S2116|2262489-89-2|-陌孚医药/Medlife

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S2116

目录号: PL15086 纯度: ≥98%

CAS No. :2262489-89-2

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中文名称	S2116
英文名称	S2116
英文别名	Ethanone, 1-[(3S)-3-amino-1-pyrrolidinyl]-2-[[(1R,2S)-2-[3,5-difluoro-2-(phenylmethoxy)phenyl]cyclopropyl]amino]-, hydrochloride (1:1);S2116
Cas No.	2262489-89-2
分子式	C₂₂H₂₆ClF₂N₃O₂
分子量	437.91
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	S2116 是 N-烷基化的反式环丙胺 (TCP) 衍生物，是一种有效的赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂。S2116 在超级增强子区域增加 H3K9 甲基化和相应的 H3K27 脱乙酰化。S2116 抑制 NOTCH3 和 TAL1 基因的转录，从而诱导 TCP 抵抗性急性淋巴细胞白血病 T-ALL 细胞凋亡 (apoptosis)。S2116 显着延迟异种移植小鼠中 T-ALL 细胞的生长。
生物活性	S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
性状	Solid
IC50 & Target[1][2]	LSD1
体外研究(In Vitro)	S2116 is particularly effective for T-ALL cell lines with the IC50 values between 1.1 μM for human T-ALL cell lines CEM and 6.8 μM for MOLT4. S2116 (4-20 μM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes. S2116 (4-8 μM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-ALL cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	S2116 (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. S2116 (50 mg/kg; IP) has a T 1/2 of 3.76 hours, a C max of 12.7 μM and an AUC of 59.2 μM?h. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Shiori Saito, et al. Eradication of Central Nervous System Leukemia of T-Cell Origin With a Brain-Permeable LSD1 Inhibitor. Clin Cancer Res. 2019 Mar 1;25(5):1601-1611.

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