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。
| 生物活性 | PI-273 is a first reversibly and specificphosphatidylinositol 4-kinase (PI4KIIα)inhibitor with anIC50of 0.47 μM. PI-273 can inhibit breastcancercell proliferation, block the cell cycle and induce cellapoptosis[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | PI-273 (2 μM; 48 hours) blocks the cell cycle at the G2-M phase[1].
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[1].
PI-273 (0.5-2 μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner[1].
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[1].
Cell Cycle Analysis[1] | 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[1] | 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[1] | 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. |
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体内研究
(In Vivo) | PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts[1].
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%[1].
| Animal Model: | Eight-week-old male BALB/c nude mice with MCF-7 cell[1] | | 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[1] | | 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%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 6.02 mg/mL(15.76 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.6185 mL | 13.0924 mL | 26.1849 mL | | 5 mM | 0.5237 mL | 2.6185 mL | 5.2370 mL | | 10 mM | 0.2618 mL | 1.3092 mL | 2.6185 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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