Bomedemstat ditosylate|1990504-72-7|-陌孚医药/Medlife

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Bomedemstat ditosylate

目录号: PL15096 纯度: ≥99%

CAS No. :1990504-72-7

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中文名称	Bomedemstat ditosylate
英文名称	Bomedemstat ditosylate
英文别名	2PYF2U9JNF;N-((2S)-5-(((1R,2S)-2-(4-Fluorophenyl)cyclopropyl)amino)-1-(4-methylpiperazin-1-yl)-1-oxopentan-2-yl)-4-(1H-1,2,3-triazol-1-yl)benzamide bis-tosylate salt;Benzamide, N-((1S)-4-(((1R,2S)-2-(4-fluorophenyl)cyclopropyl)amino)-1-((4-methyl-1-piperazinyl)carbonyl)butyl)-4-(1H-1,2,3-triazol-1-yl)-, 4-methylbenzenesulfonate (1:2);N-((2S)-5-(((1R,2S)-2-(4-Fluorophenyl)cyclopropyl)amino)-1-(4-methylpiperazin-1-yl)-1-oxopentan-2-yl)-4-(1H-1,2,3-t;IMG-7289 ditosylate;Bomedemstat ditosylate
Cas No.	1990504-72-7
分子式	C₄₂H₅₀FN₇O₈S₂
分子量	864.02
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Bomedemstat (IMG-7289) ditosylate 是一种具有口服活性和不可逆的 lysine-specific demethylase 1 (LSD1) 抑制剂。Bomedemstat ditosylate 可以增加 H3K4 和 H3K9 的甲基化，然后改变基因表达。Bomedemstat ditosylate 具有抗癌活性，可抑制癌细胞增殖并诱导细胞凋亡。

生物活性

Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.

性状

Solid

体外研究(In Vitro)

Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2 cells by concomitantly increasing expression and methylation of p53.
Bomedemstat (50 nM-1 μM; 96 h) enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest. has not independently confirmed the accuracy of these methods. They are for reference only.Apoptosis Analysis

体内研究(In Vivo)

Bomedemstat treatment (oral gavage; 45?mg/kg; once daily; 56 d) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Jonas S Jutzi,et al. LSD1 Inhibition Prolongs Survival in Mouse Models of MPN by Selectively Targeting the Disease Clone. Hemasphere.2018 Jun 8;2(3):e54.
[2]. Yuan Fang, et al. LSD1/KDM1A inhibitors in clinical trials: advances and prospects. J Hematol Oncol. 2019 Dec 4;12(1):129.

溶解度数据	In Vitro: DMSO : 100 mg/mL (115.74 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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