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

HSB401 是一种口服有效的 FLT3 抑制剂 (FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, FLT3-ITD 的 IC50 值分别为: 28, 5, 72, 51 nM)。HSB401 可下调 FLT3 信号通路，诱导细胞周期阻滞和凋亡 (apoptosis)。HSB401 不抑制 c-KIT，从而降低骨髓抑制的风险。在 MV4-11 异种移植小鼠模型中，HSB401 可显著抑制肿瘤生长。HSB401 可用于急性髓系白血病的研究。

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HSB401

HSB401 Chemical Structure

CAS No. : 3022265-51-3

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HSB401 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

HSB401 在 K562 细胞中 GI50 值为 0.772 μM，在 MV4-11 细胞中 GI50 值为 0.027 μM[1]。
HSB401 (20-500 nM, 2 小时) 可抑制 MV4-11 细胞中的 FLT3 及其下游信号通路[1]。
HSB401 (20-500 nM, 24 小时) 可诱导 MV4-11 细胞凋亡，激活 caspase 7 和 9，并裂解 PARP-1 蛋白[1]。
HSB401 与重组人 FLT3 激酶结构域具有纳摩尔级的亲和力，其解离常数 KD 与Gilteritinib (HY-12432) 相当[1]。
HSB401 (0.001-10 μM, 72 小时) 对 MOLM13 细胞及其耐药克隆的抗增殖活性与 Gilteritinib 相当，且对耐药 MOLM13 细胞和亲代 MOLM13 细胞的选择性比为 1[1]。
HSB401 (20-500 nM, 2 小时) 可降低 MOLM13 和 Ba/F3 (FLT3-ITD) 细胞系中 FLT3 在 Y589/591 位点的自磷酸化，并以浓度依赖的方式减弱 FLT3 下游信号通路[1]。
HSB401 (6.25-100 nM, 24 小时) 可发挥 FLT3 特异性抑制作用，在 FLT3 依赖性白血病细胞系 (MV4-11, MOLM-13 细胞) 中诱导 G1 期细胞剂量依赖性增加[1]。

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

HSB401 相关抗体:

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.
体内研究
(In Vivo)

HSB401 (30 mg/kg, 口服, 每日一次, 持续 29 天) 在 MV4-11 衍生异种移植小鼠模型中显示出 80.5% 的统计学显著肿瘤生长抑制 (TGI)，且对体重无不良影响[1]。

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.
分子量

445.53

Formula

C26H28FN5O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HSB401 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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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