产品描述: | 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 |
靶点: |
Ki: 45.1 nM (CA IX) and 4.5 nM (CA XII) EC50: 0.2 μM (exosome);CarbonicAnhydrase |
体内研究: |
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. 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. 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. |
参考文献: |
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. |
溶解性: |
DMSO : ≥ 100 mg/mL (323.29 mM) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.233 ml |
16.164 ml |
32.329 ml |
5 mM |
0.647 ml |
3.233 ml |
6.466 ml |
10 mM |
0.323 ml |
1.616 ml |
3.233 ml |
50 mM |
0.065 ml |
0.323 ml |
0.647 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |