HM43239|2294874-49-8|(HM43239)-陌孚医药/Medlife

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HM43239 (Synonyms: HM43239)

目录号: PL04051 纯度: ≥99%

CAS No. :2294874-49-8

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中文名称	HM43239
英文名称	HM43239
英文别名	rel-5-Chloro-N-[3-cyclopropyl-5-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)-2-pyrimidinamine;HM43239;C0WUS7XXE9;US10870639, Example 8;BDBM476700;DB15343;2-Pyrimidinamine, 5-chloro-N-(3-cyclopropyl-5-(((3R,5S)-3,5-dimethyl-1-piperazinyl)methyl)phenyl)-4-(6-methyl-1H-indol-3-yl)-, rel-;5-Chloro-N-(3-cyclopropyl-5-(((3R,5S)-3,5-dimethylpiperazine-1-yl) methyl) phenyl)-4-(6-methyl-1hindol-3-yl) pyrimidin-2-amine;5-chloro-N-(3-cyclopropyl-5-(((3R,5S)-3,5-dimethylpiperazine-1-yl)methyl)phenyl)-4-(6-methyl-1H;Unii-C0wus7xxe9
Cas No.	2294874-49-8
分子式	C₂₉H₃₃ClN₆
分子量	501.07
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

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)。

生物活性

HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s 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.

性状

Solid

IC50 & Target[1][2]

FLT3 WT 1.1 nM (IC50) FLT3 ITD 1.8 nM (IC

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.
HM43239 induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells).
HM43239 potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells. 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.
HM43239 prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models. has not independently confirmed the accuracy of these methods. They are for reference only.

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)

ClinicalTrial

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].

溶解度数据	In Vitro: DMSO : 125 mg/mL (249.47 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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