PI-273

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PI-273  纯度: ≥98.0%

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

PI-273 Chemical Structure

CAS No. : 925069-34-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3361 In-stock
1 mg ￥800 In-stock
5 mg ￥1600 In-stock
10 mg ￥2700 In-stock
25 mg ￥5500 In-stock
50 mg ￥9000 In-stock
100 mg ￥15000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis[1].

IC50 & Target[1]

PI4KIIα

0.47 μM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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%.

分子量

381.90

Formula

C16H16ClN3O2S2
CAS 号

925069-34-7
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
溶解性数据
In Vitro: 

DMSO : 6.02 mg/mL (15.76 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Li J, et al. PI-273, a Substrate-Competitive, Specific Small-Molecule Inhibitor of PI4KIIα, Inhibits the Growth of Breast Cancer Cells. Cancer Res. 2017 Nov 15;77(22):6253-6266.

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