Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KA2507 hydrochloride is a powerful and specific HDAC6 inhibitor, possessing an IC50 value of 2.5 nM. It displays no substantial toxicities while demonstrating significant antitumor efficacy and immune modulatory effects [1].
产品描述 | KA2507 hydrochloride is a powerful and specific HDAC6 inhibitor, possessing an IC50 value of 2.5 nM. It displays no substantial toxicities while demonstrating significant antitumor efficacy and immune modulatory effects [1]. |
体外活性 | KA2507 hydrochloride does not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition. The anti-proliferative effects are only observed at high concentrations of KA2507 hydrochloride, which combines with the increased acetylation of histone H3 suggests that the anti-proliferative effects of KA2507 hydrochloride are attributable to off-target inhibition of class I HDAC as well as HDAC6 [1]. |
体内活性 | 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 C max (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. Animal Model: Male C57BL/6 mice, B16-F10 melanoma model [1] Dosage: 200 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: Oral bioavailability (15%), C max (300 ng/mL). |
分子量 | 358.78 |
分子式 | C16H15ClN6O2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
KA2507 monohydrochloride Inhibitor inhibitor inhibit