2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FLT3 Apoptosis
  4. 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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HSB401

HSB401 Chemical Structure

CAS No. : 3022265-51-3

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HSB401 Related Antibodies

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Description

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[1].

In Vitro

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.

HSB401 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MOLM-13 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: MOLM13 and Ba/F3 (FLT3-ITD) cell lines
Concentration: 20, 100, 500 nM
Incubation Time: 2 h
Result: Reduced the FLT3 autophosphorylation at Y589/591.
Attenuated FLT3 downstream signaling pathways in concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 20, 100, 500 nM
Incubation Time: 24 h
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.
In Vivo

HSB401 (30 mg/kg, p.o., daily for 29 days) displays a statistically significant tumor growth inhibition (TGI) of 80.5 %, without an adverse effect on the weight in MV4-11-derived xenograft mouse model[1].

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

Animal Model: MV4-11-derived xenograft BALB/c nude female mice[1]
Dosage: 30 mg/kg
Administration: daily oral gavage (p.o.) for 29 days
Result: Displayed a statistically significant tumor growth inhibition (TGI) of 80.5 %.
Induced no adverse effect on the weight of mice.
Molecular Weight

445.53

Formula

C26H28FN5O
CAS No.
SMILES

CN(C)CCNC(C(C=C1)=CC(F)=C1C(C2=C3CCCC2)=NC4=C3C(C(C)=NN5)=C5C=C4)=O
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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HSB401 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:

HSB4013022265-51-3HSB 401HSB-401FLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Acute myeloid leukemiaKinase inhibitionInhibitorinhibitorinhibit

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