ONO-7475 is a potent inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 at nM range for both AXL and MER. AXL has been implicated in diverse tumor-promoting processes such as proliferation, migration, invasion, survival, and apoptosis, and therefore considered a promising druggable target to overcome drug resistance for acute myeloid leukemia, pancreatic cancer [2], lung cancer [3], as well as breast cancer [3]. ONO-7475 sensitizes and suppresses the emergence of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells, suggesting that ONO-7475 and osimertinib is a highly potent combination for initial treatment of NSCLC.
Technical information:
| Chemical Formula: |
C32H26N4O6 |
|
| CAS #: | 1646839-59-9 | |
| Molecular Weight: | 562.57 | |
| Purity: | > 98% | |
| Appearance: | Off-White | |
| Chemical Name: | N-(5-((6,7-dimethoxyquinolin-4-yl)oxy)pyridin-2-yl)-2,5-dioxo-1-phenyl-1,2,5,6,7,8-hexahydroquinoline-3-carboxamide | |
| Solubility: | Up to 150 mM in DMSO | |
| Synonyms: | ONO 7475, ONO7475 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Post SM, et al. AXL/Mertk Inhibitor ONO-7475 Potently Synergizes with BCL2 Inhibitor ABT-199, Overcomes ABT-199 Resistance Mechanisms, and Kills FLT3 ITD AML Cells. Blood 2019; 134 (Supplement_1): 2550. Pubmed ID: doi.org/10.1182/blood-2019-128626 |
| 2. | Du W, et al. Does Axl have potential as a therapeutic target in pancreatic cancer? Expert Opin Ther Targets 2018; 22(11):955-966. Pubmed ID: 30244621 |
| 3. | Okura N, et al. ONO-7475, a Novel AXL Inhibitor, Suppresses the Adaptive Resistance to Initial EGFR-TKI Treatment in EGFR-Mutated Non–Small Cell Lung Cancer. Clin Cancer Res 2020;26:2244–56. Pubmed ID: 31953310 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.