Active Pharmaceutical Ingredients

Catalog ID80019293

CAS NO.284461-73-0

Purity 99%

MDL NumberMFCD06411450

Molecular Formula C21H16ClF3N4O3

Molecular Weight 464.83

Melting point: 225~235°C

Category	Details
Chemical Properties	Sorafenib is a kinase inhibitor with the molecular formula C21H16ClF3N4O3 and a molecular weight of 471.82. It is a white to off-white powder.
Physical Properties	Melting point: Not explicitly mentioned in the provided data.
Solubility	Solubility information is not explicitly mentioned in the provided data.
Pharmacological Effects	Sorafenib decreases tumor cell proliferation in vitro and attenuates tumor growth in various cancer models, including hepatocellular carcinoma, renal cell carcinoma, and differentiated thyroid carcinoma. It also inhibits tumor angiogenesis and increases tumor apoptosis. Additionally, sorafenib has been shown to inhibit hepatitis C viral replication in vitro.
Mechanism of Action	Sorafenib inhibits multiple intracellular serine/threonine kinases in the Ras/mitogen-activated protein kinase (MAPK) signal transduction pathway, including Raf-1, wild-type B-Raf, and mutant B-Raf. It also inhibits cell surface tyrosine kinase receptors such as KIT, FLT-3, RET, VEGFR-1, VEGFR-2, VEGFR-3, and PDGFR-β. Its dual mechanism of action involves blocking tumor proliferation by inhibiting the RAF/MEK/ERK pathway and reducing tumor angiogenesis by inhibiting VEGFR and PDGFR signaling.
Metabolism and Elimination	Sorafenib is primarily metabolized in the liver by CYP3A4 and undergoes glucuronidation by UGT1A9. The main circulating metabolite is the pyridine N-oxide form, which comprises approximately 9–16% of the total circulating dose at steady-state and has similar pharmacological activity to the parent drug. It is excreted mainly in feces (77%) and urine (19%) as glucuronidated metabolites. The half-life of sorafenib is 25–48 hours.
Therapeutic Uses	Sorafenib is FDA-approved for the treatment of renal cell carcinoma and hepatocellular carcinoma. It is also used in combination with other targeted therapies and chemotherapies for various cancers.
Safety and Precautions	Sorafenib can cause adverse effects such as cutaneous squamous cell carcinoma/keratoacanthomas in 5%–10% of patients. It may also cause hyperbilirubinemia, which is related to genetic polymorphisms in UGT1A1 and UGT1A9.
Storage Conditions	Store in a cool, dry place, protected from light and moisture.

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