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Background: Galunisertib, or LY2157299 monohydrate) is a highly potent and selective inhibitor of TGF-β (transforming growth factor β) receptor I kinase that binds to the ATP-binding site of the protein. The TGF-β superfamily is critical for the development of cells and tissues, and their continued homeostasis. In the context of cancer, TGF-β signaling plays a protective role in the early stages of the disease, but as promoter at later stages, which abnormal signaling being implicated in glioblastoma, breast cancer and others. Targeting this pathway has thus gained interest in oncology. Galunisertib was shown to inhibit tumor growth in animal models of cancer, but exposure in the long term resulted in cardiac toxicity. It is currently being studied in a phase Ib/II clinical trial for the treatment of solid tumors and NSCLC (non-small cell lung cancer) in combination with nivolumab, a monoclonal antibody that blocks PD-1 (programmed cell death 1).
CAS Number: 700874-72-2
Description: Galunisertib is a TGF-β kinase (ALK5) antagonist.
Purity: ≥98% by NMR
Storage Stability: Upon receipt, store at -20°C. Stable for 1 year from date of receipt, when stored as directed. Solutions are stable for up to 1 month at -20°C.
Supplied As: Solid
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Nadal E., et al., 2023 BMC Cancer 23:708.
Yingling J., et al., 2018 Oncotarget 9(6):6659-6677.
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