U-104 (SLC-0111) 是一种有效的碳酸酐酶 (CA) 抑制剂，作用于 CA IX 和 CA XII，Ki 值分别为 45.1 nM 和 4.5 nM。 U-104 在小鼠模型中显示出显着的肿瘤生长延迟。
| Cas No. | 178606-66-1 |
| 别名 | SLC-0111 |
| 化学名 | 1-(4-fluorophenyl)-3-(4-sulfamoylphenyl)urea |
| Canonical SMILES | C1=CC(=CC=C1NC(=O)NC2=CC=C(C=C2)S(=O)(=O)N)F |
| 分子式 | C13H12FN3O3S |
| 分子量 | 309.32 |
| 溶解度 | ≥ 11.5 mg/mL in DMSO, ≥ 9.14 mg/mL in EtOH with ultrasonic and warming |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.IC50 value: 45.1 nM/4.5 nM(Ki, CA IX/CA XII) [1]Target: Carbonic anhydrase inhibitorin vitro: U-104 (50 μM) 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 in metastatic MDA-MB-231 LM2-4Luc+ cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells [2]. in vivo: U-104 (38 mg/kg) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg) inhibits metastases formation in the 4T1 experimental metastasis mice model [1]. U-104 (38 mg/kg) significantly delay primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells. U-104 (5 mg/mL, oral gavage) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells [2]. References:
[1]. Lou Y, et al. Targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors. Cancer Res. 2011 May 1;71(9):3364-76.
[2]. Lock FE, et al. Targeting carbonic anhydrase IX depletes breast cancer stem cells within the hypoxic niche. Oncogene. 2013 Oct 31;32(44):5210-9. |
