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Art. -Nr.: HY-179382

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3022265-51-3
Formel: C₂₆H₂₈FN₅O
Molecular Weight:445.53

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

HSB401 Chemical Structure

CAS. Nr.: 3022265-51-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 K_D 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.

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.

Chemical Information

CAS. Nr. 3022265-51-3
Molecular Weight 445.53
Formel C₂₆H₂₈FN₅O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Dayal N, et al. 3H-pyrazolo[4,3-f]quinoline hinge binder, a tunable scaffold for development of novel kinase inhibitors against FLT3-driven leukemia. Eur J Med Chem. 2026 Jan 15;302(Pt 2):118309. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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