Cat. No.: HY-103489

PI-273

9 Cited Publications

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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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Pureté: 98.47%
CAS No.: 925069-34-7
Formule: C₁₆H₁₆ClN₃O₂S₂
Masse moléculaire:381.90

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PI-273 Chemical Structure

CAS No.: 925069-34-7

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PI4KIIα

0.47 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform PI4K :

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%.

Chemical Information

CAS No. 925069-34-7
Appearance Solid
Masse moléculaire 381.90
Formule C₁₆H₁₆ClN₃O₂S₂
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

All ELISACell Proliferation/Viability AssayIn Vivo Efficacy StudyIFWB

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Journal Impact Factor

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.
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.
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

Dynamic assessment of PI4P metabolism using split GFP based sensors. [Abstract]

2025 Aug 21;15(1):30805. PMID: 40841827
University of Miami

2026.
SSRN

2025 Sep 23.
University of Pennsylvania

2024.
bioRxiv

2023 Feb 23.

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.

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PI-273

9 Cited Publications

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PI-273

Apoptosis Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PI-273

Voir tous les produits spécifiques à Isoform PI4K

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PI-273

Apoptosis Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PI-273

Voir tous les produits spécifiques à Isoform PI4K

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PI-273 Related Classifications

HY-103489 Related Classifications