U-104
货号：
IU0370
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是碳酸酐酶(Carbonic anhydrase)CA IX和CA XII高效抑制剂。 |
| MDL | MFCD00159265 |
| 别名 | NSC-213841；MST-104 |
| 英文名称 | U-104 |
| CAS | 178606-66-1 |
| 分子式 | C13H12FN3O3S |
| 分子量 | 309.32 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | Solid |
| 单位 | 瓶 |
| 生物活性 | U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model[1-2]. |
| IC50 | Ki: 45.1 nM (CA IX) and 4.5 nM (CA XII)[1]EC50: 0.2 μM (exosome)[3] |
| 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 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 (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]. |
| SMILES | NS(C1=CC=C(NC(NC2=CC=C(F)C=C2)=O)C=C1)(=O)=O |
| 靶点 | Carbonic Anhydrase |
| 数据来源文献 | [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. [3]. Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330. |
| 规格 | 5mg 10mg |