Name: SB273005
Brand: Selleck Chemicals
SKU: S7540
Availability: InStock
Rating: 5 (27 reviews)

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Quality Control

Batch: Purity: 99.59%

99.59

Related Targets	Akt Wnt/beta-catenin HSP PKC ROCK Microtubule Associated Bcr-Abl Actin FAK Kinesin
Other Integrin Inhibitors	Cilengitide trifluoroacetate Cilengitide (EMD 121974) RGD peptide (Arg-Gly-Asp) ATN-161 Cyclo(RGDyK) TFA Cyclo(-RGDfK) TFA Leukadherin-1 A-205804 OSU-T315 Pyrintegrin

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
HEK 293 cells	Function assay	Inhibition of Vitronectin receptor, integrin alphaV-beta3 expressed in HEK 293 cells, IC50=0.00015 μM	12477347
HEK	Function assay	HEK cell adhesion mediated by alpha v beta 3 integrin, IC50 = 0.003 μM.	10633035
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 16 mg/mL

Water : 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.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (9.97mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.11mM)
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	451.44	Formula	C₂₂H₂₄F₃N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	205678-31-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CNC1=CC=CC(=N1)CCOC2=CC3=C(CC(C(=O)N(C3)CC(F)(F)F)CC(=O)O)C=C2

Mechanism of Action

Targets/IC₅₀/Ki	αvβ5 receptor (Cell-free assay) 0.3 nM αvβ3 receptor (Cell-free assay) 1.2 nM
In vitro	In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. In blood containing MDA-MB-231 cells, a combination of this compound and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM).
Kinase Assay	Binding assay
Kinase Assay	Binding affinity for human αvβ3 and αvβ5 is determined in a competitive binding assay employing 3H-SK&F 107260 as the displaced ligand. The Ki values represent the means of values determined in two to three separate experiments.
In vivo	In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. In rat with adjuvant-induced arthritis, this compound (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. This compound (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. In pregnant mice, this compound reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10633035/ [2] https://pubmed.ncbi.nlm.nih.gov/11212150/ [3] https://pubmed.ncbi.nlm.nih.gov/15679053/ [4] https://pubmed.ncbi.nlm.nih.gov/18098042/ [5] https://pubmed.ncbi.nlm.nih.gov/24926365/ [6] https://pubmed.ncbi.nlm.nih.gov/36229674/

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Handling Instructions

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SB273005 Integrin inhibitor

Chemical Structure

Molecular Weight: 451.44