Name | R916562 |
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Description | R916562 is a potential and selective Axl/VEGF-R2 dual inhibitor with IC50s of 136 and 24 nM, respectively. |
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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 |
Molecular Formula | C26H30ClN9S |
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Molecular Weight | 536.09 |