PI-273
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- CAS号:
- 925069-34-7
- 英文名:
- 2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide
- 英文别名:
- PI-273;2-(3-(4-Chlorobenzoyl)thioureido)-4-ethyl-5-methylthiophene-3-carboxamide;2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide;2-({[(4-chlorobenzoyl)amino]carbonothioyl}amino)-4-ethyl-5-methyl-3-thiophenecarboxamide;3-Thiophenecarboxamide, 2-[[[(4-chlorobenzoyl)amino]thioxomethyl]amino]-4-ethyl-5-methyl-;PI4K,Inhibitor,PI4 kinases,PI 273,PI273,Apoptosis,inhibit,Phosphatidylinositol 4 kinases,PI-273
- 中文名:
- PI-273
- 中文别名:
- 化合物PI-273;2-(3-(4-氯苯甲酰基)硫脲基)-4-乙基-5-甲基噻吩-3-甲酰胺
- CBNumber:
- CB33806116
- 分子式:
- C16H16ClN3O2S2
- 分子量:
- 381.9
- MOL File:
- 925069-34-7.mol
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PI-273化学性质
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密度:
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1.425±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 6.25 mg/mL (16.37 mM)
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酸度系数(pKa):
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8.09±0.70(Predicted)
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PI-273性质、用途与生产工艺
PI-273 是第一种可逆的和特异性磷脂酰肌醇 4-激酶 (PI4KIIα) 抑制剂，IC50 为 0.47 μM。PI-273 可以抑制乳腺癌细胞的增殖，阻断细胞周期并诱导细胞凋亡。
PI-273 (2 μM; 48 hours) blocks the cell cycle at the G2-M phase.
PI-273 (2 μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.
PI-273 (0.5-2 μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner.
PI-273 of 1 μM and 2 μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner.
Cell Cycle Analysis
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Cell Line:
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MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells
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Concentration:
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2 μM
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Incubation Time:
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48 hours
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Result:
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Blocked the cell cycle at the G2-M phase.
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Apoptosis Analysis
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Cell Line:
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MCF-7, T-47D, and SK-BR-3 cells
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Concentration:
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2 μM
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Incubation Time:
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48 hours
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Result:
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Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.
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Western Blot Analysis
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Cell Line:
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MCF-7 cells
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Concentration:
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0.5, 1, 2 μM
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Incubation Time:
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For 3 days
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Result:
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Suppressed the AKT signaling pathway in a dose- and time-dependent manner.
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PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts.
PI-273 (0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.
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Animal Model:
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Eight-week-old male BALB/c nude mice with MCF-7 cell
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Dosage:
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25 mg/kg
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Administration:
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Intraperitoneal injection; daily; 15 days
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Result:
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Suppressed the tumor volume and weight in the MCF-7 xenografts.
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Animal Model:
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Male Sprague-Dawley (SD) rats
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Dosage:
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0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically) (Pharmacokinetic Study)
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Administration:
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Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours
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Result:
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Has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.
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PI-273
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/04/30 | HY-103489 | PI-273
PI-273 | 925069-34-7 | 1mg | 800元 |
| 2024/04/30 | HY-103489 | PI-273
PI-273 | 925069-34-7 | 5mg | 1400元 |
925069-34-7, PI-273 相关搜索:
- 2-(3-(4-氯苯甲酰基)硫脲基)-4-乙基-5-甲基噻吩-3-甲酰胺
- 化合物PI-273
- 925069-34-7
- PI4K,Inhibitor,PI4 kinases,PI 273,PI273,Apoptosis,inhibit,Phosphatidylinositol 4 kinases,PI-273
- 2-(3-(4-Chlorobenzoyl)thioureido)-4-ethyl-5-methylthiophene-3-carboxamide
- 3-Thiophenecarboxamide, 2-[[[(4-chlorobenzoyl)amino]thioxomethyl]amino]-4-ethyl-5-methyl-
- PI-273
- 2-({[(4-chlorobenzoyl)amino]carbonothioyl}amino)-4-ethyl-5-methyl-3-thiophenecarboxamide
- 2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide