Bomedemstat ditosylate

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1990504-72-7

IMG-7289 ditosylate

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 irreversiblelysine-specific demethylase 1(LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibitscancercell proliferation and inducesapoptosis^[1]^[2].

体外研究
(In Vitro)

Bomedemstat selectively inhibits proliferation and induces apoptosis ofJak2^V617Fcells by concomitantly increasing expression and methylation of p53^[1].
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^[1].

Apoptosis Analysis^[1]

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^[1].

Animal Model:	Mx-Jak2^V617Fmice^[1]
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.

Clinical Trial

分子量

864.02

性状

Solid

Formula

C₄₂H₅₀FN₇O₈S₂

CAS 号

1990504-72-7

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)

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。