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Basic Info
CAS Number
N/A
Pharmacopoeia
ChP
Grade
In-house Standards
Is Manufacturer
YES
Packaging & Delivery
Minimum Order Quantity
Any
Delivery Cycle
Negotiable
Product Description
Reference Standards &Impurity
AI Product Description
*The following content is generated by AI and is for reference only.
Galunisertib, also known as LY2157299 monohydrate, is a potent and selective small-molecule inhibitor targeting the Type I receptor of transforming growth factor-beta (TGF-β), specifically TGF-βRI (ALK5). Its molecular formula is C30H41N7O4, and it carries the CAS Registry Number 1226855-56-6. As a first-in-class therapeutic agent, Galunisertib functions by blocking the phosphorylation of Smad2 and Smad3 proteins, thereby inhibiting the canonical TGF-β signaling pathway. This mechanism is critical because TGF-β plays a dual role in cancer biology; while it acts as a tumor suppressor in early stages, it promotes tumor progression, metastasis, immune evasion, and fibrosis in advanced malignancies. Consequently, inhibiting this pathway offers a promising strategy to halt cancer spread and sensitize tumors to other therapies.
Clinically, Galunisertib has been extensively investigated in phase II trials for various solid tumors, including pancreatic ductal adenocarcinoma, non-small cell lung cancer, hepatocellular carcinoma, and glioblastoma. Notably, significant interest surrounds its potential in combination with standard-of-care treatments. Research indicates that Galunisertib can enhance the efficacy of chemotherapy agents like gemcitabine or immunotherapies such as PD-L1 inhibitors by modulating the tumor microenvironment, reducing stromal density, and reversing T-cell suppression. In preclinical models, the drug has demonstrated the ability to inhibit liver metastasis and improve survival rates when used alongside conventional therapies. Although the development of Galunisertib has faced challenges regarding optimal dosing and patient selection across different indications, it remains a valuable tool in oncology research for understanding TGF-β biology. Its unique pharmacological profile continues to drive exploration in combination regimens aimed at overcoming resistance mechanisms and improving clinical outcomes for patients with refractory cancers.
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