Regorafenib

Regorafenib Monohydrate is an oral multikinase inhibitor developed by Bayer, approved for the treatment of metastatic colorectal cancer (mCRC), gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC). As a potent kinase inhibitor, Regorafenib Monohydrate blocks the activity of multiple protein kinases involved in tumor angiogenesis, oncogenesis, and the tumor microenvironment. Regorafenib Monohydrate undergoes enterohepatic circulation with multiple plasma concentration peaks observed across the 24-hour dosing interval . The main circulating metabolites of Regorafenib Monohydrate—M-2 (N-oxide) and M-5 (N-oxide and N-desmethyl)—have similar in vitro pharmacological activity as the parent compound . Regorafenib Monohydrate and its related impurities serve as critical reference standards for analytical method development, method validation (AMV), and quality control (QC) in ANDA filings.

Product Parameters

Why Cosperpharm?

When your multi-kinase inhibitor manufacturing campaign or ANDA filing requires high-quality Regorafenib Monohydrate and impurity reference standards, Cosperpharm delivers with the analytical depth and supply reliability that pharmaceutical customers demand.

Multi-kinase inhibition requires precise control. The urea-linked phenoxypicolinamide scaffold of Regorafenib Monohydrate targets nine distinct kinases. Any impurity or degradation product will compromise the delicate balance of kinase inhibition. Our analytical release protocol includes HPLC purity verification (>98%), residual solvent analysis, and identity confirmation—because your final API's multi-target activity depends on the integrity of this molecule.

Documentation for regulatory submission. Every shipment includes a Certificate of Analysis (COA) with batch-specific HPLC purity and chromatographic traceability. DMF-ready documentation and custom quality agreements are available.

Flexible supply for all development stages. Cosperpharm supplies Regorafenib Monohydrate from gram-scale R&D quantities to kilogram-scale batches. R&D samples ship within 5–7 business days.

Technical support for kinase inhibitor chemistry. Our process chemistry team can advise on urea formation, phenoxy coupling, and analytical methods for detecting process-related impurities.

Bioactivity

Regorafenib (BAY-734506, Fluorosolafenib, Resihance, Stivarga) monohydrate is a novel oral multi-kinase inhibitor, and its half-maximal inhibitory concentrations against vascular endothelial growth factor receptor 1, mouse vascular endothelial growth factor receptor 2 Chemicalbook, mouse vascular endothelial growth factor receptor 3, platelet-derived growth factor receptor-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF (V600E) are 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nanomolar respectively.

Product Quality Assurance

Cosperpharm has established a comprehensive quality assurance system for Regorafenib Monohydrate:

Thorough analytical characterization. Each batch undergoes HPLC purity verification (>98%), appearance verification, residual solvent analysis, and identity confirmation .

Full batch traceability. From raw material procurement through final packaging, every step is fully documented and traceable.

Stability monitoring program. Cosperpharm conducts ongoing stability studies under recommended storage conditions.

Documentation ready for regulatory submission. Every shipment includes a Certificate of Analysis (COA), SDS, and customs documentation. DMF-ready documentation and custom quality agreements are available.

Contact Us

Need Regorafenib Monohydrate for your multi-kinase inhibitor manufacturing, impurity profiling, or cancer research? Cosperpharm is your trusted partner for high-quality kinase inhibitor intermediates and reference standards. Contact our team today—we're ready to support your project.