KA2507

KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC 50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models In Vitro KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo KA2507 (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model . KA2507 also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models . Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 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 . KA2507 exhibits poor oral bioavailability (mice 15%) and C max (mice 300 ng/mL) following oral administration (mice 200 mg/kg) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6 mice, B16-F10 melanoma model Dosage: 100 mg/kg, 200 mg/kg, 200 mg/kg Administration: Oral gavage, daily, for 20 days Result: Demonstrated antitumor efficacy. Animal Model: Male C57BL/6 mice Dosage: 200 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: Oral bioavailability (15%), C max (300 ng/mL). IC50& Target:HDAC6 2.5 nM (IC 50 ) HDAC8 621 (IC 50 )

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