HM43239

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HM43239  纯度: 99.77%

HM43239 是具有口服活性的选择性 FLT3 抑制剂，IC50 值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。HM43239 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性，并调节 p-STAT5, p-ERK SYK, JAK1/2 和 TAK1。HM43239 抑制白血病细胞的增殖，诱导细胞凋亡 (apoptosis)。

HM43239

HM43239 Chemical Structure

CAS No. : 2294874-49-8

规格 价格 是否有货 数量
5 mg ￥4800 In-stock
10 mg ￥8000 In-stock
50 mg   询价  
100 mg   询价  

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HM43239 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells[1][2][3].

IC50 & Target[1]

FLT3 WT

1.1 nM (IC50)

FLT3 ITD

1.8 nM (IC50)

FLT3 D835Y

1.0 nM (IC50)

体外研究
(In Vitro)

HM43239 potently inhibits the growth of acute myeloid leukemia cell lines harboring FLT3 ITD mutation, such as MV4-11 (IC50: 1.3 nM), MOLM-13 (IC50: 5.1 nM), and MOLM-14 (IC50: 2.9 nM). HM43239 also inhibits KG1a cells (CD34+/CD38- cells) proliferation[1].
HM43239 induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells)[1].
HM43239 potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

HM43239 shows the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell lines without any significant toxicity[1].
HM43239 prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

501.07

Formula

C29H33ClN6
CAS 号

2294874-49-8
运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (249.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9957 mL 9.9786 mL 19.9573 mL
5 mM 0.3991 mL 1.9957 mL 3.9915 mL
10 mM 0.1996 mL 0.9979 mL 1.9957 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Miyoung Lee, et.al. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res July 1 2018 (78) (13 Supplement) 804.

    [2]. Naval G. Daver, et.al. HM43239, a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations: Phase 1 /2 Study. Blood 2019; 134 (Supplement_1): 1331.

    [3]. JiSook Kim, et.al. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res July 1 2019 (79) (13 Supplement) 1293.

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