SB-265610_product_DataBase

Bioactivity

SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively[1][2].

Invitro

In vitro, SB-265610 antagonizes rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization, IC50 of 3.7 nM, and rat neutrophil chemotaxis in a concentration-dependent manner, IC50 of 70 nM. SB-265610 reduces the antiapoptotic effect of CINC-1 to the levels of those untreated with CINC-1[1].

In Vivo

SB-265610 (2 mg/kg/day; i.p.; daily; for two weeks) treatment significantly inhibits the recruitment of Gr-1+CD11b+ cells to the mammary adenocarcinoma with Tgfbr2 deletion but not the control tumors[3]. Animal Model:

Name

SB-265610

CAS

211096-49-0

Formula

C14H9BrN6O

Molar Mass

357.16

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Auten RL, et al. Nonpeptide CXCR2 antagonist prevents neutrophil accumulation in hyperoxia-exposed newborn rats. J Pharmacol Exp Ther. 2001 Oct;299(1):90-5. [2]. Milatovic S, et al. Impaired healing of nitrogen mustard wounds in CXCR2 null mice. Wound Repair Regen. 2003 May-Jun;11(3):213-9. [3]. Li Yang, et al. Abrogation of TGF beta signaling in mammary carcinomas recruits Gr-1+CD11b+ myeloid cells that promote metastasis. Cancer Cell. 2008 Jan;13(1):23-35.

PeptideDB

SB-265610

CAS: 211096-49-0 F: C14H9BrN6O W: 357.16