PI-273
Based on 9 publication(s) in Google Scholar
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.
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- 純度: 98.47%
- CAS 番号: 925069-34-7
- 分子式: C16H16ClN3O2S2
- 分子量:381.90
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 PI-273
More- Cell Metab. 2025 Dec 17:S1550-4131(25)00495-4. [Abstract]
- Nat Commun. 2023 Oct 28;14(1):6883. [Abstract]
- J Clin Invest. 2023 Apr 3;133(7):e165863. [Abstract]
- Cell Rep. 2023 Jun 13;42(6):112633. [Abstract]
- Sci Rep. 2025 Aug 21;15(1):30805. [Abstract]
- University of Miami. 2026.
- SSRN. 2025 Sep 23.
- University of Pennsylvania. 2024.
- bioRxiv. 2023 Feb 23.
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IF
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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ELISA
生物活性
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PI4KIIα 0.47 μM (IC50) |
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.
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Cell Line:MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells
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Concentration:2 μM
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Incubation Time:48 hours
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Result:Blocked the cell cycle at the G2-M phase.
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Cell Line:MCF-7, T-47D, and SK-BR-3 cells
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Concentration:2 μM
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Incubation Time:48 hours
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Result:Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.
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Cell Line:MCF-7 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:For 3 days
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Result:Suppressed the AKT signaling pathway in a dose- and time-dependent manner.
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.
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Animal Model:Eight-week-old male BALB/c nude mice with MCF-7 cell[1]
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Dosage:25 mg/kg
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Administration:Intraperitoneal injection; daily; 15 days
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Result:Suppressed the tumor volume and weight in the MCF-7 xenografts.
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Animal Model:Male Sprague-Dawley (SD) rats[1]
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Dosage:0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically) (Pharmacokinetic Study)
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Administration:Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours
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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%.
化学情報
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CAS 番号 925069-34-7
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性状 Solid
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分子量 381.90
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分子式 C16H16ClN3O2S2
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Color Light yellow to yellow
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SMILES
O=C(C1=C(NC(NC(C2=CC=C(Cl)C=C2)=O)=S)SC(C)=C1CC)N
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Metab
Serotonin-licensed macrophages potentiate chemoresistance via inositol metabolic crosstalk in ovarian cancer. [Abstract]2025 Dec 17:S1550-4131(25)00495-4. PMID: 41412121 -
Nat Commun
A phosphoinositide switch mediates exocyst recruitment to multivesicular endosomes for exosome secretion. [Abstract]2023 Oct 28;14(1):6883. PMID: 37898620
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: Nat Commun. 2023 Oct 28;14(1):6883. [Abstract]
Immunoblotting of PDL1 in the whole cell lysates and exosomes from DMSO or PI-273 (2 μM) treated cells.
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J Clin Invest
EMT-activated secretory and endocytic vesicular trafficking programs underlie a vulnerability to PI4K2A antagonism in lung cancer. [Abstract]2023 Apr 3;133(7):e165863. PMID: 36757799
PI-273 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Apr 3;133(7):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 MedChemExpress. Usage Cited in: J Clin Invest. 2023 Apr 3;133(7):e165863. [Abstract]
PI-273 (25 mg/kg; ip; daily for 2-4 weeks) decreased tumor weight and tumor size.
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Cell Rep
Phosphatidylinositol 4-kinase IIα is a glycogen synthase kinase 3-regulated interaction hub for activity-dependent bulk endocytosis. [Abstract]2023 Jun 13;42(6):112633. PMID: 37314927 -
Sci Rep
2025 Aug 21;15(1):30805. PMID: 40841827 -
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PI-273 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 23.
Effect of PI4KIIα (PI-273, 2 µM) and PI4KIIIα (10 nM, GSK-A1) inhibition on HA-NL-CD63 secretion under basal and bafilomycin-induced conditions.
溶剤 & 溶解度
DMSO : 5 mg/mL (13.09 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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (699 KB)
- English - EN (699 KB)
- Français - FR (699 KB)
- Deutsch - DE (699 KB)
- Norwegian - NO (699 KB)
- Español - ES (699 KB)
- Swedish - SV (699 KB)
- Italian - IT (699 KB)
- Korean - KR (699 KB)
- Portuguese - PT (699 KB)
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取扱説明書 (2659 KB)
参考文献
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 |