Seclidemstat mesylate(Synonyms: SP-2577 mesylate)

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Seclidemstat mesylate (Synonyms: SP-2577 mesylate) 纯度: 99.86%

Seclidemstat (SP-2577) mesylate 是一种有效的非竞争性可逆 KDM1A (LSD1) 抑制剂 (Ki=31 nM, IC50)。Seclidemstat mesylate 促进 SWI/SNF 复合物突变卵巢癌的抗肿瘤免疫,并抑制病毒产生、病毒 DNA 复制和晚期基因表达。Seclidemstat mesylate 可用于尤文肉瘤的研究。

Seclidemstat mesylate(Synonyms: SP-2577 mesylate)

Seclidemstat mesylate Chemical Structure

CAS No. : 2044953-70-8

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10 mg ¥2900 In-stock
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50 mg ¥8500 In-stock
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Seclidemstat mesylate 相关产品

相关化合物库:

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  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library

生物活性

Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma[1][2].

IC50 & Target

Ki: 31 nM (LSD1)[1]
IC50: 13 nM (LSD1)[1]

体外研究
(In Vitro)

Seclidemstat (72 hours) mesylate inhibits SWI/SNF-mutation-dependent tumor cell proliferation with IC50 ranging from 0.013 to 2.819 μM (COV434, BIN67, SCCOHT-1, TOV21G, SKOV3, A427, H522, A549, H1299, G401, G402, HCC15 cells)[2].
Seclidemstat (72 hours) mesylate promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in SCCOHT cell lines (SCCOHT-1, BIN67, and COV434 cells)[2].
Seclidemstat (3 μM) mesylate promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

547.04

Formula

C21H27ClN4O7S2

CAS 号

2044953-70-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 53.33 mg/mL (97.49 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8280 mL 9.1401 mL 18.2802 mL
5 mM 0.3656 mL 1.8280 mL 3.6560 mL
10 mM 0.1828 mL 0.9140 mL 1.8280 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Dai XJ, et al. Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1 [published correction appears in J Med Chem. 2021 May 13;64(9):6410-6411]. J Med Chem. 2021;64(5):2466-2488.

    [2]. Soldi R, et al. The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer. PLoS One. 2020;15(7):e0235705. Published 2020 Jul 10.

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