R916562

Modify Date: 2024-01-09 23:08:31

R916562 Structure
R916562 structure
Common Name R916562
CAS Number 1037798-41-6 Molecular Weight 536.09
Density N/A Boiling Point N/A
Molecular Formula C26H30ClN9S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of R916562


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

 Names

Name R916562

 R916562 Biological Activity

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

Axl:136 nM (IC50)

VEGF-R2:24 nM (IC50)

In Vivo 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].
Animal Admin 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C26H30ClN9S
Molecular Weight 536.09