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    SB590885
    SB590885

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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 #: V1008
    CAS #: 405554-55-4Purity ≥98%

    Description: SB590885 (SB 590885; SB-590885) is a novel and potent B-Raf inhibitor with potential antineoplastic activity. It inhibits B-Raf with a Ki of 0.16 nM in a cell-free assay, and exhibits a 11-fold higher selectivity for B-Raf over c-Raf. It does not inhibit other closely related kinases. It is found that SB590885 binds to B-Raf within the ATP-binding pocket and stabilizes the active conformation of B-Raf. SB590885 decreases the phosphorylation of ERK and shows anti-proliferation only in tumor cells expressing oncogenic B-Raf V600E. Malignant cells expressing oncogenic B-Raf show selective inhibition of mitogen-activated protein kinase activation, proliferation, transformation, and tumorigenicity when exposed to SB-590885 , whereas other cancer cell lines and normal cells display variable sensitivities or resistance to similar treatment.

    References: Cancer Res. 2006 Dec 1;66(23):11100-5; Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81.

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    Molecular Weight (MW)453.54
    FormulaC27H27N5O2
    CAS No.405554-55-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 5 mg/mL (11.0 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0: 30mg/mL
    SynonymsSB590885; SB590885; SB 590885


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    In Vitro

    In vitro activity: SB590885 displays significant selectivity for B-Raf over c-Raf with Ki of 0.16 nM over 1.72 nM. SB-590885 is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (Ki = 38 nM for mutant B-Raf, 6 nM for c-Raf). SB590885 displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, SB590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-RafV600E, SB590885 treatment potently inhibits ERK phosphorylation with EC50 of 28 nM, 58 nM, 290 nM, 58 nM, and 190 nM, respectively, and consistently, inhibits the proliferation with EC50 of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM, respectively. SB590885 decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner. SB590885 displays high affinity for B-Raf with Kd of 0.3 nM. Most of the melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4 mutations (451Lu, WM35, and WM983) are highly sensitive to SB590885 with IC50 of<1 μM. Increased levels of cyclin D1 resulting from genomic amplification mediate SB590885 resistance in B-Raf V600E-mutated melanomas.


    Kinase Assay: SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.


    Cell Assay: Cells are treated with increasing concentrations of SB590885 and incubated for 72 hours. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for cell cycle analysis on a Becton Dickinson FACScan. Data is acquired and analyzed using CellQuest v3.3 software.

    In VivoAdministration of SB590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth.
    Animal modelFemale nude mice injected s.c. with of A375P cells
    Formulation & DosageDissolved in vehicle [2% N,N-dimethylacetamide, 2% Cremophor EL, and 96% acidified water (pH f4-5)]; 50 mg/kg; i.p. injection
    ReferencesCancer Res. 2006 Dec 1;66(23):11100-5; Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81.


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

    SB590885

    Overexpression of cyclin D1 reduces sensitivity to the BRAF inhibitor SB590885.  2008 Sep;7(9):2876-83.

    SB590885

    Identification of human melanoma samples and a cell line with high levels of cyclin D1 (CCND1) amplification. A, DNA copy number profiles of chromosome 11 for melanoma tumor samples TB2668F1, TB2673F1, and the melanoma cell line WM39.  2008 Sep;7(9):2876-83.

    SB590885

    Melanoma cell lines with CDK4 mutations are not resistant to SB590885. A, melanoma cell lines with a CDK4 mutation (WM39, WM46, SK-Mel-28, WM902B, WM793, and 1205Lu: red, open symbols) and melanoma lines without CDK4 mutations (WM983, WM164, and 451Lu; blue, closed symbols) were treated with increasing concentrations of SB590885 (1 nmol/L – 10 μmol/L) for 72 h before being treated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide.  2008 Sep;7(9):2876-83.


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