S2116|cas:2262489-89-2|西域试剂

S2116,98.15%

产品编号：Bellancom-136522| CAS NO：2262489-89-2| 分子式：C₂₂H₂₆ClF₂N₃O₂| 分子量：437.91

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-136522		￥7500.00	杭州北京（现货）
Bellancom-136522		￥12000.00	杭州北京（现货）

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S2116

产品介绍

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell 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 Analysis

Cell 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 Analysis

Cell 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.

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.

西域 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 3.76 hours, a C_max of 12.7 μM and an AUC of 59.2 μM•h.

体内研究

西域 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 3.76 hours, a C_max of 12.7 μM and an AUC of 59.2 μM•h.

体内研究

西域 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 3.76 hours, a C_max of 12.7 μM and an AUC of 59.2 μM•h.