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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3022265-51-3
分子式: C₂₆H₂₈FN₅O
分子量:445.53

保管条件:

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

Data Sheet (272 KB)

HSB401 構造式

CAS 番号: 3022265-51-3

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

体外実験

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.

体内実験

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.

Related Protocols :

化学情報

CAS 番号 3022265-51-3
分子量 445.53
分子式 C₂₆H₂₈FN₅O
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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]

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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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100 mg

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