Evaluation of VTP‐50469, a menin‐MLL1 inhibitor, against Ewing sarcoma xenograft models by the pediatric preclinical testing consortium
Year: 2020
Type: article
Abstract: Background VTP‐50469 is a potent inhibitor of the menin‐MLL1 interaction and is implicated in signaling downstream of EWSR1‐FLI1. Procedure VTP‐50469 was evaluated against seven Ewing sarcoma (EwS) xenograft models and in vitro against EwS cell lines. Results VTP‐50469 showed limited antitumor activity, statistically significantly slowing tumor progression in four tumor models but with no evidence of tumor regression. In vitro, the IC50 concentration was 10 nM for the mixed lineage leukemia (MLL)‐rearranged leukemia cell line MV4;11, but > 3 μM for EwS cell lines. Conclusions In contrast to its high level of activity against MLL1‐rearranged leukemia xenografts, VTP‐50469 shows little activity against EwS models.
Source: Pediatric Blood & Cancer
DOI: 10.1002/pbc.28284
Language: English
Subfield: Pulmonary and Respiratory Medicine
Field: Medicine
Domain: Health Sciences
Open Access status: green
Funder: National Cancer Institute
Awards: G1143455775, Mays Cancer Center at UT Health SA, G1852923484, Pediatric Preclinical Testing Consortium: Coordinating Center, G827162950, G8294603191, Pediatric Preclinical Testing Consortium: Research Programs Non-CNS (U01), A Testing Program to Identify Novel Agents for Treatment of Pediatric and AYA High-Risk Sarcoma, Kidney and Liver Cancer
OpenAlex ID: W3018304754