CCT196969 / The University of Manchester, Institute of Cancer Research - LARVOL DELTA

CCT196969 inhibits TNBC by targeting the HDAC5/RXRA/ASNS axis to down-regulate asparagine synthesis. (PubMed, J Exp Clin Cancer Res) - "This study reveals a previously unrecognized anti-TNBC mechanism of CCT196969 through the HDAC5/RXRA/ASNS axis. This provides potential candidate targets for the treatment of TNBC and a theoretical basis for the clinical treatment of TNBC patients with CCT196969."

Journal • Breast Cancer • Colorectal Cancer • Melanoma • Oncology • Solid Tumor • Targeted Protein Degradation • Triple Negative Breast Cancer • ASNS • HDAC5 • RXRA

Novel tyrosine kinase/MEK inhibitor combinations impair the viability and invasive potential of TNBC cell lines (AACR 2025) - "We identified several cytokines secreted in response to the pan-Raf inhibitor CCT196969, the MEK inhibitor (MEKi) trametinib and the ERK inhibitor (ERKi) ulixertinib such as FGF-basic, FGF-19, MIF and angiogenin. Lastly, the trametinib/ALW-II-41-27 combination revealed a significant reduction in cell migration and invasion compared to trametinib treatment alone. These findings indicate that ponatinib and ALW-II-41-27 combined with MAPKi could be a promising novel therapeutic approach for TNBC."

Preclinical • Oncology • Triple Negative Breast Cancer • ALK • ERBB3 • FGF19 • FGFR1 • FGFR3 • HER-2

CCT196969 effectively inhibits growth and survival of melanoma brain metastasis cells. (PubMed, PLoS One) - "Furthermore, CCT196969 inhibited viability in two B-Raf Proto-Oncogene (BRAF) inhibitor resistant metastatic melanoma cell lines. Further in vivo studies should be performed to determine the treatment potential of CCT196969 in patients with treatment-naïve and resistant melanoma brain metastasis."

Journal • Melanoma • Oncology • Solid Tumor • STAT3