1. PI3K/Akt/mTOR Apoptosis
  2. PI4K Apoptosis
  3. PI-273

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

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PI-273 Chemical Structure

PI-273 Chemical Structure

CAS No. : 925069-34-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1540
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1 mg ¥800
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5 mg ¥1400
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10 mg ¥2200
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25 mg ¥3800
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50 mg ¥5500
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Customer Review

    PI-273 purchased from MCE. Usage Cited in: J Clin Invest. 2023 Feb 9;e165863.  [Abstract]

    PI-273 (25 mg/kg/day; i.p.; 2-4 weeks) inhibits growth of lung tumors in nu/nu mice.

    PI-273 purchased from MCE. Usage Cited in: Nat Commun. 2023 Oct 28;14(1):6883.  [Abstract]

    PI-273 (2 μM; 24, 48 h) causes a significant shift in PD-L1 distribution from Rab11-positive structures to LAMP1 lysosomes.

    查看 PI4K 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    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].

    MCE 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].

    MCE 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
    性状

    固体

    颜色

    Light yellow to yellow

    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 6.02 mg/mL (15.76 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    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
    查看完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: ≥98.0%

    参考文献

    完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6185 mL 13.0924 mL 26.1849 mL 65.4622 mL
    5 mM 0.5237 mL 2.6185 mL 5.2370 mL 13.0924 mL
    10 mM 0.2618 mL 1.3092 mL 2.6185 mL 6.5462 mL
    15 mM 0.1746 mL 0.8728 mL 1.7457 mL 4.3641 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    产品名称:
    PI-273
    目录号:
    HY-103489
    需求量: