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

PI-273 

Cat. No.: HY-103489
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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

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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].

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].

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.

925069-34-7

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PI-273PI273PI 273PI4KApoptosisPhosphatidylinositol 4 kinasesPI4 kinasesInhibitorinhibitorinhibit

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