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SCH 527123

CXCR1 and CXCR2 receptors antagonist CAS# 473727-83-2

SCH 527123

Catalog No. BCC1932----Order now to get a substantial discount!

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Chemical structure

SCH 527123

3D structure

Chemical Properties of SCH 527123

Cas No. 473727-83-2 SDF Download SDF
PubChem ID 9865554 Appearance Powder
Formula C21H23N3O5 M.Wt 397.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 50 mg/mL (125.81 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobuten-1-yl]amino]benzamide
SMILES CCC(C1=CC=C(O1)C)NC2=C(C(=O)C2=O)NC3=CC=CC(=C3O)C(=O)N(C)C
Standard InChIKey RXIUEIPPLAFSDF-CYBMUJFWSA-N
Standard InChI InChI=1S/C21H23N3O5/c1-5-13(15-10-9-11(2)29-15)22-16-17(20(27)19(16)26)23-14-8-6-7-12(18(14)25)21(28)24(3)4/h6-10,13,22-23,25H,5H2,1-4H3/t13-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SCH 527123

DescriptionSCH-527123 is a potent antagonist of both CXCR1 and CXCR2 with IC50 values of 42 nM and 3 nM, respectively.
TargetsCXCR1CXCR2    
IC5042 nM3 nM    

Protocol

Cell experiment[1]:

Cell lines

Human melanoma cell line (A375SM )

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

1 μg/ml, 72h

Applications

SCH-479833 or SCH 527123 inhibited the melanoma cell proliferation, chemotaxis, and invasive potentialin vitro.Treatment of melanoma cells with SCH-479833 or SCH 527123 also inhibited tumor growth. Histologic and histochemical analyses showed significant (P<0.05) decreases in tumor cell proliferation and microvessel density in tumors. Moreover, we observed a significant increase in melanoma cell apoptosis in SCH-479833- or SCH 527123-treated animals compared with controls.

Animal experiment[1]:

Animal models

Male BALB/c mice, 20-25 g

Dosage form

Sch-527123 was suspended in 0.4% methylcellulose

Application

Sch 527123 was bound with high affinity to the CXCR2 receptors of mouse (Kd=0.20 nM), rat (Kd=0.20 nM), and cynomolgus monkey (Kd=0.08 nM) and was a potent antagonist of CXCR2-mediated chemotaxis (IC50~3– 6 nM). In contrast, Sch 527123 bound to cynomolgus CXCR1 with lesser affinity (Kd=41 nM) and weakly inhibited cynomolgus CXCR1-mediated chemotaxis (IC50 ~1000 nM). Oral treatment with Sch-527123 blocked pulmonary neutrophilia (ED50=1.2 mg/kg) and goblet cell hyperplasia (32–38% inhibition at 1–3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Sch-527123 suppressed the pulmonary neutrophilia (ED=501.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED 50≤ 0.1 mg/kg) induced by intratracheal (i.t.) LPS. Sch-527123 also suppressed the pulmonary neutrophilia (ED50=1.3 mg/kg), goblet cell hyperplasia (ED 50=0.7 mg/kg), and increase in BAL mucin content (ED50<1 mg/kg) in rats after i.t. administration of vanadium pentoxide. In cynomolgus monkeys, Sch-527123 reduced the pulmonary neutrophilia induced by repeat bronchoscopy and lavage (ED50=0.3 mg/kg).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Singh S1, Sadanandam A, Nannuru KC et al. Small-molecule antagonists for CXCR2 and CXCR1 inhibit human melanoma growth by decreasing tumor cell proliferation, survival, and angiogenesis. Clin Cancer Res. 2009 Apr 1;15(7):2380-6.

2. Chapman RW1, Minnicozzi M, Celly CS et al. A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation. J Pharmacol Exp Ther. 2007 Aug;322(2):486-93. Epub 2007 May 11.

