SB273005

Catalog No.S7540 Batch:S754001

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Technical Data

Formula

C22H24F3N3O4
Molecular Weight 451.44 CAS No. 205678-31-5
Solubility (25°C)* In vitro DMSO 90 mg/mL (199.36 mM)
Ethanol 16 mg/mL (35.44 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
0.5mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.5mg/ml
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
Targets
αvβ5 receptor [1]
(Cell-free assay)		 αvβ3 receptor [1]
(Cell-free assay)
0.3 nM 1.2 nM
In vitro

In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. [1]

In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). [3]
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. [1]

In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. [2]

SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. [4]

In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels. [5]

Protocol (from reference)

Kinase Assay:

[1]
  • Binding 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.
Animal Study:

[1]
  • Animal Models

    Thyroidectomized−parathyroidectomized (TPTx) rat model of bone resorption, and ovariectomized (Ovx) rat model of osteoporosis

  • Dosages

    30 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Int J Oncol, 2017, 50(5):1899-1914]

Selleck's SB273005 has been cited by 27 publications

A synergistic regulation works in matrix stiffness-driven invadopodia formation in HCC [ Cancer Lett, 2024, 582:216597] PubMed: 38145655
Epigenetic suppression of PGC1α (PPARGC1A) causes collateral sensitivity to HMGCR-inhibitors within BRAF-treatment resistant melanomas [ Nat Commun, 2023, 14(1):3251] PubMed: 37277330
Irisin reduces amyloid-β by inducing the release of neprilysin from astrocytes following downregulation of ERK-STAT3 signaling [ Neuron, 2023, S0896-6273(23)00623-2] PubMed: 37689059
Graphene-based 3D-Printed nanocomposite bioelectronics for monitoring breast cancer cell adhesion [ Biosens Bioelectron, 2023, 226:115113] PubMed: 36764127
E-cadherin Force Transmission and Stiffness Sensing [ ODU Digital Commons , 2023, 30426293] PubMed: none
Loss of NECTIN1 triggers melanoma dissemination upon local IGF1 depletion [ Nat Genet, 2022, 10.1038/s41588-022-01191-z] PubMed: 36229674
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
CCN1 interacts with integrins to regulate intestinal stem cell proliferation and differentiation [ Nat Commun, 2022, 13(1):3117] PubMed: 35660741
ITGβ6 Facilitates Skeletal Muscle Development by Maintaining the Properties and Cytoskeleton Stability of Satellite Cells [ Life (Basel), 2022, 12(7)926] PubMed: 35888016

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.