1. Protein Tyrosine Kinase/RTK
    Neuronal Signaling
  2. TAM Receptor
    Trk Receptor
  3. ONO-7475

ONO-7475 

Cat. No.: HY-114358 Purity: 99.38%
Handling Instructions

ONO-7475 is a potent, selective, and orally active novel Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. ONO-7475 sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. ONO-7475 combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).

For research use only. We do not sell to patients.

ONO-7475 Chemical Structure

ONO-7475 Chemical Structure

CAS No. : 1646839-59-9

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Based on 1 publication(s) in Google Scholar

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Description

ONO-7475 is a potent, selective, and orally active novel Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. ONO-7475 sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. ONO-7475 combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC)[1].

IC50 & Target

IC50: 0.7 nM (AXL)[1]
IC50: 1.0 nM (MER tyrosine kinase)[2]

In Vitro

ONO-7475 is against recombinant human AXL with IC50 values of 0.414 nM and 0.7 nM in off-chip MSA and ACD cell-based tyrosine kinase assay, respectively. It is against AXL, MER, TYRO3, TRKB, PDGFR alpha, TRKA, and FLT3 activities with IC50 values of 0.7 nM, 1.0 nM, 8.7 nM, 15.8 nM, 28.9 nM, 35.7 nM and 147 nM, respectively in a Cell-based Tyrosine Kinase assay[2].
ONO-7475 (0.0001 μM-1 μM; 72 hours) increases the sensitivity to Osimertinib and Dacomitinib and reduces the viability of high AXL-expressing PC-9 and HCC4011 cells, but not of low-AXL-expressing HCC827 cells. Besides, ONO-7475 enhances Osimertinib efficacy on the viability of cell lines PC-9, PC-9KGR, and HCC4011, and H1975, all of which express high levels of AXL. But it has a marginal effect on the viability of cell lines HCC827, HCC4006, and H3255 with low levels of AXL[1].
ONO-7475 (1 μM; 4 or 48 hours) combines with Osimertinib markedly inhibits the phosphorylation of AXL, AKT, and p70S6K compared with the treatment of the high-AXL-expressing cell lines treated with Osimertinib alone at 4 hours. It combines with osimertinib increases cleaved PARP in PC-9 and HCC4011 cells compared with the treatment with Osimertinib alone[1].

Cell Viability Assay[1]

Cell Line: High AXL-expressing cell: PC-9,HCC4011,H1975, PC-9KGR cells
Low AXL-expressing cell: HCC827, HCC4006, and H3255 cells
Concentration: 0.0001 μM; 0.001 μM; 0.01 μM; 0.1 μM; 1 μM
Incubation Time: 72 hours
Result: Increased the sensitivity and efficacy to Osimertinib in AXL-high level cells.

Western Blot Analysis[1]

Cell Line: PC-9, HCC4011 cells
Concentration: 1 μM
Incubation Time: 4 or 48 hours
Result: Increased p-AXL, AKT, and p70S6K expression at 4 hours and increases p-PARP expression at 48 hours when combindes with Osimertinib.
In Vivo

ONO-7475 (oral gavage; 10 mg/kg or combines with 5 mg/kg Osimertinib; 29 days) treatment alone has little effect on the tumor growth. Besides, Osimertinib alone causes tumor regression within one week, but the tumors reappear within three weeks. The combined initial treatment causes tumor regression and the size of tumors is maintained for 4 weeks. No apparent adverse events, including weight loss are observed during these treatments[1].

Animal Model: Mouse CDX model using high-AXL-expressing PC-9KGR cells (exon 19 deletion and the exon21-T790M mutation in EGFR)[1]
Dosage: 10 mg/kg; once daily; 19 days
Administration: oral gavage
Result: Had little effects alone, but combined treatments significantly decreased tumor volume without reappear.
Molecular Weight

562.57

Formula

C₃₂H₂₆N₄O₆

CAS No.

1646839-59-9

SMILES

O=C(C1=CC2=C(N(C3=CC=CC=C3)C1=O)CCCC2=O)NC4=NC=C(OC5=CC=NC6=CC(OC)=C(OC)C=C56)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (444.39 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7776 mL 8.8878 mL 17.7756 mL
5 mM 0.3555 mL 1.7776 mL 3.5551 mL
10 mM 0.1778 mL 0.8888 mL 1.7776 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

ONO-7475ONO7475ONO 7475TAM ReceptorTrk ReceptorTyro3AxlMerTropomyosin related kinase receptorEGFRmutuntNSCLCcancerlungTKItolerantAXLacuteleukemiaadvancedmetastaticsolidtumorInhibitorinhibitorinhibit

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ONO-7475
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