SCH 527123 Dilution Calculator

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SCH 527123 Molarity Calculator

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Preparing Stock Solutions of SCH 527123

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5162 mL 12.5811 mL 25.1623 mL 50.3246 mL 62.9057 mL
5 mM 0.5032 mL 2.5162 mL 5.0325 mL 10.0649 mL 12.5811 mL
10 mM 0.2516 mL 1.2581 mL 2.5162 mL 5.0325 mL 6.2906 mL
50 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.0065 mL 1.2581 mL
100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.5032 mL 0.6291 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on SCH 527123

SCH-527123 is a novel, selective CXC chemokine receptor 2 (CXCR2) antagonist.

SCH-527123 was able to suppress CXCR2-mediated signal transduction as shown through decreased phosphorylation of the NF-κB/mitogen-activated protein kinase (MAPK)/AKT pathway [1]. 

Cells were treated with increasing concentrations of SCH-527123 for 72 hours and showed dose-dependent growth inhibitory activity with IC50 (72 h) values ranging from 18 to 40 μmol/L. Importantly the IL-8–overexpressing cells showed a higher IC50 (72 h) concentration of SCH-527123 than parental cells [HCT116 and E2 (P < 0.005): 28.9 ± 0.02 μmol/L and 39.5 ± 0.01 μmol/L, respectively; Caco2 and IIIe (P < 0.005): 18.8 ± 0.03 μmol/L and 25.5 ± 0.02 μmol/L, respectively]. Therefore, SCH-527123 decreased growth inhibitory activity in colorectal cancer cell lines [2].

References

References:
[1]. Holz O, Khalilieh S, Ludwig-Sengpiel A et al. SCH527123, a novel CXCR2 antagonist, inhibits ozone-induced neutrophilia in healthy subjects. Holz O1, Khalilieh S, Ludwig-Sengpiel A et al.
[2]. Holz O1, Khalilieh S, Ludwig-Sengpiel A et al. The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models. Mol Cancer Ther. 2012 Jun;11(6):1353-64.

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References on SCH 527123

The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models.[Pubmed:22391039]

Mol Cancer Ther. 2012 Jun;11(6):1353-64.

Colorectal cancer is the second most common cause of cancer-related death in the United States. Recent studies showed that interleukin-8 (IL-8) and its receptors (CXCR1 and CXCR2) are significantly upregulated in both the tumor and its microenvironment, and act as key regulators of proliferation, angiogenesis, and metastasis. Our previous study showed that IL-8 overexpression in colorectal cancer cells triggers the upregulation of the CXCR2-mediated proliferative pathway. The aim of this study was to investigate whether the CXCR2 antagonist, SCH-527123, inhibits colorectal cancer proliferation and if it can sensitize colorectal cancer cells to oxaliplatin both in vitro and in vivo. SCH-527123 showed concentration-dependent antiproliferative effects in HCT116, Caco2, and their respective IL-8-overexpressing variants colorectal cancer cell lines. Moreover, SCH-527123 was able to suppress CXCR2-mediated signal transduction as shown through decreased phosphorylation of the NF-kappaB/mitogen-activated protein kinase (MAPK)/AKT pathway. These findings corresponded with decreased cell migration and invasion, while increased apoptosis in colorectal cancer cell lines. In vivo results verified that SCH-527123 treatment decreased tumor growth and microvessel density when compared with vehicle-treated tumors. Importantly, these preclinical studies showed that the combination of SCH-527123 and oxaliplatin resulted in a greater decrease in cell proliferation, tumor growth, apoptosis, and angiogenesis that was superior to single-agent treatment. Taken together, these findings suggest that targeting CXCR2 may block tumor proliferation, migration, invasion, and angiogenesis. In addition, CXCR2 blockade may further sensitize colorectal cancer to oxaliplatin treatment.

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.[Pubmed:17181143]

J Med Chem. 2006 Dec 28;49(26):7603-6.

Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and may be a potential therapeutic agent for the treatment of various inflammatory diseases.

Description

Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.

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