化合物KA2507 T9148

Product Introduction
Bioactivity


英文名: KA2507

描述: 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。

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

体内活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (186.15 mM)


关键字: KA2507 | KA 2507 | modulatory | KA-2507 | colorectal | Histone deacetylases | immune | cancer | antitumor | Inhibitor | melanoma | HDAC | inhibit

相关产品: CRA-026440 | GK444 | Citarinostat | RTS-V5 | HFY-4A | CAY10603 | Entinostat | HDAC-IN-5 | AES-135 | BRD2492

相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | NF-κB Signaling Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Orally Active Compound Library | Histone Modification Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途