Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) withIC₅₀s of 0.9, 0.9, 1.2 μM for recombinantHDAC1, 2 and 3 respectively.

Tacedinaline (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinical models. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. Tacedinaline (N-acetyldinaline) is combined with antineoplastic agents commonly used in non-small cell lung cancer cell line management, a marked synergism of action (R=1.8, R=1.5) is observed between Tacedinaline (N-acetyldinaline) (40 μM) and gemcitabine (0.01 μM) at 48 and 72 h of treatment^[2]. Tacedinaline (N-acetyldinaline) inhibits mitogen-stimulated blood lymphocyte proliferation with an IC₅₀value of 3 μM^[4].

Tacedinaline (CI-994) has activity against 8/8 solid tumors tested: pancreatic ductal adenocarcinoma #02 (4.7); pancreatic adenocarcinoma #03 (3.0; 1/6 cures); colon adenocarcinoma #38 (1.6); colon adenocarcinoma #51/A (1.1); mammary adenocarcinoma #25 (1.7); mammary adenocarcinoma #17/ADR (0.5); Dunning osteogenic sarcoma (4.0); and the human prostate carcinoma LNCaP (1.2). CI-994 is the acetylated metabolite of dinaline and has the same spectrum of activityin vivoas dinaline. It also behaves similarly in schedule comparison/toxicity trials^[3]. Tacedinaline (CI-994) can effect lymphoid tissue in rats within 1 day of a single oral dose, that effects are generally reversible within 7 days^[4].

269.30

Solid

C₁₅H₁₅N₃O₂

112522-64-2

乙酰地那林；他地那兰

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL(185.67 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (9.28 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (9.28 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液