Carbonic Anhydrase IX/XII Inhibitor II(U-104)
Carbonic Anhydrase IX/XII Inhibitor II(U-104) Basic information
- Product Name:
- Carbonic Anhydrase IX/XII Inhibitor II(U-104)
- Synonyms:
-
- NSC 213841
- Carbonic Anhydrase IX/XII Inhibitor II(U-104)
- U-104
- MST-104
- 4-[[[(4-Fluorophenyl)amino]carbonyl]amino]benzenesulfonamide
- CS-1653
- arbonic Anhydrase IX/XII Inhibitor II(U-104)
- NSC-213841; MST-104;U104;U 104
- CAS:
- 178606-66-1
- MF:
- C13H12FN3O3S
- MW:
- 309.32
- Product Categories:
-
- Inhibitors
- Inhibitor
- Mol File:
- 178606-66-1.mol
Carbonic Anhydrase IX/XII Inhibitor II(U-104) Chemical Properties
- Melting point:
- 242-243℃
- Density
- 1.523±0.06 g/cm3 (20 ºC 760 Torr)
- storage temp.
- 2-8°C
- solubility
- DMSO: >15mg/mL
- form
- powder
- pka
- 9.94±0.12(Predicted)
- color
- white to beige
- biological source
- rabbit
Carbonic Anhydrase IX/XII Inhibitor II(U-104) Usage And Synthesis
Chemical Properties
White to Light yellow powder to crystal.
Uses
U 104 targets hypoxia-induced carbonic anhydrase IX, which inhibits tumor growth and metastasis.
Biological Activity
u-104 is a novel ureido-sulfonamide inhibitor of carbonic anhydrase ix (caix). 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.yuanmei lou, paul c. mcdonald, arusha oloumi, stephen chia, christina ostlund, ardalan ahmadi, alastair kyle, ulrich auf dem keller, samuel leung, david huntsman, blaise clarke, brent w. sutherland, dawn waterhouse, marcel bally, calvin roskelley, christopher m. overall, andrew minchinton, fabio pacchiano, fabrizio carta, andrea scozzafava, nadia touisni, jean-yves winum, claudiu t. supuran, shoukat dedhar. targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase ix inhibitors. cancer research may 1, 2011 71; 3364
Biochem/physiol Actions
U-104 is an inhibitor of CA IX that binds only to CA IX under hypoxic conditions in vivo. The binding results in significant inhibition of tumor growth and metastasis formation in both spontaneous and experimental models of metastasis. U-104 reduces the medium acidity by inhibiting the catalytic activity of the CA IX. It binds specifically only to hypoxic cells expressing CA IX.
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].
IC 50
CA XII; CA Ⅸ
References
[1] YUANMEI LOU. Targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors.[J]. Cancer research, 2011, 71 9: 3364-3376. DOI:10.1158/0008-5472.CAN-10-4261.
[2] MIGLĖ PAŠKEVIČIŪTĖ Vilma P. Application of carbonic anhydrase inhibitors to increase the penetration of doxorubicin and its liposomal formulation into 2D and 3D triple negative breast cancer cell cultures.[J]. American journal of cancer research, 2020, 10 6: 1761-1769.
[3] TIMOTHY A DINH. Hotspots of Aberrant Enhancer Activity in Fibrolamellar Carcinoma Reveal Candidate Oncogenic Pathways and Therapeutic Vulnerabilities.[J]. Cell reports, 2020, 31 2: 107509. DOI:10.1016/j.celrep.2020.03.073.
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