1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
    VEGFR

R916562 

Cat. No.: HY-104075
Handling Instructions

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

For research use only. We do not sell to patients.

R916562 Chemical Structure

R916562 Chemical Structure

CAS No. : 1037798-41-6

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8654 mL 9.3268 mL 18.6536 mL
5 mM 0.3731 mL 1.8654 mL 3.7307 mL
10 mM 0.1865 mL 0.9327 mL 1.8654 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

536.09

Formula

C₂₆H₃₀ClN₉S

CAS No.

1037798-41-6

SMILES

NC1=NC(NC(C=C2)=CC=C2N3CCN([[email protected]]4[[email protected]@H]5CC[[email protected]@H](C5)C4)CC3)=NN1C6=NC(Cl)=NC7=C6SC=C7C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
R916562
Cat. No.:
HY-104075
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R916562

Cat. No.: HY-104075