ONO-7475 is a potent and orally active 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 provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
Mice fed a diet containing ONO-7475 exhibited significantly longer survival and, interestingly, blocked leukemia cell infiltration in the liver. In summary, ONO-7475 effectively kills acute myeloid leukemia cells in vitro and in vivo by mechanisms that involve disruption of diverse survival and proliferation pathways.
Cell Experiment | |
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Cell lines | MOLM13, MV4;11, HL60, OCI-AML3, MOLM13 luc/gfp cells, MOLM13 p53 shRNA cells, BM-MSC |
Preparation method | MOLM13 and MV4;11 (FLT3 ITD) and OCI-AML3 (FLT3 WT) cells are incubated with vehicle (0.1% DMSO) or varying doses of ONO-7475 for 48 hours. Viable cell number and apoptosis are measured by flow cytometry. |
Concentrations | 50-500 nM |
Incubation time | 24 h, 48 h, 72 h |
Animal Experiment | |
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Animal models | 4-week old female NSG mice bearing MOLM13 cells |
Formulation | diet containing 0.004% and 0.013% ONO-7475 |
Dosages | 6 mg/kg, 20 mg/kg |
Administration | Oral gavage |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Molecular Weight | 562.57 |
Formula | C32H26N4O6 |
CAS Number | 1646839-59-9 |
Purity | >99% |
Solubility | DMSO 100 mg/mL |
Storage | at -20°C |
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TP-0903 is a potent and selective AXL inhibitor with an IC50 value of 27 nM. |
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Bemcentinib
R428 is a potent and selective small-molecule inhibitor of Axl kinase with IC50 of 14 nM. |
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