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  • DC Chemicals Limited
  • China
  • Product Name: R916562
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

1037798-41-6

1037798-41-6 structure
1037798-41-6 structure
  • Name: R916562
  • Chemical Name: R916562
  • CAS Number: 1037798-41-6
  • Molecular Formula: C26H30ClN9S
  • Molecular Weight: 536.09
  • Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK TAM Receptor
  • Create Date: 2018-09-06 14:44:24
  • Modify Date: 2024-01-09 23:08:31
  • R916562 is a potential and selective Axl/VEGF-R2 dual inhibitor with IC50s of 136 and 24 nM, respectively.

Name R916562
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.

Molecular Formula C26H30ClN9S
Molecular Weight 536.09