| Identification | Back Directory | [Name]
2(1H)-Pyrimidinone, 4-amino-1-[5-O-(1,3,4,5,5-pentahydroxy-4-methyl-1,3,5-trioxido-2-oxa-1,3,5-triphosphapent-1-yl)-β-D-arabinofuranosyl]- | [CAS]
332863-86-2 | [Synonyms]
MBC-11
2(1H)-Pyrimidinone, 4-amino-1-[5-O-(1,3,4,5,5-pentahydroxy-4-methyl-1,3,5-trioxido-2-oxa-1,3,5-triphosphapent-1-yl)-β-D-arabinofuranosyl]- | [Molecular Formula]
C11H20N3O14P3 | [MDL Number]
MFCD28502828 | [MOL File]
332863-86-2.mol | [Molecular Weight]
511.21 |
| Hazard Information | Back Directory | [Uses]
MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 has the potential for tumor-induced bone disease (TIBD) research[1]. | [in vivo]
MBC-11 (0.04 μg/day, s.c.) has a lower incidence of bone metastases of 40% compared to those treated with PBS (90%) or 0.04 μg/day zoledronate (100%). MBC-11 also significantly decreases bone tumor burden compared to PBS- or zoledronate-treated mice[1].
Weight gained in mice treated with up to 500 μg/day of MBC-11 is similar to the PBS treated group[1].
These results demonstrate that MBC-11 decreases bone tumor burden, maintains bone structure, and may increase overall survival, warranting further investigation as a treatment for tumor-induced bone disease (TIBD)[1]. | Animal Model: | Approximately four-week old female Balb/c mice inoculated (s.c. injection into their mammary fatpads) with 500,000 4T1/luc cells at day 0 (breast tumor model)[1]. | | Dosage: | 0.04, 0.4, or 4.0 μg/day. | | Administration: | S.C. daily from day 7 to 21. | | Result: | The dose of 0.04 μg/day had a lower incidence of bone metastases compared to those treated with PBS or 0.04 μg/day zoledronate. |
| Animal Model: | Female Balb/c and SCID mice (four-six weeks old)[1]. | | Dosage: | 500, 100, 1, or 0.01 μg/100 μL. | | Administration: | S.C. daily for 24 or 49 days. | | Result: | Weight gained in MBC-11 treated mice with different doses was similar to the PBS treated group. |
| [References]
[1] Reinholz MM, et al. A promising approach for treatment of tumor-induced bone diseases: utilizing bisphosphonate derivatives of nucleoside antimetabolites. Bone. 2010 Jul;47(1):12-22. DOI:10.1016/j.bone.2010.03.006
[2] Zinnen SP, et al. First-in-Human Phase I Study of MBC-11, a Novel Bone-Targeted Cytarabine-Etidronate Conjugate in Patients with Cancer-Induced Bone Disease. Oncologist. 2019 Mar;24(3):303-e102. DOI:10.1634/theoncologist.2018-0707 |
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MedChemExpress
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021-58955995 |
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www.medchemexpress.com |
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