CAS:1423715-37-0Seclidemstat

Seclidemstat is a potent LSD1 inhibitor, with a mean IC50 of 127 nM.

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

1423715-37-0

储存条件

分子式

C20H23ClN4O4S

运输

蓝冰

分子量

450.94

别名

溶解度

DMSO	33.33 mg/mL (73.9 mM)
Water	insoluble

动物实验配方

生物活性

描述Histone methylation plays an important role in the regulation of chromatin structure, and its dynamics regulates important cellular processes. Lysine-specific demethylase 1 (LSD1, also known as KDM1A), the first discovered histone lysine demethylase, is able to demethylase H3K4me1/2 and H3K9me1/2 at target loci in a context-dependent manner. LSD1 regulates the balance between self-renewal and differentiation of stem cells, and is highly expressed in various cancers^[1]. Seclidemstat (SP-2577) is a potent and orally bioavailable LSD1 inhibitor, with IC50 of 127 nM^[2]. Seclidemstat has been granted Fast Track Designation by the FDA for the treatment of relapsed/refractory patients with Ewing sarcoma and is currently under investigation in an ongoing phase I trial (NCT03600649) in patients with Ewing sarcoma. The starting dose of seclidemstat is 75 mg PO BID with seven dose levels planned by modified Fibonacci schema^[3].