ChemicalBook CAS DataBase List 332863-86-2

332863-86-2

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
Molecular Formula	C11H20N3O14P3
MDL Number	MFCD28502828
Molecular Weight	511.21
MOL File	332863-86-2.mol

Chemical Properties

Boiling point	880.1±75.0 °C(Predicted)
density	2.32±0.1 g/cm3(Predicted)
pka	1.14±0.50(Predicted)

Hazard Information

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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