MV4-11 cells[1].
HSB401 (20-500 nM, 24 h) induces apoptotic cell death in MV4-11 cells, the activation of caspases 7 and 9 and the cleavage of protein PARP-1[1].
HSB401 shows nanomolar affinity to bind the kinase domain of recombinant human FLT3, with a KD comparable to that of Gilteritinib (HY-12432)[1].
HSB401 (0.001-10 μM, 72 h) exhibits antiproliferative activity against MOLM13 cells and their resistant clones comparable to that of Gilteritinib, with a selectivity ratio of 1 between resistant and parental MOLM13 cells[1].
HSB401 (20-500 nM, 2 h) reduces the FLT3 autophosphorylation at Y589/591 and attenuates FLT3 downstream signaling pathways in concentration-dependent manner in MOLM13 and Ba/F3 (FLT3-ITD) cell lines[1].
HSB401 (6.25-100 nM, 24 h) exerts FLT3-specific inhibitory effects, inducing a dose-dependent increase in G1 cells in the FLT3-dependent leukemia cell lines (MV4-11, MOLM-13 cells)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13 cells
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 h
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Result:Exhibited comparable antiproliferative activity against parental MOLM13 cells and their resistant clones.
Showed the selectivity ratio of 1 between resistant MOLM13 cells and parental MOLM13 cells.
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Cell Line:MOLM13 and Ba/F3 (FLT3-ITD) cell lines
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Concentration:20, 100, 500 nM
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Incubation Time:2 h
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Result:Reduced the FLT3 autophosphorylation at Y589/591.
Attenuated FLT3 downstream signaling pathways in concentration-dependent manner.
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Cell Line:MV4-11 cells
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Concentration:20, 100, 500 nM
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Incubation Time:24 h
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Result:Induced apoptotic cell death in MV4-11 cells.
Induced the activation of caspases 7 and 9 and the cleavage of protein PARP-1.
Reduced the level of Mcl-1 dose-dependently.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11-derived xenograft BALB/c nude female mice[1]
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Dosage:30 mg/kg
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Administration:daily oral gavage (p.o.) for 29 days
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Result:Displayed a statistically significant tumor growth inhibition (TGI) of 80.5 %.
Induced no adverse effect on the weight of mice.
Chemical Information
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No. CAS 3022265-51-3
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Peso molecular 445.53
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Fòrmula C26H28FN5O
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SMILES
CN(C)CCNC(C(C=C1)=CC(F)=C1C(C2=C3CCCC2)=NC4=C3C(C(C)=NN5)=C5C=C4)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HSB401 Related Classifications
HY-179382 Related Classifications
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