ONO-7475
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1750 | Check With Us |
| 500mg | $2950 | Check With Us |
| 1g | $4425 | Check With Us |
: Cat #: V37620 CAS #: 1646839-59-9 Purity ≥ 99%
Description: ONO-7475 is a novel and orally bioactive dual Axl/Mer inhibitor with anticancer activity by targeting both Axl and Mer, and preventing their activity.
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| Molecular Weight (MW) | 562.57 |
|---|---|
| Molecular Formula | C32H26N4O6 |
| CAS No. | 1646839-59-9 |
| SMILES Code | 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 |
| Synonyms | ONO-7475; ONO 7475; ONO7475; |
| Protocol | In Vitro | Tamnorzatinib (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. Tamnorzatinib (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, Tamnorzatinib 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. Tamnorzatinib 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. |
|---|---|---|
| In Vivo | Tamnorzatinib (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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.7776 mL | 8.8878 mL | 17.7756 mL | 35.5511 mL |
| 5mM | 0.3555 mL | 1.7776 mL | 3.5551 mL | 7.1102 mL |
| 10mM | 0.1778 mL | 0.8888 mL | 1.7776 mL | 3.5551 mL |
| 20mM | 0.0889 mL | 0.4444 mL | 0.8888 mL | 1.7776 mL |
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Method for preparing in vivo formulation:
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