MPC-3100: Pan-PI3K Inhibitor for Cancer Research
MPC-3100: Pan-PI3K Inhibitor for Cancer Research
MPC-3100 is a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor investigated for its ability to suppress oncogenic PI3K signaling across multiple cancer cell models.
- Product Name
- MPC-3100
- SKU
- M734105
- Target
- Pan-Class I PI3K (PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ)
- Compound Class
- Small molecule kinase inhibitor
- Primary Application
- Oncology signal transduction research
- Recommended Storage
- Store at -20 °C, protected from light and moisture
Background: The PI3K Signaling Pathway
Phosphoinositide 3-kinases (PI3Ks) are a conserved family of lipid kinases that phosphorylate the 3-hydroxyl group of phosphoinositides, generating the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3). Class I PI3Ks, comprising the α, β, γ, and δ isoforms, are central regulators of cell growth, proliferation, survival, and metabolism. Aberrant activation of the PI3K/AKT/mTOR axis is one of the most frequently observed oncogenic alterations in human cancers, making PI3K an attractive therapeutic and research target. Inhibition of pan-class I PI3K activity enables researchers to dissect pathway contributions to tumor biology and evaluate downstream pharmacodynamic responses.
MPC-3100: Mechanism of Action
MPC-3100 functions as a pan-class I PI3K inhibitor, competitively blocking the ATP-binding pocket shared among the PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ isoforms. By preventing ATP from binding to the catalytic subunit, MPC-3100 inhibits kinase activity and consequently reduces intracellular PIP3 levels. This suppresses downstream activation of AKT and mTOR, leading to effects on cell cycle progression, protein synthesis, and apoptotic regulation. The broad isoform coverage of MPC-3100 makes it a valuable tool for studying total PI3K pathway flux rather than isoform-specific contributions.
Research Applications
MPC-3100 is principally employed in in vitro and in vivo preclinical oncology studies. Typical applications include: (1) assessment of PI3K pathway dependency in cancer cell lines via proliferation and apoptosis assays; (2) pharmacodynamic biomarker studies measuring pAKT (Ser473) and pS6K levels by immunoblot or ELISA following inhibitor treatment; (3) combination studies pairing MPC-3100 with MEK inhibitors, chemotherapy agents, or other targeted therapies to explore synergistic effects; and (4) tumor xenograft models where oral or parenteral dosing regimens are evaluated for efficacy and tolerability. Researchers in hematologic malignancy and solid tumor biology have used pan-PI3K inhibitors of this class to characterize resistance mechanisms and biomarkers of sensitivity.
Handling, Solubility, and Storage Recommendations
MPC-3100 is a small organic molecule typically supplied as a solid powder. For optimal stability, store the compound at -20 °C in a desiccated environment away from light. Stock solutions are commonly prepared in dimethyl sulfoxide (DMSO) at concentrations of 10–50 mM; vortex thoroughly and warm gently if precipitation occurs. When preparing working solutions, dilute DMSO stocks into aqueous cell culture media immediately before use to minimize compound degradation, and ensure the final DMSO concentration does not exceed 0.1% (v/v) to avoid cytotoxicity artifacts. Aliquot stock solutions to avoid repeated freeze-thaw cycles. Always consult the product-specific Certificate of Analysis (CoA) for confirmed purity, exact molecular weight, and lot-specific storage conditions before initiating experiments.
Safety and Regulatory Considerations
MPC-3100 is supplied for research use only (RUO) and is not approved for human therapeutic use. Standard laboratory safety precautions apply: wear appropriate personal protective equipment (PPE) including nitrile gloves, safety glasses, and a laboratory coat when handling. Avoid inhalation of dust or aerosols. Dispose of compound and DMSO solutions in accordance with institutional chemical waste regulations. A Safety Data Sheet (SDS) specific to this product should be consulted prior to use. As with all investigational kinase inhibitors, cytotoxic potential at high concentrations should be considered when designing dose-response experiments.
Frequently asked questions
What is the target selectivity profile of MPC-3100?
MPC-3100 is designed as a pan-class I PI3K inhibitor, targeting the α, β, γ, and δ isoforms. Researchers should consult peer-reviewed biochemical profiling data and the product CoA for confirmed IC50 values against each isoform and for selectivity data versus other kinases.
In which solvents can MPC-3100 be dissolved?
MPC-3100 is most commonly dissolved in DMSO to prepare concentrated stock solutions. Aqueous solubility may be limited; if an aqueous formulation is required, consider using a co-solvent system or cyclodextrin-based vehicle, and verify compound stability under the chosen conditions. Always confirm solubility experimentally for your specific application.
How should MPC-3100 stock solutions be stored to maintain potency?
Prepare single-use aliquots of DMSO stock solutions and store them at -20 °C in tightly sealed vials away from light and moisture. Avoid repeated freeze-thaw cycles, as these can lead to compound degradation and reduced biological activity. Discard any aliquots showing visible precipitation or discoloration.
Is MPC-3100 suitable for in vivo studies?
MPC-3100 has been investigated in preclinical in vivo settings, including tumor xenograft models. Formulation for in vivo use requires careful optimization of vehicle, dose, and administration route. Researchers should review published preclinical literature and consult institutional animal care guidelines before initiating in vivo studies with this compound.
Can MPC-3100 be used in combination with other inhibitors?
Yes, combination studies are a common application of MPC-3100 in oncology research. Pan-PI3K inhibitors have been explored in combination with MEK inhibitors, mTOR inhibitors, and cytotoxic chemotherapy agents. Synergy should be evaluated using validated methods such as the Chou-Talalay combination index assay, and appropriate vehicle controls must be included.
References
- Courtney KD, Corcoran RB, Engelman JA. The PI3K pathway as drug target in human cancer. J Clin Oncol. 2010;28(6):1075-1083. doi:10.1200/JCO.2009.25.3641
- Fruman DA, Chiu H, Hopkins BD, Bagrodia S, Cantley LC, Abraham RT. The PI3K pathway in human disease. Cell. 2017;170(4):605-635. doi:10.1016/j.cell.2017.07.029
- Aladdin Scientific. MPC-3100 Product Page, SKU M734105. Aladdin Scientific website.
Products are supplied for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
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