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Seclidemstat {[allProObj[0].p_purity_real_show]}

货号:A486013 同义名: SP-2577;SP-2577 mesylate Ambeed 开学季,买赠积分,赢豪礼

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

Seclidemstat 化学结构 CAS号:1423715-37-0
Seclidemstat 化学结构
CAS号:1423715-37-0
Seclidemstat 3D分子结构
CAS号:1423715-37-0
Seclidemstat 化学结构 CAS号:1423715-37-0
Seclidemstat 3D分子结构 CAS号:1423715-37-0
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Seclidemstat 纯度/质量文件 产品仅供科研

货号:A486013 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 KDM1 KDM2 KDM3 KDM4 KDM5 KDM6 其他靶点 纯度
OG-L002 +++

LSD1, IC50: 20 nM

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ORY-1001 +++

LSD1, IC50: 20 nM

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SP-2509 ++++

LSD1, IC50: 13 nM

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GSK2879552 2HCl +

LSD1, Ki: 1.7 μM

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T-3775440 HCl ++++

LSD1, IC50: 2.1 nM

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GSK-LSD1 2HCl +++

LSD1, IC50: 16 nM

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Pulrodemstat benzenesulfonate {[allProObj[0].p_purity_real_show]}
IOX1 +

KDM2A, IC50: 1.8 μM

+++

KDM3A, IC50: 0.1 μM

++

KDM4C, IC50: 0.6 μM

KDM4E, IC50: 2.3 μM

+

KDM5C, IC50: 19 μM

+

KDM6B, IC50: 1.6 μM

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PFI-90 {[allProObj[0].p_purity_real_show]}
ML324 +

JMJD2, IC50: 920 nM

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NCGC00244536 ++++

KDM4, IC50: 10 nM

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KDM4D-IN-1 ++

KDM4D, IC50: 0.41 μM

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GSK467 ++++

KDM5B, Ki: 10 nM

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GSK-J1 +++

JMJD3, IC50: 60 nM

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(Z)-JIB-04 ++

JMJD2A, IC50: 1100 nM

JMJD2E, IC50: 340 nM

++

JARID1A, IC50: 230 nM

++

JMJD3, IC50: 855 nM

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CPI-455 ++++

KDM5A, IC50: 10 nM

++++

KDM5, IC50: 10 nM

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JIB-04 ++

JMJD2E, IC50: 435 nM

JMJD2D, IC50: 290 nM

++

JARID1A, IC50: 230 nM

++

JMJD3, IC50: 855 nM

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GSK-J4 HCl +++

JMJD3, IC50: 60 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Seclidemstat 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].

Seclidemstat 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 <<

Seclidemstat 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.

Seclidemstat 实验方案

计算器
存储液制备 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

Seclidemstat 技术信息

CAS号1423715-37-0
分子式C20H23ClN4O4S
分子量 450.939
别名 SP-2577;SP-2577 mesylate
运输蓝冰
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
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