KA2507 是一种高效的，具有口服活性的、选择性的 HDAC6 抑制剂， 其 IC₅₀ 值为 2.5 nM。KA2507 在临床前模型中表现出抗肿瘤活性和免疫调节作用。

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.

Solid

HDAC6 2.5 nM (IC50) HDAC8 621 (IC50

KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition.
has not independently confirmed the accuracy of these methods. They are for reference only.

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).
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Apostolia M Tsimberidou, et al. Preclinical Development and First-in-Human Study of KA2507, a Selective and Potent Inhibitor of Histone Deacetylase 6, for Patients with Refractory Solid Tumors. Clin Cancer Res. 2021 May 4.

In Vitro: DMSO : 66.67 mg/mL (206.84 mM; Need ultrasonic)配制储备液