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YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts.
These findings represent the first attempt to show tumor regression and suppression of survivin in p53-deficient human HRPC cells by a single small molecular compound treatment. Expand
Broad spectrum and potent antitumor activities of YM155, a novel small‐molecule survivin suppressant, in a wide variety of human cancer cell lines and xenograft models
The broad and potent antitumor activity presented in the present study is indicative of the therapeutic potential of YM155 in the clinical setting. Expand
Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia
- Masamichi Mori, N. Kaneko, +6 authors S. Kuromitsu
- Biology, Medicine
- Investigational New Drugs
- 17 May 2017
Results indicate that gilteritinib may be an important next-generationFLT3 inhibitor for use in the treatment of FLT3 mutation-positive AML. Expand
The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice
- Masamichi Mori, Y. Ueno, +12 authors S. Kuromitsu
- Molecular Cancer Therapeutics
- 13 January 2014
Findings indicate that ASP3026 has potential efficacy for NSCLC and is expected to improve the therapeutic outcomes of patients with cancer with ALK abnormality and exhibited potent antitumor activity against cells expressing EML4-ALK. Expand
Antitumor effects of YM155, a novel survivin suppressant, against human aggressive non-Hodgkin lymphoma.
This study suggests that YM155 may represent an effective treatment for aggressive lymphomas, and increased survival significantly versus rituximab in disseminated Ramos models. Expand
Minodronic acid, a third-generation bisphosphonate, antagonizes purinergic P2X(2/3) receptor function and exerts an analgesic effect in pain models.
- S. Kakimoto, Y. Nagakura, +6 authors M. Okada
- Chemistry, Medicine
- European journal of pharmacology
- 28 July 2008
Subcutaneously administered minodronic acid significantly inhibited the alpha,beta-methylene ATP-, acetic acid- and formalin-induced nociceptive behaviors in mice, which would be beneficial for the treatment of accelerated bone turnover diseases accompanied by bone pain, including bone metastases. Expand
ASP2215, a novel FLT3/AXL inhibitor: Preclinical evaluation in acute myeloid leukemia (AML).
This data indicates that activation mutations in FLT3 receptor tyrosine kinase, characterized by internal tandem duplication (ITD) and tyrosin kinase domain point mutations near position D835, are likely to be related to each other. Expand
Evaluation of gilteritinib in combination with chemotherapy in preclinical models of FLT3-ITD+ acute myeloid leukemia
Findings support the investigation of gilteritinib combined with chemotherapy in patients with FLT3-ITD+ AML, including those who are ineligible for intensive chemotherapy. Expand
Abstract 2678: First demonstration ofin vivoPET imaging for ALK inhibitor using [11C]ASP3026, a novel brain-permeable type of ALK inhibitor.
The study has revealed that ASP3026 shows a brain tumor permeability in an intracranial xenograft model of H2228-luc ALK fusion positive cells and comparison of pharmacokinetic profiles in several tumor models showed that tumor uptake of ASP3026 was higher than that of surrounding tissue, suggesting that tumor accumulation of ASP30 26 was dependent on the microenvironment of tumor. Expand