PI-273
| 中文名称 | PI-273 |
|---|---|
| 中文同义词 | 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;化合物PI-273,10 MM DMSO 溶液;PI-273 ,E2374;PI-273 试剂;PI-273 试剂 |
| 英文名称 | 2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide |
| 英文同义词 | 2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide;2-({[(4-chlorobenzoyl)amino]carbonothioyl}amino)-4-ethyl-5-methyl-3-thiophenecarboxamide;PI-273;3-Thiophenecarboxamide, 2-[[[(4-chlorobenzoyl)amino]thioxomethyl]amino]-4-ethyl-5-methyl-;2-(3-(4-Chlorobenzoyl)thioureido)-4-ethyl-5-methylthiophene-3-carboxamide;PI4K,Inhibitor,PI4 kinases,PI 273,PI273,Apoptosis,inhibit,Phosphatidylinositol 4 kinases,PI-273;PI-273, 10 mM in DMSO;2-({[(4-Chlorophenyl)carbonyl]carbamothioyl}amino)-4-ethyl-5-methylthiophene-3-carboxamide |
| CAS号 | 925069-34-7 |
| 分子式 | C16H16ClN3O2S2 |
| 分子量 | 381.9 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 925069-34-7.mol |
| 结构式 |  |
PI-273 性质
| 密度 | 1.425±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：6.25 mg/mL（16.37 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.09±0.70(Predicted) |
| 颜色 | 浅黄至黄色 |
|
PI4KIIα 0.47 μM (IC 50 ) |
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
| Cell Line: | MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells |
| Concentration: | 2 μM |
| Incubation Time: | 48 hours |
| Result: | Blocked the cell cycle at the G2-M phase. |
Apoptosis Analysis
| Cell Line: | MCF-7, T-47D, and SK-BR-3 cells |
| Concentration: | 2 μM |
| Incubation Time: | 48 hours |
| Result: | Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3. |
Western Blot Analysis
| Cell Line: | MCF-7 cells |
| Concentration: | 0.5, 1, 2 μM |
| Incubation Time: | For 3 days |
| Result: | Suppressed the AKT signaling pathway in a dose- and time-dependent manner. |
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%.
| Animal Model: | Eight-week-old male BALB/c nude mice with MCF-7 cell |
| Dosage: | 25 mg/kg |
| Administration: | Intraperitoneal injection; daily; 15 days |
| Result: | Suppressed the tumor volume and weight in the MCF-7 xenografts. |
| Animal Model: | Male Sprague-Dawley (SD) rats |
| Dosage: | 0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically) (Pharmacokinetic Study) |
| Administration: | Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours |
| Result: | 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%. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-103489 | PI-273 PI-273 | 925069-34-7 | 1mg | 480元 |
| 2025/12/22 | HY-103489 | PI-273 PI-273 | 925069-34-7 | 5mg | 1120元 |