| Chemical Properties | Back Directory | [Boiling point ]
822.0±75.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [form ]
Solid | [pka]
7.55±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. ABN401 has cytotoxic activity against MET-addicted cancer cells. ABN401 can inhibit c-MET phosphorylation in tumor tissues. ABN401 can be used for researching anticancer[1]. | [Uses]
ABN401 is an orally active and selective ATP-competitive c-MET inhibitor with an IC50 of 10 nM. ABN401 is cytotoxic to MET-addicted cancer cells with the IC50 of 2-43 nM. ABN401 has bioavailability in rats and dogs of 42.1-56.2% and 27.4-37.7%, respectively. ABN401 has antitumor activity[1][2]. | [in vivo]
ABN401 (3-30 mg/kg; oral administration; five consecutive days a week for 3 weeks) has antitumor effect in mouse lung cancer and gastric cancer models[1].
ABN401 (3-30 mg/kg; oral administration; once a day for 3 weeks) shows antitumor activity in a xenograft model derived from patients with non-small cell lung cancer in mice, and the combination with Erlotinib (HY-50896) has better effect[2]. | Animal Model: | SNU5, EBC-1 and SNU638 treated BALB/c-nude mice[1] | | Dosage: | 3, 10 and 30 mg/kg | | Administration: | Oral administration (p.o.); Five consecutive days a week for three weeks | | Result: | Significantly inhibited tumor growth in a dose-dependent manner.
Significantly suppressed SNU-5 tumor growth with a TGI index of 24.47% and 89.49% at doses of 3 and 30 mg/kg, respectively.
Inhibited EBC-1 tumor growth with a TGI index of 51.26% and 77.85% at doses of 10 and 30 mg/kg, respectively.
Suppressed SNU638 tumor growth with a TGI index of 65.31% and 78.68% at doses of 10 and 30 mg/kg, respectively. |
| [References]
[1] Kim J, et al. Therapeutic Efficacy of ABN401, a Highly Potent and Selective MET Inhibitor, Based on Diagnostic Biomarker Test in MET-Addicted Cancer. Cancers (Basel). 2020;12(6):1575. Published 2020 Jun 15. DOI:10.3390/cancers12061575
[2] Kim NA, et al. New Preclinical Development of a c-Met Inhibitor and Its Combined Anti-Tumor Effect in c-Met-Amplified NSCLC. Pharmaceutics. 2020 Feb 3;12(2):121. DOI:10.3390/pharmaceutics12020121 |
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