| Name | SB-590885 |
| Description | SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to other human kinases. |
| Cell Research | 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) |
| In vitro | In mice with A375P melanoma xenografts that express the B-Raf(V600E) variant, SB590885 significantly reduces tumor incidence and exhibits a certain inhibitory effect on tumor growth. |
| In vivo | SB590885 effectively inhibits ERK phosphorylation (EC50: 28/58/290/58/190 nM) and proliferation (EC50: 0.1/0.87/0.37/0.12/0.15 μM) in Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing the carcinogenic B-RafV600E. Compared to c-Raf (Ki: 1.72 nM), SB590885 displays significantly higher selectivity for B-Raf (Ki: 0.16 nM). Unlike the multikinase inhibitor BAY43-9006, SB590885 stabilizes the active conformation of the oncogenic B-Raf kinase domain and shows a high affinity for B-Raf (Kd: 0.3 nM). Melanoma cell lines with the BRAF V600E mutation but without the CDK4 mutation (451Lu, WM983, and WM35) are highly sensitive to SB590885 (IC50 <1 μM). |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.41 mM), Sonication is recommended.
DMSO : 12.5 mg/mL (27.56 mM), Sonication is recommended.
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| Keywords | SB-590885 | SB590885 | SB 590885 | Raf kinases | Raf | Inhibitor | inhibit | B-Raf |
| Inhibitors Related | Regorafenib monohydrate | Exarafenib | Doramapimod | Vemurafenib | Sulindac sulfide | Sorafenib | Regorafenib | Dabrafenib | Dabrafenib Mesylate | LY3009120 | GW 441756 | RMC-7977 |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Active Compound Library |
United States
