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Association details:
| Biomarker: | KRAS G12A |
|---|---|
| Cancer: | Acute Myelogenous Leukemia |
| Drug: | GT19077 (MYC inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
1547 Discovery of GT19077, a c-Myc/Max Protein-Protein Interaction (PPI) Small Molecule Inhibitor, for Targeting c-Myc-Driven Blood Cancers
Published date:
11/04/2020
Excerpt:
Dysregulated c-Myc is one of major oncogene drivers in B-cell lymphoma, MM and AML. Therefore, GT19077 was evaluated in a panel of 14 hematologic malignant cell lines expressing dysregulated c-Myc or other oncogene drivers. The results showed that GT19077 selectively inhibited the proliferation of all seven B-cell malignant cell lines tested, carrying IGH/Myc translocations (6/7) or Kras G12A mutation (1/7), with IC50s as low as 160 nM. In addition, two myeloblast cell lines and one monoblast cell line were also sensitive to GT19077 with IC50 of 300-700 nM. . Importantly, GT19077 effectively inhibits the proliferation of B-cell lymphoma, MM and AML cells carrying c-Myc genetic alterations, including IGH/Myc translocations, but lacks activity in blood cancer cells expressing other oncogene drivers.
Source:
Title:
Abstract LB-111: GT19077, a c-Myc/Max protein-protein interaction (PPI) small molecule inhibitor, selectively targets c-Myc-additive B-cell and myeloid malignancies
Published date:
06/23/2020
Excerpt:
Profiling on the proliferation of a selected 14 hematologic malignant cell panel with c-Myc overexpression, GT19077 selectively inhibited the proliferation of all seven B-cell malignant cell lines tested, which include three carrying Myc-IGH translocations and two expressing Kras G12A mutations, with IC50s as low as 160 nM.
DOI:
10.1158/1538-7445.AM2020-LB-111
