KA2507 hydrochloride (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model[1].
KA2507 hydrochloride also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models[1].
Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 hydrochloride administration resulting in reduced STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response), reduced PD-L1 expression, and increased expression of MHC class I[1].
KA2507 hydrochloride exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg)[1].
| Animal Model: | Male C57BL/6 mice, B16-F10 melanoma model[1] |
| Dosage: | 100 mg/kg, 200 mg/kg, |
| Administration: | P.o.; once a day for 20 days |
| Result: | Inhibited tumor growth in the syngeneic B16-F10 mouse melanoma model.
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| Animal Model: | Male C57BL/6 mice, B16-F10 melanoma model[1] |
| Dosage: | 200 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Oral administration |
| Result: | Oral bioavailability (15%), Cmax (300 ng/mL).
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