^
5ms
Focal adhesion kinase and its epigenetic interactors as diagnostic and therapeutic hints for pediatric hepatoblastoma. (PubMed, Front Oncol)
Finally, TAE226 caused a significant reduction of pTyr397FAK, epigenetic regulators, AFP, EPCAM, OCT4, and SOX2, in association with anti-proliferative and pro-apoptotic effects on HB cells. Our results suggest a role of FAK in HB that requires further investigations mainly focused on the exploration of its effective diagnostic and therapeutic translatability.
Journal
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AFP (Alpha-fetoprotein) • SOX2 • POU5F1 (POU Class 5 Homeobox 1)
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NVP-TAE226
1year
Design, synthesis, and biological evaluation of diaminopyrimidine derivatives as novel focal adhesion kinase inhibitors. (PubMed, RSC Med Chem)
Herein, 24 diaminopyrimidine derivatives were designed and synthesized based on TAE-226...Compound A12 was also selected for molecular docking studies and the prediction of molecular properties and drug-like properties. These results indicated that compound A12 could be used as a potential lead compound targeting FAK for further development.
Journal
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PTK2 (Protein Tyrosine Kinase 2)
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NVP-TAE226
over1year
FERMT1 Is a Prognostic Marker Involved in Immune Infiltration of Pancreatic Adenocarcinoma Correlating with mA Modification and Necroptosis. (PubMed, Genes (Basel))
Finally, FERMT1 overexpression may be sensitive to chemotherapy drugs such as Palbociclib, AM-5992 and TAE-226. FERMT1 can serve as a diagnostic and prognostic marker of PAAD, which is connected with immune cell infiltration and the modulation of mA and necroptosis.
Journal
|
FERMT1 (Fermitin Family Member 1)
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FERMT1 expression
|
Ibrance (palbociclib) • AM-5992 • NVP-TAE226
over1year
Design, synthesis and evaluation of nitric oxide releasing derivatives of 2,4-diaminopyrimidine as novel FAK inhibitors for intervention of metastatic triple-negative breast cancer. (PubMed, Eur J Med Chem)
The most active compound 8f not only significantly inhibited FAK kinase activity (IC = 27.44 nM), displayed potent inhibitory effects on the proliferation (IC = 0.126 μM), invasion and migration of MDA-MB-231 cells, superior to the most widely studied FAK inhibitor, TAE226, bearing 2,4-diaminopyrimidine, but also released high levels of NO, contributing to blockage of FAK mediated-signaling pathways by upregulating of p53 as well as suppressing the Y397 phosphorylation and its downstream effectors, including p-Akt, MMP-2, and MMP-9 via kinase-independent manner, leading to apoptosis induction and decrease of FAs and SFs in TNBC cells. Importantly, 8f inhibited the lung metastasis of TNBC in vivo. Together, 8f may serve as a promising candidate for the treatment of metastatic TNBC.
Journal • Metastases
|
MMP2 (Matrix metallopeptidase 2) • MMP9 (Matrix metallopeptidase 9)
|
NVP-TAE226
almost2years
The dual FAK-HDAC inhibitor MY-1259 displays potent activities in gastric cancers in vitro and in vivo. (PubMed, Bioorg Chem)
MY-1259 exhibited more effective antitumor effect in vivo than the HDAC inhibitor SAHA and FAK inhibitor TAE-226 alone or in combination, showing the advantages of FAK/HDAC dual inhibitors in the treatment of gastric cancers. Therefore, the results in this work suggested that inhibition of FAK and HDAC by MY-1259 might represent a promising strategy for the treatment of gastric cancers.
Preclinical • Journal
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HDAC2 (Histone deacetylase 2) • HDAC1 (Histone Deacetylase 1) • HDAC3 (Histone Deacetylase 3)
|
Zolinza (vorinostat) • NVP-TAE226
2years
Rho-associated kinase1 promotes laryngeal squamous cell carcinoma tumorigenesis and progression via the FAK signaling pathway. (PubMed, Discov Oncol)
Inhibiting FAK activity with TAE226 observably impairs the tumor-promoting effects. In conclusion, ROCK1 promotes LSCC tumorigenesis and progression via the FAK signaling pathway, targeting the ROCK1 molecule may represent potential targets for clinical LSCC treatment.
Journal
|
ROCK1 (Rho Associated Coiled-Coil Containing Protein Kinase 1)
|
NVP-TAE226
almost3years
Focal adhesion kinase inhibitor TAE226 combined with Sorafenib slows down hepatocellular carcinoma by multiple epigenetic effects. (PubMed, J Exp Clin Cancer Res)
Altogether, our findings provide the first evidence that TAE226 combined with SOR efficiently reduces HCC growth in vitro and in vivo. Also, our data highlight that deep analysis of FAK nuclear interactome may lead to the identification of new promising targets for HCC therapy.
Journal
|
HDAC1 (Histone Deacetylase 1)
|
sorafenib • VS-4718 • benzesulfonate (PF-562271) • NVP-TAE226
4years
TAE226, a dual inhibitor of focal adhesion kinase and insulin-like growth factor-I receptor, is effective for Ewing sarcoma. (PubMed, Cancer Med)
TAE226 is a dual inhibitor of FAK and insulin-like growth factor-I receptor (IGF-IR), while PF-562,271 is a dual inhibitor of FAK and proline-rich tyrosine kinase 2. Furthermore, the combination of TAE226 and conventional chemotherapy proved to exert synergistic effects. TAE226 may be a candidate single agent or combined therapy drug to be developed for patients who have relapse and metastatic EWS tumors in future.
Journal
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IGF1R (Insulin-like growth factor 1 receptor) • TYK2 (Tyrosine Kinase 2)
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benzesulfonate (PF-562271) • NVP-TAE226