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JAB-8263 is a highly potent, selective, orally bioavailable small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, including BRD2, BRD3, BRD4, and BRDT. By inhibiting BET proteins—key epigenetic regulators that control the expression of oncogenes such as c-MYC—JAB-8263 disrupts chromatin modeling and gene expression patterns critical for tumor cell growth. This leads to downregulation of MYC transcription and subsequent inhibition of tumor proliferation in both hematological malignancies and solid tumors. Preclinical studies have demonstrated strong anti-tumor activity at very low concentrations with favorable safety profiles. JAB-8263 is being developed by Jacobio Pharma for indications including myelofibrosis, acute myeloid leukemia (AML), small-cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), esophageal squamous cell carcinoma (ESCC), hormone-refractory prostate cancer, ovarian cancer, colorectal cancer (CRC), and other solid tumors.
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