SB273005

製品コードS7540 バッチS754002

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C22H24F3N3O4

分子量 451.44 CAS No. 205678-31-5
Solubility (25°C)* 体外 DMSO 90 mg/mL warmed with 50ºC water bath (199.36 mM)
Ethanol 10 mg/mL warmed with 50ºC water bath (22.15 mM)
Water Insoluble
* <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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 A375 cells
濃度 100 nM
反応時間
実験の流れ
動物実験 動物モデル Thyroidectomized−parathyroidectomized (TPTx) rat model of bone resorption, and ovariectomized (Ovx) rat model of osteoporosis
投薬量 30 mg/kg
投与方法 p.o.

カスタマーフィードバック

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

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

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
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
Cell clusters adopt a collective amoeboid mode of migration in confined nonadhesive environments [ Sci Adv, 2022, 8(39):eabp8416] PubMed: 36179021

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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