CAS:1062368-49-3ML347

Synonyms: LDN-193719

ML347 is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM and shows > 300-fold selectivity for ALK2 vs. ALK3.

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

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实验数据

技术信息

CAS号

1062368-49-3

储存条件

分子式

C22H16N4O

运输

蓝冰

分子量

352.39

别名

LDN-193719

溶解度

DMSO	53.0 mg/mL (150.4 mM)
Water	insoluble

动物实验配方

生物活性

描述The transforming growth factor (TGF)-β superfamily has been implicated into different physiological and pathological processes in a broad range of cell systems. The TGF-β receptor complex is composed of type I, type II and accessory receptors. TGF-β type I receptors have seven isoforms termed activin receptor-like kinases (ALKs) 1 - 7^[2]. ML347 is a selective inhibitor of ALK1/2/3/6 with IC50 values of 46 nM, 32 nM, 10.8 μM and 9.83 μM, respectively^[1]. In vitro, ML347 at dose of 50 nM dampened the GDF2-induced SMAD1/5 phosphorylation in MCF10A cells that express high levels of ALK2^[3]. Utilizing rapid equilibrium dialysis, the protein binding of ML347 was determined in human, rat and mouse plasma shown that similar in all three species with ML347 displaying high plasma protein biding (Fu~0.01 - 0.015). ML347 was unstable to oxidative metabolism – possibly due to the labile methoxy group and therefore was predicted to display high clearance in human and mouse, and moderate to-high clearance in the rat^[1].