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Regorafenib
    Publish time 2024-10-17 17:09    

CAS Number: 755037-03-7

Regorafenib

Basic Information

  • Product Name: Regorafenib

  • CAS Number: 755037-03-7

  • Chemical Formula: C21H15ClF4N4O3

  • Molecular Weight: 482.82 g/mol

  • Appearance: White powder (which translates to a light pink oval film-coated tablet in Chinese)

  • Purity: Typically very high, such as 99.9%

Chemical Properties

  • Structure: Regorafenib has a specific chemical structure that targets multiple kinases involved in tumor growth.

  • Mechanism of Action: Regorafenib inhibits the activity of various tyrosine kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFR-β, Kit, RET, and Raf-1, thereby inhibiting tumor angiogenesis, cell proliferation, and tumor microenvironment signaling.

Biological Activity

  • Antitumor Activity: Regorafenib demonstrates antitumor activity in multiple types of cancer, including colorectal cancer, gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC).

  • Preclinical Studies: Preclinical studies have shown that Regorafenib can inhibit tumor growth and prolong survival in animal models.

Applications

  • Therapeutic Use: Regorafenib is indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluorouracil, oxaliplatin, and irinotecan, as well as anti-VEGF and anti-EGFR therapies (if KRAS wild-type). It is also indicated for patients with locally advanced, inoperable, or metastatic GIST who have been previously treated with imatinib and sunitinib. Additionally, it is used for the treatment of HCC in patients who have previously received sorafenib therapy.

  • Research Use: Regorafenib is also used in scientific research to study its mechanisms of action, antitumor activity, and interactions with other drugs or biological systems.