SB590885

Catalog No.S2220

SB590885 Chemical Structure

Molecular Weight(MW): 453.54

SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 170 In stock
USD 670 In stock
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2 Customer Reviews

  • Western blotting of the indicated proteins in WM266-4 cells treated for 48 h with 1 μM of BRAF (PLX4032 or SB590885) or MEK (AZD6244 or AS703026) inhibitors.

    Oncotarget, 2015, 6(17):15250-64.. SB590885 purchased from Selleck.

    Cell morphology of BCPAP, K1 and 8505C cells treated and untreated with SB590885 using IC50 dose. Massive vacuolization is easily visible around the nuclei in treated cells.

    Invest New Drugs 2014 32(4), 626-35. SB590885 purchased from Selleck.

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Biological Activity

Description SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
Features Displays significant selectivity for B-Raf over c-Raf.
Targets
B-Raf [1]
(Cell-free assay)
0.16 nM(Ki)
In vitro

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. [1] SB590885 displays high affinity for B-Raf with Kd of 0.3 nM. [2] 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. [3]

In vivo Administration of SB590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth. [1]

Protocol

Cell Research:[1]
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  • Cell lines: Colo205, HT29, A375P, SKMEL28, and MALME-3M
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female nude mice injected s.c. with of A375P cells
  • Formulation: Dissolved in vehicle [2% N,N-dimethylacetamide, 2% Cremophor EL, and 96% acidified water (pH f4-5)]
  • Dosages: 50 mg/kg/day
  • Administration: Injection i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL (11.02 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 453.54
Formula

C27H27N5O2

CAS No. 405554-55-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID