What Is GLUT1/EGFR-IN-1 (Compound H)?

GLUT1/EGFR-IN-1, designated compound H in the primary literature, is a rationally designed small-molecule dual inhibitor that targets two key oncogenic drivers: GLUT1 and EGFR. GLUT1 (SLC2A1) is the predominant facilitative glucose transporter overexpressed in many solid tumors, enabling the elevated glucose uptake characteristic of the Warburg effect. EGFR is a receptor tyrosine kinase whose dysregulation promotes cell proliferation, survival, and metastasis across multiple cancer types. By combining inhibitory activity against both targets in a single molecule, GLUT1/EGFR-IN-1 offers researchers a tool to study the interplay between oncogenic signaling and metabolic reprogramming.

This compound is catalogued under SKU G1419310 at Aladdin Scientific and is cross-referenced as HY-163726 in the MedChemExpress (MCE) catalog.

Biological Rationale for Dual GLUT1 and EGFR Inhibition

The co-targeting of GLUT1 and EGFR is supported by mechanistic evidence linking EGFR signaling to the upregulation of glucose metabolism. Activation of EGFR stimulates downstream pathways including PI3K/AKT/mTOR and RAS/MAPK, which transcriptionally and post-translationally enhance GLUT1 expression and membrane localization, thereby fueling glycolysis to support rapid tumor cell growth. Inhibiting EGFR alone may therefore be insufficient if the metabolic supply of glucose remains intact, and conversely, blocking GLUT1 alone may be circumvented by compensatory signaling.

A dual inhibitor addresses both axes simultaneously, potentially producing additive or synergistic antiproliferative effects, reducing the likelihood of resistance, and providing a more complete disruption of tumor bioenergetics. This strategy is of particular interest in EGFR-driven cancers such as non-small cell lung cancer (NSCLC) and certain subtypes of breast and colorectal cancers where GLUT1 overexpression has also been documented.

Recommended Handling, Storage and Solubility

As specific physicochemical data for GLUT1/EGFR-IN-1 (compound H) are not fully detailed in the current source material, the following guidance reflects general best practices for small-molecule kinase and transporter inhibitors of this class. Users should consult the Certificate of Analysis (CoA) and Safety Data Sheet (SDS) supplied with each lot for confirmed values.

• Storage: Store lyophilized or solid compound at −20°C, protected from light and moisture, in a sealed container. Stock solutions should be aliquoted to avoid freeze-thaw cycles.
• Solubility: DMSO is the recommended primary solvent for most small-molecule dual inhibitors. Prepare a concentrated stock (e.g., 10–50 mM in DMSO) and dilute into aqueous assay buffer immediately before use; keep final DMSO concentration ≤0.1% in cell-based assays to avoid cytotoxic artefacts.
• Stability: Avoid repeated freeze-thaw cycles. Short-term working solutions may be stored at 4°C for up to one week when protected from light.

Note: Confirmed solubility, molecular weight, purity, and formulation recommendations will be provided on the product CoA. Contact Aladdin Scientific technical support for lot-specific data.

Applications in Cancer Research

GLUT1/EGFR-IN-1 (compound H) is primarily intended as a research tool compound for in vitro and in vivo studies investigating the intersection of receptor tyrosine kinase signaling and cellular glucose metabolism. Key application areas include:

• Mechanistic studies: Elucidating the contribution of GLUT1-driven glycolysis to EGFR-dependent tumor cell survival and proliferation.
• Drug resistance research: Assessing whether concurrent metabolic blockade can overcome or delay resistance to EGFR-targeted monotherapies.
• Combination therapy evaluation: Comparing the efficacy of the dual inhibitor versus single-agent GLUT1 or EGFR inhibitors alone, or in combination with standard-of-care chemotherapeutics.
• Tumor model studies: Use in EGFR-overexpressing or EGFR-mutant cell lines (e.g., A431, HCC827, PC-9) and xenograft mouse models to evaluate antiproliferative and antitumor activity.

This compound is not approved for therapeutic or diagnostic use in humans or animals. It is strictly for laboratory research purposes.

Ordering and Technical Support

GLUT1/EGFR-IN-1 (compound H) is available from Aladdin Scientific under SKU G1419310. To place an order or request a quote, visit the Aladdin Scientific website or contact your regional sales representative. For bulk quantities or custom packaging, please reach out to our sales team directly.

Technical documentation including the Certificate of Analysis (CoA), Safety Data Sheet (SDS), and any available characterization data can be requested at the time of purchase or by contacting Aladdin Scientific technical support. For questions regarding experimental design, dosing recommendations, or assay compatibility, our scientific support team is available to assist.

Cross-reference: This product corresponds to MedChemExpress (MCE) catalog number HY-163726 and may be referenced as such in the primary literature.