计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells
In Vitro
S2157 is particularly effective for T-ALL cell lines with the IC 50 values between 1.1 µM for human T-ALL cell lines CEM and 6.8 µM for MOLT4. S2157 (4-20 µM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes. S2157 (4-8 µM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Normal T-lymphocytes Concentration: 4, 8, 12, 16, 20 µM Incubation Time: For 72 hours Result: Modestly inhibited mitogen-activated normal T-lymphocytes. Apoptosis AnalysisCell Line: T-cell acute lymphoblastic leukemia (T-ALL) cells Concentration: 4, 6, 8 µM Incubation Time: For 24 hours Result: Induced apoptosis, as evidenced by increased annexin-V reactivity on flow cytometry in T-ALL cells in a dose- and time-dependent manner without affecting cell cycle distribution. Western Blot AnalysisCell Line: T-ALL cells Concentration: 4, 6, 8 µM Incubation Time: For 24 hours Result: Down-regulated the expression of NOTCH3 and TAL1 proteins in T-ALL cells.
In Vivo
S2157 (50 mg/kg; IP; 3 times a week; for 28 days) causes the size of subcutaneous tumors reduced to less than 20% of that in the untreated control . S2157 (50 mg/kg; IP) has a T 1/2 of 0.88 hours, a C max of 4.33 μM and an AUC of 5.75 μM•h . S2157 (30 mg/kg or 50 mg/kg; twice a week for 3 weeks) almost completely suppressed the growth of MOLT4 cells in most but not all NOD/SCID mice with MOLT4 cells. S2157 eradicates CNS leukemia in murine xenotransplanted models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice with MOLT4 cells Dosage: 50 mg/kg Administration: IP; 3 times a week; for 28 days Result: The size of subcutaneous tumors reduced to less than 20% of that in the untreated control. Animal Model: 8-week-old ICR mice Dosage: 50 mg/kg (Pharmacokinetic Analysis) Administration: IP Result: Had a T 1/2 of 0.88 hours, a C max of 4.33 μM and an AUC of 5.75 μM•h.
Form:Solid
IC50& Target:LSD1
规格
规格或纯度
≥98%
英文名称
S2157
生化机理
S2157是一种N-烷基化氨酰环丙胺（TCP）衍生物，是一种强效的赖氨酸特异性去甲基化酶1（LSD1）抑制剂。S2157 可增加超级增强子区域的 H3K9 甲基化和相互的 H3K27 去乙酰化。S2157 可诱导 TCP 抗性 T-ce 细胞凋亡。
储存条件
2-8°C储存,干燥
运输条件
低温运输
纯度
≥98%
名称和识别符
分子类型
小分子
Smiles
[H]Cl.CN1CCN(C(CN[C@H]2[C@H](C3=CC(F)=CC(F)=C3OCC4=CC=CC=C4)C2)=O)CC1.[Relative stereochemistry]
分子量
451.94
技术文档
高级数据
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溶液计算器
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