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      U-104
      U-104

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0895
      CAS #: 178606-66-1Purity ≥98%

      Description: U-104 (also known as MST-104, SLC-0111 and NSC 213841) is a novel and potent inhibitor of transmembrane carbonic anhydrase (CA) with Ki of 45.1 nM and 4.5 nM for CA IX and CA XII, respectively, it has very low inhibition for CA I and CA II. Tumor volume measurements show important inhibition of primary tumor growth in the mice treated with the U-104 compound compared with vehicle controls. It also has ability to inhibit metastasis formation in the 4T1 experimental metastasis model. 

      References: Cancer Res. 2011 May 1;71(9):3364-76; Oncogene. 2013 Oct 31;32(44):5210-9.

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      Molecular Weight (MW)309.32
      FormulaC13H12FN3O3S
      CAS No.178606-66-1
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 62 mg/mL (200.4 mM)
      Water: < 1 mg/mL
      Ethanol: < 1 mg/mL
      Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
      SynonymsMST-104, SLC0111; SLC 0111; U-104; NSC 213841; MST104;  MST 104; NSC-213841; NSC213841; SLC-0111; U104; U 104.


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      In Vitro

      In vitro activity: 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. U-104 possesses aromatic groups at the second nitrogen ureido group.

      Cell Assay: 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.

      In VivoU-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. 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.
      Animal modelBalb/c mice orthotopically implanted with 4T1 cells.
      Formulation & DosageDissolved in 55.6% PEG 400, 11.1% ethanol and 33% water; 5 mg/kg; oral gavage
      ReferencesCancer Res. 2011 May 1;71(9):3364-76; Oncogene. 2013 Oct 31;32(44):5210-9.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      U-104

      The metastatic 4T1 primary tumor is a valid preclinical model of hypoxia-induced CAIX expression. Cancer Res. 2011 May 1;71(9):3364-76. 
      		 

      U-104

      Silencing CAIX expression in metastatic 4T1 cells inhibits cell survival and alters pHe in hypoxia. Cancer Res. 2011 May 1;71(9):3364-76.  
      		 

      U-104

      Growth of primary breast tumors characterized by hypoxia requires the expression of CAIX. Cancer Res. 2011 May 1;71(9):3364-76. 
       

      U-104

      Inhibition of CAIX expression or activity attenuates metastasis of 4T1 mouse mammary tumors. Cancer Res. 2011 May 1;71(9):3364-76. 
      		 

      U-104

      Targeting CAIX activity with selective small molecule inhibitors of CAIX attenuates the growth of mouse and human breast tumors. Cancer Res. 2011 May 1;71(9):3364-76. 
      		 

      U-104

      Novel selective small molecule inhibitors of CAIX inhibit metastasis formation by 4T1 mammary tumor cells. Cancer Res. 2011 May 1;71(9):3364-76. 

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