DABRAFENIB
Cytosine arabinoside is a nucleoside analogue interfering with DNA synthesis, used in leukemia. Side effects include bone marrow suppression and neurotoxicity.
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Product Description
Mechanism of Action
Dabrafenib is a selective inhibitor of mutant BRAF serine‑threonine kinase, particularly BRAF V600E/K. By binding the ATP pocket, it blocks aberrant MAPK/ERK signalling in tumour cells carrying these mutations, reducing proliferation and promoting apoptosis. It has limited activity on wild‑type BRAF at therapeutic concentrations.
Benefits and Advantages
Used in oncogenic‑MAPK pathway research, BRAF‑mutant tumour modelling, kinase‑inhibitor SAR studies, resistance‑mechanism analysis (e.g., MEK reactivation, NRAS mutations), and combination therapy research (e.g., with MEK inhibitors).
Side Effects and Risks
Risks include cutaneous squamous‑cell carcinomas, pyrexia, arthralgia, cardiomyopathy, uveitis and hepatotoxicity. Handle as a potent targeted kinase inhibitor with cytotoxic precautions.
Datasheet
| Molecular Formula | C23H20F2N4O2S2 |
|---|---|
| Molecular Weight | 519.6 g/mol |
| CAS Number | 1195765-45-7 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | very slightly soluble at pH 1 |
| Purity | Purity information is available upon request (COA). |
| Synonym | Dabrafenib; 1195765-45-7; GSK2118436A; GSK-2118436; QGP4HA4G1B |
| IUPAC/Chemical Name | N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide |
| InChl Key | BFSMGDJOXZAERB-UHFFFAOYSA-N |
| InChl Code | InChI=1S/C23H20F3N5O2S2/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25/h4-11,31H,1-3H3,(H2,27,28,29) |
| References |
3D Conformer.
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