Name: SB590885
Brand: Selleck Chemicals
SKU: S2220
Availability: InStock
Rating: 5 (42 reviews)

Jump to

Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	ERK p38 MAPK K-Ras JNK MEK Ras S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Other Raf Products	LY3009120 GDC-0879 Avutometinib (Ro 5126766) Exarafenib PLX-4720 AZ 628 TAK-632 RAF265 (CHIR-265) GW5074 PLX7904

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (11.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2% Cremophor EL 1 2% N 2 N-dimethylacetamide 3 pH 5.0 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (66.15mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	453.54	Formula	C₂₇H₂₇N₅O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	405554-55-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN(C)CCOC1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC5=C(C=C4)C(=NO)CC5

Mechanism of Action

Features	Displays significant selectivity for B-Raf over c-Raf.
Targets/IC₅₀/Ki	B-Raf (Cell-free assay) 0.16 nM(Ki)
In vitro	SB590885 displays significant selectivity for B-Raf over c-Raf with K_i of 0.16 nM over 1.72 nM. This compound is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (K_i = 38 nM for mutant B-Raf, 6 nM for c-Raf). It displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, this chemical stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-RafV600E, this compound 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. It decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner. This chemical displays high affinity for B-Raf with Kd of 0.3 nM. Most of the melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4 mutations (451Lu, WM35, and WM983) are highly sensitive to this compound with IC50 of <1 μM. Increased levels of cyclin D1 resulting from genomic amplification mediate this compound resistance in B-Raf V600E-mutated melanomas.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17145850/ [2] https://pubmed.ncbi.nlm.nih.gov/16260133/ [3] https://pubmed.ncbi.nlm.nih.gov/18790768/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-MEK / MEK / p-ERK / ERK		25879420

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

SB590885 B-Raf inhibitor

Chemical Structure

Molecular Weight: 453.54