[CAS NO. 387877-45-4] MBC-11 trisodium
PRODUCTS SPECIFICATIONS [387877-45-4]
DESCRIPTION [387877-45-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 577.15 |
| Molecular Formula | C11H17N3Na3O14P3 |
| SMILES | CC(P(O[Na])(O[Na])=O)(P(OP(O)(OC[C@@H]1[C@@H](O)[C@H](O)[C@H](N2C=CC(N)=NC2=O)O1)=O)(O[Na])=O)O |
Summary
MBC-11 trisodium is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C. MBC-11 trisodium has the potential for tumor-induced bone disease (TIBD) research [1] .
In Vitro
MBC-11 shows similar activity profiles and significantly inhibits growth of all three cell lines between 10 -8 and 10 -4 M. MBC-11 decreases KAS-6/1 cell growth from approximately 56% at 10 -8 M to 6% at 10 -5 M [1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | Human multiple myeloma cell lines (KAS-6/1, DP-6, KP-6). |
| Concentration: | Between 10 -8 and 10 -4 M. |
| Incubation Time: | 48 hours. |
| Result: | Significantly inhibited multiple myeloma cell proliferation of each cell line at the majority of the tested concentrations. |
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]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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: | 47% of 17 mice treated with MBC-11 had detectable bone metastases. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02673060 | Osteros Biomedica Ltd |
Bone Metastasis
|
July 2014 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
H 2 O : 125 mg/mL ( 216.58 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7327 mL | 8.6633 mL | 17.3265 mL |
| 5 mM | 0.3465 mL | 1.7327 mL | 3.4653 mL |
| 10 mM | 0.1733 mL | 0.8663 mL | 1.7327 mL |
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.
- [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.
