1309444-75-4
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- CAS号:
- 1309444-75-4
- 英文名:
- K145
- 英文别名:
- K145;K145,K-145;K145 ，K145 HCl salt;3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione;2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-
- 中文名:
- 1309444-75-4
- 中文别名:
- 化合物 T11739
- CBNumber:
- CB92677052
- 分子式:
- C18H24N2O3S
- 分子量:
- 348.46
- MOL File:
- 1309444-75-4.mol
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1309444-75-4化学性质
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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1309444-75-4性质、用途与生产工艺
K145 是一种选择性的，具有底物竞争性和口服活性的 SphK2 抑制剂，IC50 为 4.3 µM，Ki 为 6.4 µM。K145 对 SphK1 和其他蛋白激酶没有活性。K145 可诱导细胞凋亡，并具有强大的抗肿瘤活性。
IC50: 4.3 µM (SphK2)
Ki: 6.4 µM (SphK2)
K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner.
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells.
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt.
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels.
Cell Viability Assay
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Cell Line:
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U937 cells
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Concentration:
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0 µM, 4 µM, 6 µM, 8 µM, 10 µM
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Incubation Time:
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24 hours, 48 hours, 72 hours
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Result:
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Significantly inhibited the growth of U937 cells in a concentration-dependent manner.
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Apoptosis Analysis
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Cell Line:
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U937 cells
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Concentration:
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10 µM
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Incubation Time:
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24 hours
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Result:
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Significantly induced apoptosis in U937 cells.
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Western Blot Analysis
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Cell Line:
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U937 cells
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Concentration:
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4 µM, 8 µM
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Incubation Time:
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3 hours
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Result:
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Phosphorylated ERK and Akt were decreased.
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K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice.
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Animal Model:
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BALB/c-nu mice injected with U937 cells
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Dosage:
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50 mg/kg
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Administration:
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Oral gavage; daily; for 15 days
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Result:
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Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
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1309444-75-4
上下游产品信息
上游原料
下游产品
1309444-75-4, 1309444-75-4 相关搜索:
- 化合物 T11739
- 1309444-75-4
- K145,K-145
- K145 ，K145 HCl salt
- 2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-
- 3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione
- K145