CCT137690 / Chroma Therap, Institute of Cancer Research - LARVOL DELTA

Aurora kinase as a putative target to tick control. (PubMed, Parasitology) - "In silico docking assay showed an interaction between Aurora kinase and CCT137690 with exclusive interaction sites in Rm-AURKA. The characterization of exclusive regions of the enzyme will enable new studies aimed at promoting species-specific enzymatic inhibition in ectoparasites."

Journal • AURKA • AURKB

AURKA Identified as Potential Lung Cancer Marker through Comprehensive Bioinformatic Analysis and Experimental Verification. (PubMed, Crit Rev Eukaryot Gene Expr) - "The CCK-8 assay was used to determine the IC50 of the AURKA inhibitor CCT137690 in H1993 cells...AURKA, BIRC5, CCNB1, DLGAP5, KIF11, and KIF15 may be critical genes that influence the occurrence, development, and prognosis of NSCLC. AURKA significantly affects the proliferation and migration of lung cancer cells by disrupting the cell cycle."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • AURKA • BIRC5 • CCNB1 • KIF11

GM-CSF - an oncogenic driver of HER2+ breast leptomeningeal metastasis. (PubMed, Oncoscience) - No abstract available

Journal • Brain Cancer • Oncology • Solid Tumor • CSF2 • HER-2

Enhancing the efficacy of conventional chemotherapy with novel targeted small molecules to kill Ewing sarcoma cancer stem-like cells (AACR 2022) - "In the drug screen, 6% (75/1293) of small molecules were more effective at killing ES-CSCs than doxorubicin...The efficacy of aurora kinase inhibitors, CCT137690 and CD532, was confirmed in 6 ES-CSCs...2021. Cellular Oncology, 44(5):1065-1085 >"

Clinical • Ewing Sarcoma • Oncology • Sarcoma • Solid Tumor • FCGR2A • FCGR2B

GM-CSF is an autocrine driver of HER2+ breast leptomeningeal carcinomatosis (SABCS 2021) - "Lastly, intrathecal delivery of neutralizing anti-GM-CSF antibodies and a pan-Aurora kinase inhibitor (CCT137690) synergistically inhibited GM-CSF and suppressed activity of GM-CSF effectors, reducing HER2+ LC growth in vivo. Thus, OPC suppress GM-CSF-driven growth of HER2+ LC in the leptomeningeal environment, providing a potential targetable axis."

Brain Cancer • Breast Cancer • HER2 Breast Cancer • Oncology • CSF2 • HER-2

Autocrine GM-CSF signaling contributes to growth of HER2+ breast leptomeningeal carcinomatosis. (PubMed, Cancer Res) - "Lastly, intrathecal delivery of neutralizing anti-GM-CSF antibodies and a pan-Aurora kinase inhibitor (CCT137690) synergistically inhibited GM-CSF and suppressed activity of GM-CSF effectors, reducing HER2+ LC growth in vivo. Thus, OPC suppress GM-CSF-driven growth of HER2+ LC in the leptomeningeal environment, providing a potential targetable axis."

Journal • Brain Cancer • Breast Cancer • HER2 Breast Cancer • Oncology • Solid Tumor • CSF2 • HER-2

The Evaluation of Effect of Aurora Kinase Inhibitor CCT137690 in Melanoma and Melanoma Cancer Stem Cell. (PubMed, Anticancer Agents Med Chem) - "Aurora kinases inhibitor CCT137690 displays promising anticancer activity in melanoma and especially melanoma cancer stem cells. The effect of CCT137690 on melanoma and MCSC may provide a new approach to treatment protocols."

Cancer stem cells • Journal • Melanoma • Oncology • Solid Tumor • CASP7 • CCNB1 • MMP10 • MMP2 • MMP7 • PTEN • TP53

Identification and evaluation of novel drug combinations of Aurora kinase inhibitor CCT137690 for enhanced efficacy in oral cancer cells. (PubMed, Cell Cycle) - "Moreover, we demonstrate that polyethylene glycol-based nanocapsules harboring combinations of CCT137690 with gefitinib or pictilisib inhibit the growth of oral cancer cell lines in 3D spheroid cultures and induce apoptosis that is comparable to free drug combinations. In conclusion, we have demonstrated the in vitro efficacy of CCT137690 in oral cancer cell lines, identified novel drug combinations with CCT137690 and synthesized nanocapsules containing these drug combinations for co-administration."

Clinical • Journal • Head and Neck Cancer • Oncology • Oral Cancer • Solid Tumor

Gene mutations and molecularly targeted therapies in acute myeloid leukemia (Am J Blood Res) - PMID: 23358589; “We review characteristic gene mutations, discuss their biological functions and clinical significance and present small molecule compounds in clinical development, which are expected to have a role in treating AML subtypes with characteristic molecular alterations.”

Review • Oncology

Effect of CCT137690 on long non-coding RNA expression profiles in MCF-7 and MDA-MB-231 cell lines. (PubMed, Bosn J Basic Med Sci) - "In addition, MER11C, SCA8, BC200, HOTAIR, PCAT-1, UCA1, SOX2OT, and HULC lncRNAs were downregulated in the ER-negative cell lines. The results of the present study indicated that Aurora kinase inhibitor CCT137690 could be a potential anti-cancer agent for breast cancer treatment."

Journal

Identification and evaluation of novel drug combinations with aurora kinase inhibitor CCT137690 for enhanced efficacy in 2D monolayer and 3D spheroid model of oral cancer cells (AACR 2019) - "Our results suggest that the combination of CCT137690 with ZD1839 or GDC-0941 can be further evaluated for the treatment of oral cancer. Moreover, these combinations can be delivered through nanocapsules to confer additional advantages of reduced cytotoxicity and sustained release for better therapeutic index and efficacy."

Clinical