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MedKoo product information:
MB 07133
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MedKoo Code#:
201810
Name:
MB 07133
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CAS#:
685111-92-6
Synonym:
MB 07133; CA Index Name:
2(1H)-Pyrimidinone,
4-amino-1-[5-O-[(2R,4S)-2-oxido-4-(4-pyridinyl)-1,3,2-dioxaphosphorinan-2-yl]-.beta.-D-arabinofuranosyl]-;
Other Names: MB 07133
IUPAC/Chemical name:
4-amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-((((2R,4S)-2-oxido-4-(pyridin-4-yl)-1,3,2-dioxaphosphinan-2-yl)oxy)methyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one
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Chemical structure: |
Theoretical analysis
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Chemical Formula: C17H21N4O8P
Exact Mass: 440.10970
Molecular Weight: 440.34
m/z: 440.10970 (100.0%), 441.11306 (18.4%),
442.11395 (1.6%), 442.11641 (1.6%), 441.10674 (1.5%) .
Elemental Analysis: C, 46.37; H, 4.81; N,
12.72; O, 29.07; P, 7.03
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Quality control data:
Product will be shipped with supporting
analytical data.
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Information about this agent
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MB07133 is a novel cytarabine (araC) prodrug that
uses the HepDirect technology to target production of the active
form of araC, araC triphosphate (araCTP), to the liver. In a phase
I/II trial, MB07133 is well tolerated at doses up to
1800 mg/m2/d in pts with unresectable HCC.
Enrollment of a 2400 mg/m2 cohort is ongoing. The disease
stabilization observed in this study, although preliminary,
warrants further investigation in Phase 2. For detail see:
http://meeting.ascopubs.org/cgi/content/abstract/24/18_suppl/2054.
Current developer: Metabasis
Therapeutics, Inc.
1. MacKenna, Deidre A.; Montag, Annika; Boyer, Serge H.; Linemeyer,
David L.; Erion, Mark D. Delivery of high levels of anti-proliferative
nucleoside triphosphates to CYP3A-expressing cells as a potential
treatment for hepatocellular carcinoma. Cancer Chemotherapy and
Pharmacology (2009), 64(5), 981-991.
2. Erion, M. Liver-targeted drug delivery using HepDirect prodrugs.
Microsomes and Drug Oxidations, Proceedings of the International
Symposium, 17th, Saratoga Springs, NY, United States, July 6-10, 2008
(2008), 7-12. CODEN: 69LJBI CAN 150:571747 AN 2009:170765
3. Salonen, Jukka T.; Hyppoenen, Jelena; Kaikkonen, Jari; Pirskanen,
Mia; Uimari, Pekka; Aalto, Juha-Matti. Alleles and polymorphisms
associated with type 2 diabetes mellitus and obesity and their
diagnostic use. PCT Int. Appl. (2007), 456pp. CODEN: PIXXD2 WO
2007128884
4. Boyer, Serge H.; Sun, Zhili; Jiang, Hongjian; Esterbrook, Julie;
Gomez-Galeno, Jorge E.; Craigo, William; Reddy, K. Raja; Ugarkar,
Bheemarao G.; MacKenna, Deidre A.; Erion, Mark D. Synthesis and
Characterization of a Novel Liver-Targeted Prodrug of Cytosine-1- -D-arabinofuranoside
Monophosphate for the Treatment of Hepatocellular Carcinoma. Journal of
Medicinal Chemistry (2006), 49(26), 7711-7720.
5. Avila, M. A.; Berasain, C.; Sangro, B.; Prieto, J. New therapies for
hepatocellular carcinoma. Oncogene (2006), 25(27), 3866-3884.
6. Erion, Mark D.; Van Poelje, Paul D.; MacKenna, Deidre A.; Colby,
Timothy J.; Montag, Annika C.; Fujitaki, James M.; Linemeyer, David L.;
Bullough, David A. Liver-targeted drug delivery using HepDirect prodrugs.
Journal of Pharmacology and Experimental Therapeutics (2005), 312(2),
554-560.
7. Boyer, Serge; Erion, Mark D. Preparation of nucleotides cytarabine
monophosphate prodrugs as antitumor and antiviral agents. U.S. Pat.
Appl. Publ. (2004), 46 pp. CODEN: USXXCO US 2004092476
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