SB590885

SKU: orb1305771

Description

SB590885 is a potent and selective B-Raf inhibitor with a Ki of 0.16 nM, demonstrating approximately 11-fold selectivity over c-Raf. This small molecule is a valuable research tool for investigating the RAF/MEK/ERK signaling pathway in both cellular and biochemical assays, supporting cancer research and targeted therapy development.

Research Area

Signal Transduction

Key Properties

• CAS Number: 405554-55-4
• MW: 453.5
• Purity: 99.06% (May vary between batches)
• Formula: C₂₇H₂₇N₅O₂
• SMILES: CN(C)CCOc1ccc(cc1)-c1nc(c([nH]1)-c1ccncc1)-c1ccc2\C(CCc2c1)=N\O
• Target: Kinase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.41 mM);DMSO:12.5 mg/mL (27.56 mM)

Bioactivity

• Target IC50:
  B-Raf:0.16 nM(Ki)|C-Raf:1.72 nM (Ki)
• 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).
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• 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

B-Raf, inhibit, Inhibitor, SB590885, SB-590885, SB 590885, Raf kinases, Raf

Compound Identifiers

PubChem CID

135421339