1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
    VEGFR
  3. R916562

R916562 

Cat. No.: HY-104075
Handling Instructions

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

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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Description

R916562 is a potential, selective, dual Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis[1].

IC50 & Target[1]

Axl

136 nM (IC50)

VEGF-R2

24 nM (IC50)

In Vivo

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].

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage

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

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
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R916562
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