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  3. PI-273

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.

For research use only. We do not sell to patients.

PI-273 Chemical Structure

PI-273 Chemical Structure

CAS No. : 925069-34-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 336 In-stock
Solution
10 mM * 1 mL in DMSO USD 336 In-stock
Solid
1 mg USD 80 In-stock
5 mg USD 160 In-stock
10 mg USD 270 In-stock
25 mg USD 550 In-stock
50 mg USD 900 In-stock
100 mg USD 1500 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PI-273 purchased from MedChemExpress. 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.

    PI-273 purchased from MedChemExpress. 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.

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    Description

    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)

    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].

    MedChemExpress (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.
    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].

    MedChemExpress (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%.
    Molecular Weight

    381.90

    Formula

    C16H16ClN3O2S2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=C(NC(NC(C2=CC=C(Cl)C=C2)=O)=S)SC(C)=C1CC)N

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 6.02 mg/mL (15.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    In Vivo Dissolution Calculator
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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: ≥98.0%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    • 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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    Product Name:
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    Cat. No.:
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