Home MAPK Raf inhibitor SB590885 For research use only.

SB590885

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.

SB590885 Chemical Structure

SB590885 Chemical Structure

CAS: 405554-55-4

Selleck's SB590885 has been cited by 39 publications

Purity & Quality Control

Batch: Purity: 99.91%
99.91

SB590885 Related Products

Signaling Pathway

Raf Signaling Pathways

Raf Signaling Pathway

Choose Selective Raf Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 Function assay Binding affinity to human N-His6-tagged B-Raf expressed in Sf9 cells, Kd=0.00016μM 22024030
white blood cells Antifibrotic assay 25 to 150 mg/kg 13 days Antifibrotic activity in bleomycin-induced C57B1/6 mouse model assessed as inhibition of white blood cells in bronchoalveolar lavage at 25 to 150 mg/kg, po bid administered 2 hrs prior bleomycin induction for 13 days 22222036
insect cells Function assay 30 mins Inhibition of full length human 6His-tagged BRAF V600E mutant expressed in baculovirus infected insect cells co-expressing human CDC37 (1 to 378 residues) using MEK1 as substrate after 30 mins, IC50=0.00016μM 29461827
A549 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A549 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
Colo205 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human Colo205 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
HT-29 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human HT-29 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
MALME3M Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human MALME3M cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
SKMEL28 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human SKMEL28 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
A375 Function assay Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50=0.29μM 22808911
A375 Function assay Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by immunoblot analysis, IC50=0.29μM 29461827
A375 Antiproliferative assay Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50=0.37μM 22808911
A375 Cytotoxicity assay 48 hrs Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 48 hrs by CellTiter-Glo assay, IC50=0.37μM 29461827
HFF Function assay 60 mins Inhibition of B-Raf-mediated Erk phosphorylation in human HFF cells after 60 mins by Western blot analysis, EC50=1.1μM 22222036
HMEC Function assay 60 mins Inhibition of B-Raf-mediated Erk phosphorylation in human HMEC cells after 60 mins by Western blot analysis, EC50=1.1μM 22222036
PREC Function assay 60 mins Inhibition of B-Raf-mediated Erk phosphorylation in human PREC cells after 60 mins by Western blot analysis, EC50=1.1μM 22222036
HCT116 Growth inhibition assay 72 hrs Growth inhibition of human HCT116 cells expressing wild-type B-Raf and K-Ras2 G13D mutant after 72 hrs by WST-1 assay, EC50=1.1μM 22222036
SK-MEL-2 Growth inhibition assay 72 hrs Growth inhibition of human SK-MEL-2 cells expressing wild-type B-Raf and N-Ras2 Q61R mutant after 72 hrs by WST-1 assay, EC50=1.1μM 22222036
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant, IC50=4.6μM 22808911
Click to View More Cell Line Experimental Data

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
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-MEK / MEK / p-ERK / ERK 25879420
In Vivo
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]
Animal Research Animal Models Female nude mice injected s.c. with of A375P cells
Dosages 50 mg/kg/day
Administration Injection i.p.

Chemical Information & Solubility

Molecular Weight 453.54 Formula

C27H27N5O2
CAS No. 405554-55-4 SDF Download SB590885 SDF
Smiles CN(C)CCOC1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC5=C(C=C4)C(=NO)CC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (11.02 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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