Bomedemstat ditosylate IMG-7289 ditosylate|cas:1990504-72-7|西域试剂

Bomedemstat ditosylate IMG-7289 ditosylate,99.17%

产品编号：Bellancom-109169A| CAS NO：1990504-72-7| 分子式：C₄₂H₅₀FN₇O₈S₂| 分子量：864.02

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货号	价格	库存与货期
Bellancom-109169A	￥3500.00	杭州北京（现货）
Bellancom-109169A	￥5800.00	杭州北京（现货）
Bellancom-109169A	￥11500.00	杭州北京（现货）

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Bomedemstat ditosylate IMG-7289 ditosylate

产品介绍

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.

体外研究

Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2^V617F 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.

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

Apoptosis Analysis

Cell Line:	SET-2 cells
Concentration:	50 nM, 100 nM, and 1 μM
Incubation Time:	96 hours
Result:	Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA.

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.

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

Animal Model:	Mx-Jak2^V617F mice
Dosage:	45 mg/kg
Administration:	Oral gavage; 45 mg/kg; once daily; 56 days
Result:	Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.

体内研究

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

Animal Model:	Mx-Jak2^V617F mice
Dosage:	45 mg/kg
Administration:	Oral gavage; 45 mg/kg; once daily; 56 days
Result:	Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.

体内研究

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

Animal Model:	Mx-Jak2^V617F mice
Dosage:	45 mg/kg
Administration:	Oral gavage; 45 mg/kg; once daily; 56 days
Result:	Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (115.74 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1574 mL	5.7869 mL	11.5738 mL
5 mM	0.2315 mL	1.1574 mL	2.3148 mL
10 mM	0.1157 mL	0.5787 mL	1.1574 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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

参考文献