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    Dabrafenib (GSK2118436)
    Dabrafenib (GSK2118436)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1004
    CAS #: 1195765-45-7 Purity ≥98%

    Description: Dabrafenib (formerly known as GSK2118436; GSK-2118436; GSK-2118436A; GSK-2118436B. Trade name: Tafinlar) is a novel, specific, orally bioavailable inhibitor of BRAF V600 mutants with potential anticancer activity. It inhibits BRAF V600 with an IC50 of 0.8 nM in cell-free assays and is 4- and 6-fold less potent against B-Raf (wildype) and c-Raf, respectively. Dabrafenib potently inhibits BRAF V600 mutants such as 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. Dabrafenib FDA gained approval in 2013 to treat melanoma.

    References: Arch Pharm Res. 2011 May;34(5):699-701.

    Related CAS#: 1195768-06-9 (mesylate)

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    Molecular Weight (MW)519.56
    CAS No.1195765-45-7(free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 30 mg/mL (57.74 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 8 mg/mL
    SynonymsGSK2118436A; GSK-2118436B; GSK 2118436A; GSK2118436B (Dabrafenib Mesylate ); GSK-2118436A; GSK 2118436B. Trade name: Tafinlar.

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    GeneralDabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice.
    Animal modelA375P cells were implanted subcutaneously in female CD1 nu/nu mice and grown to form tumors [1]; Dabrafenib (orally gavage) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice [2].
    FormulationDissolved in 0.5% hydroxypropylmethylcellulose, 0.2% Tween 80 in pH 8.0 distilled water
    Dosages10, 30, and 100 mg/kg
    AdministrationAdministered orally once daily
    Reference[1] PLoS One. 2013; 8(7): e67583; [2] Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Dabrafenib (GSK2118436)

    Dabrafenib inhibits MAPK signalling in BRAFV600E cells and is abrogated by ARAF or CRAF depletion. PLoS One. 2013; 8(7): e67583.

    Dabrafenib (GSK2118436)

    Modulation of pharmacodynamic markers by dabrafenib in BRAFV600E tumors.

    Dabrafenib (GSK2118436)

    Inhibition of BRAFV600E tumor xenograft growth by dabrafenib.


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