R916562

R916562 is a potential and selective Axl/VEGF-R2 dual inhibitor with IC50s of 136 and 24 nM, respectively.

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> TAM Receptor

Research Areas >> Cancer

Axl:136 nM (IC50)

VEGF-R2:24 nM (IC50)

R916562 delays and inhibits tumor growth in MDA-MB-231 human breast cancer xenograft model. R916562 also shows efficacy in the Caki-1 human renal carcinoma xenograft model. R916562 treatment at 85 mg/kg or 125 mg/kg orally b.i. d for 21 days results in statistically significant tumor growth inhibitions of 69% or 83% respectively. R916562 shows 73% reduction in fibroblast growth factor-induced neovascularization in a mouse corneal micropocket assay at a dose of 100 mg/kg and 50% reduction at 50 mg/kg[1].

Mice[1] The nu/nu mice are used in the study. In the MDA-MB-231 human breast cancer xenograft model, mice are given 125 mg/kg b.i.d. orally for 21 days. Mean tumor volume is measured[1].

[1]. Goff D, et al. Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. Bioorg Med Chem Lett. 2017 Aug 15; 27(16):3766-3771.

Bemcentinib (R428) | Nintedanib (BIBF 1120) | SU5416 | Gilteritinib | Apatinib Mesylate | PD173074 | Foretinib (GSK1363089) | SU 5402 | Linifanib (ABT-869) | Cediranib | Lucitanib | RAF265 (CHIR-265) | LY2784544 | BMS-777607 | SU14813