All AbMole products are for research use only, cannot be used for human consumption.
SB-590885 is a selective small-molecule inhibitor of the B-Raf kinase and Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively. SB590885 has been used to overcome the dependence of MAPK signaling and tumor cell growth on BRaf kinase activity. In melanoma and colorectal cancer cell lines with B-Raf V600E mutation, an effective inhibition of cell proliferation was achieved at concentrations that blocked ERK phosphorylation. The inhibition of MAP kinase is one of the vital ways to get rid of un-wanted tumor growth. SB590885 also act as an angiogenesis inhibitor and also helps in the research studies of different important kinase pathways.
 |
Source | J Cell Mol Med (2015). Figure 2. SB590885 |
| Method | MTT assay | |
| Cell Lines | TT cells | |
| Concentrations | 0.01–100 μM | |
| Incubation Time | 72 hrs | |
| Results | RAF265 was the most effective compound, showing an IC50 = 0.09 μM, while SB590885 showed an IC50 = 3.36 μM, and ZSTK474 an IC50 = 0.59 μM |
| Cell Experiment | |
|---|---|
| Cell lines | Colo205, HT-1080, HT-29, A395p and SK-MEL28 cells line |
| Preparation method | Cellular assays. For proliferation assays, cells were treated with compounds in 0.1% DMSO and incubated for 72 hours at 37°C, 5% CO2. Viable cells were quantified using CellTiter-Glo reagent (Promega, Madison, WI) and luminescence detection on a Victor 2V plate reader (Perkin-Elmer, Turku, Finland). Cells were prepared for cell cycle analysis on a Becton Dickinson FACScan, according to the manufacturer's instructions. Data was acquired and analyzed using CellQuest v3.3 software. Anchorage-independent growth assays were done as described elsewhere ( 6), with inhibitors or DMSO vehicle included in the agar layer. Cultures were re-fed with media and inhibitor or DMSO every 5 to 7 days for a total of 28 days. Colonies were visualized and photographed by conventional light microscopy and quantified by counting on a grid in triplicate. |
| Concentrations | 0.1, 1 and 10 μ M |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | A375P xenograft model |
| Formulation | 2% N,N-dimethylacetamide, 2% Cremophor EL, and 96% acidified water (pH ∼4-5) |
| Dosages | 50 mg/kg daily for 21 days |
| Administration | i.p. |
| Molecular Weight | 453.54 |
| Formula | C27H27N5O2 |
| CAS Number | 405554-55-4 |
| Solubility (25°C) | DMSO 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Raf Products |
|---|
| GDC-0879
GDC-0879 is a potent and selective B-Raf kinase inhibitor with an EC50 of 0.75 µM. |
| Vemurafenib (PLX4032)
Vemurafenib (PLX4032) is a first-in-class, potent, selective inhibitor of B-Raf that inhibits RAFV600E and C-RAF-1 activity with IC50s of 31 nM and 48 nM, respectively.In addition, Vemurafenib induces autophagy. |
| PLX-4720
PLX-4720 is a selective BRAFV600E inhibitor with the IC50 values of 160 nM and 130 nM for B-Raf and BRK respectively. |
| ZM 336372
ZM 336372 is a potent, selective ATP-competitive inhibitor of c-Raf in vitro (IC50 = 70 nM for inhibition of human c-Raf). |
| Dabrafenib Mesylate
Dabrafenib (GSK2118436) is a selective, orally bioavailable inhibitor of Mutant B-raf (BRAF) protein kinase with potential antineoplastic activity. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
