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Seclidemstat

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Chemical Structure| 1423715-37-0 同义名 : SP-2577;SP-2577 mesylate
CAS号 : 1423715-37-0
货号 : A486013
分子式 : C20H23ClN4O4S
纯度 : 99%+
分子量 : 450.939
MDL号 : MFCD31630770
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(110.88 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03600649 Ewing Sarcoma Phase 1 Recruiting August 2020 United States, California ... 展开 >> Childrens Hospital Los Angeles Recruiting Los Angeles, California, United States, 90027 Contact: Leo Mascarhenas, MD          Contact: Magnolia Manzano          United States, Florida Johns Hopkins All Children's Hospital Not yet recruiting Saint Petersburg, Florida, United States, 33701 Contact: Jessica Crimella          Principal Investigator: Jonathan Metts, MD          Moffitt Cancer Center Recruiting Tampa, Florida, United States, 33612 Contact: Tiffany Smith, MS, CRC          Principal Investigator: Damon Reed, MD          United States, Massachusetts Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Morgan Krush          Principal Investigator: Steven Dubois, MD          United States, Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Douglas Harrison, MD          Contact: Sherry Melton 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.09mL

2.22mL

1.11mL

22.18mL

4.44mL

2.22mL
参考文献

[1]Hosseini A, Minucci S. A comprehensive review of lysine-specific demethylase 1 and its roles in cancer. Epigenomics. 2017;9(8):1123-1142.

[2]Hariprasad V, et al. Substituted benzohydrazide analogs as histone demethylase inhibitors. WO 2017004519 A1.

[3]A Phase I dose escalation and expansion study of seclidemstat (SP-2577) a first-in class reversible LSD1 inhibitor for patients with relapsed or refractory Ewing sarcoma.