ODM-203, a selective inhibitor of FGFR and VEGFR, shows strong antitumor activity, and induces antitumor immunity was written by Holmstrom, Tim H.;Moilanen, Anu-Maarit;Ikonen, Tarja;Bjorkman, Mari L.;Linnanen, Tero;Wohlfahrt, Gerd;Karlsson, Stefan;Oksala, Riikka;Korjamo, Timo;Samajdar, Susanta;Rajagopalan, Srinivasan;Chelur, Shekar;Narayanan, Kishore;Ramachandra, Raghuveer K.;Mani, Jiju;Nair, Rashmi;Gowda, Nagaraj;Anthony, Thomas;Dhodheri, Samiulla;Mukherjee, Subhendu;Ujjinamatada, Ravi K.;Srinivas, Nanduri;Ramachandra, Murali;Kallio, Pekka J.. And the article was included in Molecular Cancer Therapeutics in 2019.Related Products of 1035270-39-3 This article mentions the following:
Alterations in the gene encoding for the FGFR and upregulation of the VEGFR are found often in cancer, which correlate with disease progression and unfavorable survival. In addition, FGFR and VEGFR signaling synergistically promote tumor angiogenesis, and activation of FGFR signaling has been described as functional compensatory angiogenic signal following development of resistance to VEGFR inhibition. Several selective small-mol. FGFR kinase inhibitors are currently in clin. development. ODM-203 is a novel, selective, and equipotent inhibitor of the FGFR and VEGFR families. In this report we show that ODM-203 inhibits FGFR and VEGFR family kinases selectively and with equal potency in the low nanomolar range (IC50 6-35 nmol/L) in biochem. assays. In cellular assays, ODM-203 inhibits VEGFR-induced tube formation (IC50 33 nmol/L) with similar potency as it inhibits proliferation in FGFR-dependent cell lines (IC50 50-150 nmol/L). In vivo, ODM-203 shows strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses. In addition, ODM-203 inhibits metastatic tumor growth in a highly angiogenesis-dependent kidney capsule syngenic model. In the experiment, the researchers used many compounds, for example, rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3Related Products of 1035270-39-3).
rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Related Products of 1035270-39-3
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics