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product name U-104


Description: U-104, also known as MST-104 and NSC 213841, is a novel and potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM, 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.



Molecular Weight (MW)

309.32
Formula

C13H12FN3O3S
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
Synonyms

MST-104, NSC 213841

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19404555

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.


Kinase Assay:


Cell Assay

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

GNE-140 (racemate)

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Author: Sodium channel

Share this post on:

product name U-104


Description: U-104, also known as MST-104 and NSC 213841, is a novel and potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM, 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.



Molecular Weight (MW)

309.32
Formula

C13H12FN3O3S
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
Synonyms

MST-104, NSC 213841

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19404555

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.


Kinase Assay:


Cell Assay

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

GNE-140 (racemate)

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Author: Sodium channel