产品
编 号：F715289
分子式：C22H26ClF2N3O2
分子量：437.91
分子式：C22H26ClF2N3O2
分子量：437.91
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规格
价格
是否有货
1mg
询价
询价
5mg
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询价
10mg
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CAS No: 2262489-89-2
产品详情
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.
体内研究：
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 T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM?h. 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 T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM?h.
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.
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.
体内研究：
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 T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM?h. 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 T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM?h.
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.
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