REGN-10597
REGN-10597, composed of an anti-huPD-1-targeting antibody and IL2Ra-IL2 moiety, is a PD-1-dependent IL-2 agonist. REGN-10597 binds PD-1 to deliver masked native IL-2 to PD-1+ T cells, engaging trimeric IL-2 receptors to activate downstream signaling. REGN-10597 can be used for the research on melanoma, prostate cancer, colorectal cancer, and ovarian cancer.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Human
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IL-2 |
REGN-10597 (Serial dilutions; 30 min at 4°C) shows minimal binding to PD-1-knockout IL-2Rβ/γ+ and IL-2Rα/β/γ+ YT/STAT5-Luc reporter cells, with slightly enhanced binding to IL-2Rα-expressing cells[1].
REGN-10597 (4.5 h) exhibits PD-1-targeting-dependent IL-2 agonist activity in IL-2Rβ/γ+ YT/STAT5-Luc reporter cells, with enhanced potency correlating with increased PD-1 expression[1].
REGN-10597 (20 min) selectively enhances STAT5 phosphorylation in primary human PD-1+ CD8+ T cells compared to PD-1− CD8+ T cells, demonstrating PD-1-targeted IL-2 activity[1].
REGN-10597 (72 h) potently enhances primary human T cell activation in a mixed lymphocyte reaction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
REGN-10597 (0.5 mg/kg; i.p.; every 3-4 days; 3 total doses)-mediated anti-tumor activity in MC38 tumor-bearing human PD-1 knockin mice is strictly dependent on CD8+ T cells, with pre-existing intratumoral CD8+ T cells playing a more significant role than newly recruited T cells[1].
REGN-10597 (0.5 mg/kg; i.p.) achieves 80% complete tumor regression and long-term survival in MC38 tumor-bearing human PD-1 knockin mice[1].
REGN-10597 (1.5 mg/kg; i.p.) induces significant tumor growth inhibition and 25% complete tumor regression in B16F10 melanoma-bearing human PD-1 knockin mice[1].
REGN-10597 (1.5 mg/kg; i.p.) induces significant tumor growth inhibition and 25% complete tumor regression in MCA205 fibrosarcoma-bearing human PD-1 knockin mice[1].
REGN-10597 treatment induces long-term anti-tumor memory, protecting MC38 tumor-cured human PD-1 knockin mice from tumor rechallenge[1].
REGN-10597 (0.5 mg/kg; i.p.; two doses on days 10 and 13 post-tumor engraftment) expands intratumoral PD-1+ CD8+ T cells with diverse effector and progenitor profiles, driving clonally expanded tumor-reactive T cell responses in MC38 tumor-bearing human PD-1 knockin mice[1].
REGN-10597 (0.5 mg/kg; i.p.; two doses on days 0 and 3) selectively expands PD-1+ CD8+ T cells in the peripheral blood of MC38 tumor-bearing human PD-1 knockin mice, demonstrating targeted activity[1].
REGN-10597 (1.8 mg/kg; i.p.; daily; 4 total doses) exhibits reduced systemic toxicity in healthy human PD-1 knockin mice, causing no significant body weight loss or pulmonary edema with daily dosing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:0.2 mg/kg
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Administration:i.p.; single dose
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Result:Triggered efficient tumor growth control, with 8 out of 10 mice undergoing tumor regression within the first week of treatment.
Led to relapse in 6 out of 8 initial responders, leaving 2 out of 10 mice with complete tumor regression and long-term survival.
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:0.5 mg/kg
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Administration:i.p.; every 3-4 days; 3 total doses
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Result:Had its tumor growth inhibition and tumor-free survival completely abrogated by depletion of CD8+ T cells.
Showed no effect change with depletion of CD4+ T cells or NK cells.
Retained most anti-tumor activity when T cell egress from lymph nodes was blocked with FTY720.
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:0.5 mg/kg
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Administration:i.p.
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Result:Showed far superior potency in inhibiting tumor growth and improving tumor-free survival compared to non-targeting NT-IL2Ra-IL2, anti-PD-1 blocker, or their combination.
Led to 8 out of 10 mice achieving complete tumor regression and long-term survival.
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:1.5 mg/kg
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Administration:i.p.
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Result:Significantly inhibited tumor growth, with 2 out of 8 mice achieving complete tumor regression.
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:1.5 mg/kg
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Administration:i.p.
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Result:Significantly inhibited tumor growth, with 2 out of 8 mice achieving complete tumor regression.
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:0.5 mg/kg
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Administration:i.p.; two doses on days 10 and 13 post-tumor engraftment
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Result:Led to pronounced expansion of intratumoral T cell populations, reducing myeloid populations.
Specifically expanded multiple PD-1+ CD8+ T cell clusters with robust effector gene expression (Gzma, Prf1, Ifng), proliferative activity, and clonal expansion indicative of tumor antigen recognition.
Enriched a subset of stem-like progenitor CD8+ T cells (TCF1+ PD-1+).
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:0.5 mg/kg
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Administration:i.p.; two doses on days 0 and 3
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Result:Led to selective expansion of PD-1+ CD8+ T cells in peripheral blood, with minimal effect on PD-1- CD8+ T cells.
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Animal Model:Human PD-1 knockin mice (female, 8-16 weeks old)[2]
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Dosage:1.8 mg/kg
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Administration:i.p.; daily; 4 total doses
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Result:Did not result in significant body weight loss or increased pulmonary wet weight (a marker of pulmonary edema), indicating reduced systemic toxicity compared to unmasked IL-2 molecules.
PDCD1/PD-1/CD279
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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anti-PD-1/IL-2Ra/IL-2 fusion protein
ELISA, FACS, Functional assay
Chemical Information
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Wu J, et al. A PD-1-targeted, receptor-masked IL-2 immunocytokine that engages IL-2Rα strengthens T cell-mediated anti-tumor therapies. Cell Rep Med. 2024 Oct 15;5(10):101747. [Content Brief]
[2]. Pousse L, et al. Advanced cytokine-based immunotherapies: targeted cis-delivery strategies for enhanced anti-tumor efficacy and reduced toxicity. MAbs. 2025;17(1):2590250. [Content Brief]
[3]. Li S, et al. Synergistic potential of PD-1 blockade and IL-2 in cancer therapy via targeted bi-functional molecule design. Sci Bull (Beijing). 2025 Aug 11:S2095-9273(25)00809-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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