Name: Dabrafenib (GSK2118436)
Price: 188.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Dabrafenib is a specific inhibitor of BRAF V600 mutants with IC50 values of 0.5nM, 0.6nM and 1.9nM against V600E, V600K and V600D, respectively [1].
    BRAF plays a central role in regulating MAPK signaling pathway which regulates cell growth, division and differentiation. The V600E mutation of BRAF increases the kinase activity and is involved in metastatic melanomas. Dabrafenib is an ATP-competitive and reversible inhibitor of BRAF mutants. It potently inhibits BRAFV600E, BRAFV600K and BRAFV600D with IC50 values of 0.5nM, 0.6nM and 1.9nM, respectively. Dabrafenib is currently approved by FDA and is widely used in cancer patients harboring BRAF mutations. It is reported that treatment of dabrafenib shrinks the overall size of brain metastases in patients. It also has an impressive 60% response rate for melanomas outside of the brain. Dabrafenib provides a significant survival benefit in patients with metastatic melanoma [1, 2].
    
    [1] Hong S, Hong S. Overcoming metastatic melanoma with BRAF inhibitors. Archives of pharmacal research, 2011, 34(5): 699-701.
    [2] Hong D S, Vence L, Falchook G, et al. BRAF (V600) inhibitor GSK2118436 targeted inhibition of mutant BRAF in cancer patients does not impair overall immune competency. Clinical Cancer Research, 2012, 18(8): 2326-2335.
- Properties
  - Alternative Name
    
    N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
    
    CAS Number
    
    1195765-45-7
    
    Molecular Formula
    
    C23H20F3N5O2S2
    
    Molecular Weight
    
    519.56
    
    Appearance
    
    A solid
    
    Purity
    
    99.63%
    
    Solubility
    
    ≥26 mg/mL in DMSO; insoluble in H2O; ≥2.59 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Yina Liao, Yao Gao, et al. "Melatonin synergizes BRAF-targeting agent dabrafenib for the treatment of anaplastic thyroid cancer by inhibiting AKT/hTERT signalling." J Cell Mol Med. 2020 Sep 15. PMID:32935463
    2. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID:30038713
    3. Azimi A, Caramuta S, et al. "Targeting CDK2 overcomes melanoma resistance against BRAF and Hsp90 inhibitors." Mol Syst Biol. 2018 Mar 5;14(3):e7858. PMID:29507054
    4. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID:29249695

Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436)

Background

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