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Ref Type Journal Article
PMID (28711351)
Authors Goff D, Zhang J, Heckrodt T, Yu J, Ding P, Singh R, Holland S, Li W, Irving M
Title Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy.
Journal Bioorganic & medicinal chemistry letters
Vol 27
Issue 16
Date 2017 Aug 15
URL
Abstract Text Axl tyrosine kinase has been shown to be involved in multiple pathways contributing to tumor development, angiogenesis, and metastasis. High Axl expression has been observed in many human tumors where it appears to confer aggressive tumor behavior. Here we present several series of dual Axl-VEGF-R2 kinase inhibitors based on extensive optimization of an acyl diaminotriazole. It was hypothesized that dual inhibition of these two receptor tyrosine kinases may have a synergistic affect in inhibiting tumor angiogenesis and metastasis. One of these molecules, R916562 showed comparable activity to Sunitinib in two mouse tumor xenograft models and a mouse corneal micropocket model.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
R916562 R916562 2 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
R916562 AXL Inhibitor 27 VEGFR2 Inhibitor 35 R916562 is a small molecule that inhibits both Axl and Vegfr2, therefore results in synergistic inhibition of tumor angiogenesis and metastasis (PMID: 28711351).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown breast cancer not applicable R916562 Preclinical - Cell line xenograft Actionable In a preclinical study, R916562 inhibited tumor cell growth and resulted in tumor regression in a cell line xenograft model of breast cancer (PMID: 28711351). 28711351
Unknown unknown renal carcinoma not applicable R916562 Preclinical - Cell line xenograft Actionable In a preclinical study, R916562 inhibited tumor cell growth and resulted in tumor regression in a cell line xenograft model of renal carcinoma (PMID: 28711351). 28711351