IMD-0354 (IKK2 Inhibitor V) is a selectiveIKKβinhibitor which inhibitsNF-κBactivity^[1]. IMD0354 inhibits TNF-α inducedNF-κBtranscription activity with anIC₅₀of 1.2 uM^[2].

IMD-0354 inhibits NF-κB activity in HMC-1 cells, resulting in complete repression of growth factor-independent proliferation of mast cells. When the DNA-binding activity of NF-κB is inhibited by treatment with IMD-0354, cell proliferation is completely suppressed. HMC-1 cells are incubated with increasing concentrations of IMD-0354 or STI571 for 24, 48, and 72 hours, and numbers and viability of cells are determined by a dye exclusion test and an MTT assay. IMD-0354 suppresses cell proliferation in a time- and dose-dependent manner. The inhibitory effect of IMD-0354 is remarkable, even at lower concentrations, when compared with that of STI571^[1]. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC₅₀of 1.2±0.3 uM^[2].

Daily administration with 5 mg/kg IMD-0354 significantly suppresses tumor expansion in nude mice implanted with established MDA-MB-231 tumors. In mice treated with IMD-0354, tumor progression is restrained^[3]. The number of infiltrating cells in aqueous humor is 53.6±9.8×10⁵, 72.5±17.0×10⁵, 127.25±32.0×10⁵, and 132.0±25.0×10⁵cells/mL in rats treated with 30, 10, 3, or 0 mg/kg of IMD-0354, respectively. The total protein concentrations of aqueous humor are 92.6±3.1 mg/mL, 101.5±6.8 mg/mL, 112.6±1.9 mg/mL, and 117.33±1.8 mg/mL in rats treated with 30, 10, 3, and 0 mg/kg of IMD-0354, respectively^[4].

383.67

Solid

C₁₅H₈ClF₆NO₂

978-62-1

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(260.64 mM)

H₂O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

*"≥" 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 (6.52 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.52 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
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 2.5 mg/mL (6.52 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.52 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明