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Specifications of Dabrafenib丨CAS 1195765-45-7
|
Appearance |
Off-white solid |
|
Purity |
99% min |
|
Content |
99.0% min |
|
Identification |
The nuclear magnetic resonance data of this product should be consistent with the literature |
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Moisture |
1.0% max |
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Regarding impurities |
1.0% max |
Chemical Overview:
Dabrafenib丨CAS 1195765-45-7 is a small-molecule, orally bioavailable inhibitor of the BRAF V600E kinase, a mutant form of the BRAF protein commonly associated with certain types of cancer. It belongs to the class of targeted cancer therapies known as kinase inhibitors. Dabrafenib is marketed under the trade name Tafinlar®, usually in combination with other agents such as trametinib.
Applications
Targeted Cancer Therapy
Dabrafenib is FDA- and EMA-approved for the treatment of various cancers characterized by BRAF V600 mutations, including:
Melanoma: For unresectable or metastatic melanoma with BRAF V600E mutation (often used in combination with trametinib).
Non-Small Cell Lung Cancer (NSCLC): For metastatic NSCLC with BRAF V600E mutation.
Anaplastic Thyroid Cancer (ATC): For rare, aggressive cases harboring BRAF mutations.
Low-Grade Glioma (Pediatric use): Approved for BRAF V600E mutation-positive tumors.
Combination Therapy with Trametinib
Dabrafenib is frequently used alongside trametinib, a MEK inhibitor, to enhance therapeutic efficacy and reduce resistance. This dual blockade of the MAPK/ERK pathway results in more sustained tumor control.
Research and Drug Development
Dabrafenib is used in preclinical and clinical research to study:
Mechanisms of drug resistance in cancer.
Signal transduction in the RAS-RAF-MEK-ERK pathway.
Synergistic effects with immunotherapies and other targeted agents.
Benefits
Selective and Potent Inhibition
Dabrafenib丨CAS 1195765-45-7 selectively targets the mutated BRAF V600E kinase, allowing for precision therapy that minimizes off-target effects compared to conventional chemotherapy.
Improved Progression-Free Survival
In clinical trials, dabrafenib has shown significant improvements in progression-free survival and overall survival for patients with BRAF-mutant melanoma, especially in combination with trametinib.
Oral Administration
Dabrafenib is administered orally, offering a convenient and non-invasive treatment option for patients.
Reduced Side Effects Compared to Chemotherapy
As a targeted therapy, dabrafenib typically has a more favorable safety profile than traditional chemotherapy, with side effects more often limited to skin rash, fever, and fatigue.
Expanded Use in Pediatric Oncology
Its approval for pediatric low-grade glioma highlights dabrafenib's evolving role in personalized medicine for children with genetically defined cancers.
Pathway-Specific Cancer Suppression
By targeting the MAPK/ERK pathway, dabrafenib not only inhibits tumor growth but also helps prevent cancer cell survival and metastasis in BRAF-mutant tumors.
Summary
Dabrafenib丨CAS 1195765-45-7 is a potent and selective BRAF inhibitor used in the treatment of multiple BRAF V600E mutation-positive cancers, including melanoma, NSCLC, and anaplastic thyroid cancer. As a cornerstone of modern targeted therapy, especially in combination with trametinib, dabrafenib offers improved clinical outcomes, manageable toxicity, and convenient oral dosing. It represents a paradigm shift toward precision oncology, targeting the genetic drivers of cancer.
