Seclidemstat | SP-2577 | LSD1 Inhibitor | AmBeed-信号通路专用抑制剂

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Seclidemstat {[allProObj[0].p_purity_real_show]}

货号：A486013 同义名： SP-2577;SP-2577 mesylate

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

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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

组蛋白去甲基酶亚型比较

产品名称	KDM1 ↓ ↑	KDM2 ↓ ↑	KDM3 ↓ ↑	KDM4 ↓ ↑	KDM5 ↓ ↑	KDM6 ↓ ↑	纯度
OG-L002	+++ LSD1, IC50: 20 nM						99%+
ORY-1001	+++ LSD1, IC50: 20 nM						98%
SP-2509	++++ LSD1, IC50: 13 nM						98+%
GSK2879552 2HCl	+ LSD1, Ki: 1.7 μM						99%+
T-3775440 HCl	++++ LSD1, IC50: 2.1 nM						98%
GSK-LSD1 2HCl	+++ LSD1, IC50: 16 nM						98%
Pulrodemstat benzenesulfonate	✔						99%+
IOX1		+ KDM2A, IC50: 1.8 μM	+++ KDM3A, IC50: 0.1 μM	++ KDM4E, IC50: 2.3 μM KDM4C, IC50: 0.6 μM	+ KDM5C, IC50: 19 μM	+ KDM6B, IC50: 1.6 μM	99%
PFI-90			✔				99%+
ML324				+ JMJD2, IC50: 920 nM			99%+
NCGC00244536				++++ KDM4, IC50: 10 nM			95%
KDM4D-IN-1				++ KDM4D, IC50: 0.41 μM			99%+
GSK467					++++ KDM5B, Ki: 10 nM		98%
GSK-J1						+++ JMJD3, IC50: 60 nM	99%+
(Z)-JIB-04				++ JMJD2A, IC50: 1100 nM JMJD2E, IC50: 340 nM	++ JARID1A, IC50: 230 nM	++ JMJD3, IC50: 855 nM	97%
CPI-455					++++ KDM5A, IC50: 10 nM	++++ KDM5, IC50: 10 nM	98%
JIB-04				++ JMJD2E, IC50: 435 nM JMJD2D, IC50: 290 nM	++ JARID1A, IC50: 230 nM	++ JMJD3, IC50: 855 nM	98%
GSK-J4 HCl						+++ JMJD3, IC50: 60 nM	98%
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

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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

Seclidemstat {[allProObj[0].p_purity_real_show]}

Seclidemstat 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Seclidemstat 质控信息

Seclidemstat 生物活性

Seclidemstat 临床研究

Seclidemstat 参考文献

Seclidemstat 实验方案

Seclidemstat 技术信息

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Seclidemstat {[allProObj[0].p_purity_real_show]}

Seclidemstat 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Seclidemstat 质控信息

Seclidemstat 生物活性

Seclidemstat 临床研究

Seclidemstat 参考文献

Seclidemstat 实验方案

Seclidemstat 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Seclidemstat 纯度/质量文件产品仅供科研