| 产品描述: | Seclidemstat (SP-2577) 是一种有效的、口服的、可生物利用的 lysine-specific demethylase 1 (LSD1/KDM1A) 的抑制剂,IC50值为13 nM。 Seclidemstat(SP-2577)具有潜在的抗肿瘤活性 |
| 靶点: |
LSD1/KDM1A(Cell-free assay):127 nM;HistoneDemethylase |
| 体外研究: |
The combination therapy of Seclidemstat (SP-2577) with checkpoint inhibitors may induce or augment immunogenic responses of SWI/SNF-mutated ovarian cancers. Seclidemstat promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in small cell carcinoma of the ovary hypercalcemic type (SCCOHT) cell lines. Seclidemstat (3 μM) promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line |
| 体内研究: |
SP-2577 (Seclidemstat) is an inhibitor of lysine-specific demthylase KDM1A (LSD1) potential antineoplastic activity against pediatric sarcomas. |
| 细胞实验: |
Cell lines: Small cell carcinoma of the ovary hypercalcemic type (SCCOHT) cell lines, ovarian clear cell carcinomas (OCCC) cell lines Concentrations: 1μM,3 μM Incubation Time: 72 h Method: The SCCOHT and OCCC cell lines are seeded in T-25 tissue culture treated flasks at 3 x 105 cells in 5mL of the appropriate phenol red free complete growth medium. After 48 h, at 70–80% confluency, the cells are treated with 3μM or 1μM of Seclidemstat. After 72 h, the media is collected from the flasks and stored at -80°C until use for various assays. |
| 动物实验: |
Animal Models: C.B.17SC scid−/− female mice Dosages: 100 mg/kg Administration: i.p. |
| 参考文献: |
1. 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 Jul 10;15(7):e0235705. 2. Hariprasad V, et al. Substituted benzohydrazide analogs as histone demethylase inhibitors. WO 2017004519 A1. 3. Kurmasheva R, et al. In vivo evaluation of the lysine-specific demethylase (KDM1A/LSD1) inhibitor SP-2577 (Seclidemstat) against pediatric sarcoma preclinical models: A report from the Pediatric Preclinical Testing Consortium (PPTC). Pediatr Blood Cancer. 2021 Nov;68(11):e29304. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.218 ml |
11.088 ml |
22.176 ml |
| 5 mM |
0.444 ml |
2.218 ml |
4.435 ml |
| 10 mM |
0.222 ml |
1.109 ml |
2.218 ml |
| 50 mM |
0.044 ml |
0.222 ml |
0.444 ml |
|
| 注意: |
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