KA2507 是一种具有口服活性的选择性HDAC6抑制剂， 其IC50值为 2.5 nM。它有抗肿瘤活性和免疫调节作用。

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

At concentrations selective for HDAC6 inhibition, KA2507 did not inhibit in vitro proliferation of mouse or human cancer cells.

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 Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg).[1]

1636894-46-6

C16H14N6O2

322.328

DMSO:60 mg/mL (186.15 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years