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|Ref Type||Journal Article|
|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|
|Date||2017 Aug 15|
|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.|
|Molecular Profile||Treatment Approach|
|Gene Name||Source||Synonyms||Protein Domains||Gene Description||Gene Role|
|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|