S2157|cas:2262488-39-9|西域试剂

S2157,98.44%

产品编号：Bellancom-136523| CAS NO：2262488-39-9| 分子式：C₂₃H₂₈ClF₂N₃O₂| 分子量：451.94

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-136523		￥8500.00	杭州北京（现货）
Bellancom-136523		￥13800.00	杭州北京（现货）

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S2157

产品介绍

S2157 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。S2157 在超级增强子区域增加 H3K9 甲基化和相应的 H3K27 脱乙酰化。S2157 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)。S2157 有效地透过血脑屏障，几乎可以完全根除 T-ALL 细胞移植小鼠的中枢神经系统白血病。

生物活性

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.

体外研究

S2157 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.
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.

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)

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.

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 0.88 hours, a C_max of 4.33 μM and an AUC of 5.75 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 0.88 hours, a C_max of 4.33 μM and an AUC of 5.75 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 0.88 hours, a C_max of 4.33 μM and an AUC of 5.75 μM•h.