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Association details:
| Biomarker: | KRAS G12A |
|---|---|
| Cancer: | Lymphoma |
| 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:
...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.
