2019
DOI: 10.1002/ijc.32224
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Rogaratinib: A potent and selective pan‐FGFR inhibitor with broad antitumor activity in FGFR‐overexpressing preclinical cancer models

Abstract: Aberrant activation in fibroblast growth factor signaling has been implicated in the development of various cancers, including squamous cell lung cancer, squamous cell head and neck carcinoma, colorectal and bladder cancer. Thus, fibroblast growth factor receptors (FGFRs) present promising targets for novel cancer therapeutics. Here, we evaluated the activity of a novel pan‐FGFR inhibitor, rogaratinib, in biochemical, cellular and in vivo efficacy studies in a variety of preclinical cancer models. In vitro kin… Show more

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Cited by 80 publications
(52 citation statements)
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“…The IC50 for palbociclib in the 7 cell lines is shown in Supplemental Table 2. We next tested the effects of FGFR1 inhibition with the selective pan-FGFR inhibitor rogaratinib [51]. Rogaratinib effectively inhibited ERK, FGFR1, and FRS2 phosphorylation in response to the FGFR1 ligand bFGF in FGFR1-high or LTED-R cell lines (Supplemental Figure 3).…”
Section: Prolonged Hormonal Deprivation Leads To Increased Fgfr1 Tranmentioning
confidence: 99%
“…The IC50 for palbociclib in the 7 cell lines is shown in Supplemental Table 2. We next tested the effects of FGFR1 inhibition with the selective pan-FGFR inhibitor rogaratinib [51]. Rogaratinib effectively inhibited ERK, FGFR1, and FRS2 phosphorylation in response to the FGFR1 ligand bFGF in FGFR1-high or LTED-R cell lines (Supplemental Figure 3).…”
Section: Prolonged Hormonal Deprivation Leads To Increased Fgfr1 Tranmentioning
confidence: 99%
“…They showed the efficacy of CDK4 and CDK6 inhibitors for HNSCC with CCND1 and CDKN2A genomic alterations [89,90]. For breast cancer, Grunewald et al evaluated the activity of a novel fibroblast growth factor receptor (FGFR) inhibitor, rogaratinib, using cancer cell lines and breast cancer PDX models [91]. They found that the inhibitor has a strong efficacy for FGFR overexpressing cells, both in vitro and in vivo.…”
Section: Application Of Pdx Models For Clinical Usementioning
confidence: 99%
“…Rogaratinib is an oral, potent, selective FGFR1–4 inhibitor. Preclinical studies showed response to rogaratinib correlated with high FGFR mRNA expression in tumors [27].…”
Section: Rogaratinibmentioning
confidence: 99%