U-104 (SLC-0111) 是一种有效的 CA IX 和 CA XII 碳酸酐酶 (CA) 抑制剂,Ki值分别为 45.1 nM 和 4.5 nM。U-104 在小鼠模型中显示出明显的肿瘤生长延迟。
生物活性 | U-104 (SLC-0111) is a potentcarbonic anhydrase(CA)inhibitor for CA IX andCA XIIwithKivalues of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model[1][2]. |
IC50& Target | Ki: 45.1 nM (CA IX) and 4.5 nM (CA XII)[1] EC50: 0.2 μM (exosome)[3] |
体外研究 (In Vitro) | U-104 (SLC-0111) is a potent exosome inhibitor[3]. U-104 has low inhibition for CA I (Ki=5080 nM) and CA II (Ki=9640 nM)[1]. U-104 (50 μM; for 72 hours) blocks the mesenchymal phenotype in the cancer stem cells population in hypoxia condition of 4T1 cells. U-104 (<50 μm) significantly reduces migration in a dose-dependent manner metastatic mda-mb-231 lm2-4Luc+cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells[2].
|
体内研究 (In Vivo) | U-104 (19, 38 mg/kg; daily; for 27 days) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg; daily; for 5 days) inhibits metastases formation in the 4T1 experimental metastasis mice model[1]. U-104 (38 mg/kg; i.p.; from 11 to 27 days) significantly delays primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+cells[2]. U-104 (50 mg/kg; oral gavage; continuously for 4 days and suspended for 1 day; from 10 to 30 days) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells[2].
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(323.29 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 3.2329 mL | 16.1645 mL | 32.3290 mL | 5 mM | 0.6466 mL | 3.2329 mL | 6.4658 mL | 10 mM | 0.3233 mL | 1.6164 mL | 3.2329 mL |
*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。 In Vivo: 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: ≥ 2.08 mg/mL (6.72 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.72 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.72 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.72 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|