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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $36 | In Stock | In Stock | |
| 5 mg | $85 | In Stock | In Stock | |
| 10 mg | $133 | In Stock | In Stock | |
| 25 mg | $268 | In Stock | In Stock | |
| 50 mg | $513 | In Stock | - | |
| 100 mg | $747 | In Stock | - | |
| 1 mL x 10 mM (in DMSO) | $148 | In Stock | In Stock |
| 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. |
| Targets&IC50 | B-Raf:0.16 nM(Ki), C-Raf:1.72 nM (Ki) |
| 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). |
| 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) |
| Molecular Weight | 453.54 |
| Formula | C27H27N5O2 |
| Cas No. | 405554-55-4 |
| Smiles | CN(C)CCOc1ccc(cc1)-c1nc(c([nH]1)-c1ccncc1)-c1ccc2\C(CCc2c1)=N\O |
| Relative Density. | 1.27 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 12.5 mg/mL (27.56 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.41 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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