Uses
SB 265610 is an anti-tumor pharmaceutical developed to act as an antagonist to cysteine-amino acid-cysteine (CXC) chemokines receptor 2 antagonist.
Biological Activity
Potent CXCR2 antagonist that inhibits CINC-1-mediated but not C5a-mediated Ca 2+ mobilization (IC 50 values are 3.4 and 6800 nM respectively). Inhibits CINC-induced chemotaxis and attenuates neutrophil accumulation in inflammatory lung injury in vivo .
Biochem/physiol Actions
SB265610 is a potent and selective CXCR2 chemokine receptor antagonist. It has a Kd = 2.5 nM.
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: | MMTV-PyVmT/Tgfbr2MGKO and MMTV-PyVmT/Tgfbr2flox/flox tumors from donor mice[3] |
| Dosage: | 2 mg/kg/day
|
| Administration: | Intraperitoneal injection; daily; for two weeks |
| Result: | Significantly inhibited the recruitment of Gr-1+CD11b+ cells to the mammary adenocarcinoma. |
