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ONO-7475, potent inhibitor of Anexelekto(Axl)/MER tyrosine kinase

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ONO-7475, potent inhibitor of Anexelekto(Axl)/MER tyrosine kinase

 

 

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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.

 

Details

Chemical Formula:

 

C32H26N4O6

CAS No.:

 

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

Storage:

 

For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.

 

References

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

 

  

Ordering information

   

Catalog No.

Product Name

Size

C6667

ONO-7475, potent inhibitor of Anexelekto(Axl)/MER tyrosine kinase

5mg, 25mg & 100mg

     

 

▣ 관련 페이지 ; Cellagen Technology

 

   

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