| Description |
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a humanized monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation[1].
|
| Related Catalog |
|
| Target |
IGF1, IGF2[1]
|
| In Vitro |
Xentuzumab (0.01-1 mM; 96 h) inhibits IGF type 1 receptor signaling and (0.1 μM; 48 h) AKT serine/threonine kinase (AKT) phosphorylation in VCaP, DuCaP, and MDA PCa 2b cell in a dose-dependent manner[1]. Xentuzumab (0.01-1 mM; 5-10 d) losses of antiproliferative activity against PTEN-null LNCaP or PC-3 cells when PTEN knockdown[1]. Xentuzumab (1 μM; 24-72 h) arrests cell cycle at sub-G1 phase and induces apoptosis in VCaP cells[1]. Western Blot Analysis[1] Cell Line: Prostate cancer VCaP cells Concentration: 0.1 μM Incubation Time: 24 h and 48 h Result: Increased in cleaved caspase 3/7 and PARP. Decreased the level of phosphorylation of FoxO3a (S253)/FoxO1 (T24). Cell Cycle Analysis[1] Cell Line: Prostate cancer VCaP cells Concentration: 1 μM Incubation Time: 24 h, 48 h, and 72 h Result: Increased in cleaved caspase 3/7 and induces cell apoptosis. Increased the sub-G1 cell population.
|
| In Vivo |
Xentuzumab (200 mg/kg i.p., once weekly for 10 weeks) in inhibits tumor growth in LuCaP 96CR patient-derived xenograft model in mice[1]. Animal Model: Fox Chase CB17 severe combined immunodeficiency (SCID; CB17/lcr-Prkdc scid/lcrlcoCrl) male mice with LuCaP 96CR cell (s.c.)[1] Dosage: 200 mg/kg Administration: Intraperitoneal injection; once weekly for 10 weeks; sacrificed 6 hours after the last dose Result: Resulted in significant reductions in tumor volume.
|
| References |
[1]. Weyer-Czernilofsky U, et al. Antitumor Activity of the IGF-1/IGF-2-Neutralizing Antibody Xentuzumab (BI 836845) in Combination with Enzalutamide in Prostate Cancer Models. Mol Cancer Ther. 2020 Apr;19(4):1059-1069.
|
