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Lucicebtide is a peptide antagonist of the transcription factor C/EBPβ, a key activator of the transcriptional program in immunosuppressive macrophages. In immunocompetent, macrophage-rich triple-negative breast and colorectal cancer models, lucicebtide induces repolarization of tumor-associated macrophages (TAMs) to a pro-inflammatory M1-like phenotype and suppresses tumor growth. Lucicebtide synergizes with anti-PD-1 therapy and overcomes resistance to checkpoint inhibition in anti-PD-1-refractory tumors, but in vivo responses are impaired by systemic macrophage depletion, indicating that macrophage reprogramming is integral to lucicebtide activity. Lucicebtide induces cell cycle arrest in cancer cells with IC50 of 18.56 and 15.32 uM agianst KCL008 (Her2+/ER-/PR-) and KCL012 (Her2-/ER-/PR-) breast cancer cells, shows no effect against normal human mammary epithelial cells (HMECs). Lucicebtide (50 mg/kg three times per week for three weeks by subcutaneous (SC) injection) caused durable tumor regressions in mice bearing U251 GBM subcutaneous xenograft.
| Molecular Weight | 4724.46 |
| CAS Number | 2407100-74-5 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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