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DRUG:

AMG 900

i
Other names: AMG 900, AMG-900
Company:
Amgen
Drug class:
Aurora kinase inhibitor
4ms
Identification of Hub of the Hub-Genes From Different Individual Studies for Early Diagnosis, Prognosis, and Therapies of Breast Cancer. (PubMed, Bioinform Biol Insights)
Finally, we suggested hHubGs-guided top-ranked 10 candidate drug molecules (SORAFENIB, AMG-900, CHEMBL1765740, ENTRECTINIB, MK-6592, YM201636, masitinib, GSK2126458, TG-02, and PAZOPANIB) by molecular docking analysis for the treatment against BC. The literature review also supported our findings much more for BC compared with the results of individual studies. Therefore, the findings of this study may be useful resources for early diagnosis, prognosis, and therapies of BC.
Journal
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EGFR (Epidermal growth factor receptor) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • CCND1 (Cyclin D1) • TOP2A (DNA topoisomerase 2-alpha) • CCNA2 (Cyclin A2) • CDK1 (Cyclin-dependent kinase 1) • CCNB1 (Cyclin B1)
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sorafenib • Rozlytrek (entrectinib) • pazopanib • omipalisib (GSK2126458) • AMG 900 • zotiraciclib (TG02) • Kinaction (masitinib)
5ms
The construction of a prognostic model by apoptosis-related genes to predict survival, immune landscape, and medication in cholangiocarcinoma. (PubMed, Clin Res Hepatol Gastroenterol)
Our project suggested that the prognostic model with apoptotic features can effectively predict prognosis in CCA patients, proffering prognostic biomarkers and potential therapeutic targets for CCA patients.
Journal
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MAP3K1 (Mitogen-Activated Protein Kinase Kinase Kinase 1)
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Estybon (rigosertib) • AMG 900
over1year
The inhibition of Aurora A kinase regulates phospholipid remodeling by upregulating LPCAT1 in glioblastoma. (PubMed, Neoplasma)
Notably, the inhibition of Aurora A kinase by shRNA knockdown and treatment with Aurora A kinase inhibitors such as Alisertib, AMG900, or AT9283 upregulated LPCAT1 mRNA and protein expression in vitro. Aurora A kinase inhibition increased LPCAT1 expression and suppressed GBM cell proliferation. The combination of Aurora kinase inhibition with LPCAT1 inhibition may exert promising synergistic effects on GBM.
Journal
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AURKA (Aurora kinase A) • LPCAT1 (Lysophosphatidylcholine Acyltransferase 1)
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alisertib (MLN8237) • AMG 900 • AT9283
2years
2-Phenoxy-3, 4'-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization. (PubMed, Eur J Med Chem)
Hierarchical clustering of cell fitness profiles reveals that these compounds cluster with each other, rather than with known AURK inhibitors such as AMG900 and VX-680. The discovery and optimization of compounds that disrupt AURKB localization are successfully facilitated by MIPS. Our findings suggest that 2-phenoxy-3, 4'-bipyridine derivatives have the potential to be further developed as effective therapeutics for the treatment of malignancy by delocalizing AURKB.
Journal
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AURKB (Aurora Kinase B)
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AMG 900 • tozasertib (MK-0457)
almost4years
Inhibition of Aurora kinase A activity enhances the antitumor response of beta- catenin blockade in human adrenocortical cancer cells. (PubMed, Mol Cell Endocrinol)
The overall survival of patients diagnosed with ACC is low and treatment for metastatic stages remain limited to mitotane, which has low efficiency in advanced stages of the disease and is associated with high toxicity...We studied the combinatorial effects of AMG 900, an aurora kinase inhibitor and PNU-74654, a beta-catenin pathway blocker, on proliferation, survival and tumor progression in multiple ACC cell lines: NCI-H295, CU-ACC1 and CU-ACC2...In contrast, PNU-74654 was more effective in decreasing cortisol secretion. These data suggest that inhibition of aurora kinases activity combined with blockade of the beta-catenin pathway may provide a combinatorial approach for targeting ACC tumors.
Journal
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AURKA (Aurora kinase A)
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Lysodren (mitotane) • AMG 900
4years
AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor‑sensitive and ‑resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B. (PubMed, Oncol Rep)
Imatinib is the gold standard in the conventional treatment of chronic myeloid leukemia (CML)...To overcome this resistance, second‑generation (dasatinib, nilotinib, and bosutinib) and third‑generation (ponatinib) tyrosine kinase inhibitors (TKIs) have been developed and have been shown to be effective against refractory CML...In addition, we found that AMG900, a selective Aurora A and Aurora B inhibitor, increased the G2/M phase cell population and induced apoptosis via inhibition of Aurora A and Aurora B in both TKI‑sensitive and TKI‑resistant CML cells. Our studies show that Aurora A and Aurora B are promising therapeutic targets for TKI‑sensitive and TKI‑resistant CML, and AT9283 may have potential clinical applications for the treatment of TKI‑resistant CML patients.
Journal
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STAT3 (Signal Transducer And Activator Of Transcription 3) • CASP3 (Caspase 3)
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dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • Bosulif (bosutinib) • AMG 900 • AT9283