MBC-11
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.
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- CAS No.: 332863-86-2
- Formule: C11H20N3O14P3
- Masse moléculaire:511.21
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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Cell Line:Human multiple myeloma cell lines (KAS-6/1, DP-6, KP-6).
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Concentration:Between 10-8 and 10-4 M.
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Incubation Time:48 hours.
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Result:Significantly inhibited multiple myeloma cell proliferation of each cell line at the majority of the tested concentrations.
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.
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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].
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Dosage:0.04, 0.4, or 4.0 μg/day.
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Administration:S.C. daily from day 7 to 21.
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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.
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Animal Model:Female Balb/c and SCID mice (four-six weeks old)[1].
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Dosage:500, 100, 1, or 0.01 μg/100 μL.
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Administration:S.C. daily for 24 or 49 days.
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Result:Weight gained in MBC-11 treated mice with different doses was similar to the PBS treated group.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 332863-86-2
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Masse moléculaire 511.21
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Formule C11H20N3O14P3
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SMILES
CC(P(O)(O)=O)(P(O)(OP(O)(OC[C@@H]1[C@@H](O)[C@H](O)[C@H](N2C=CC(N)=NC2=O)O1)=O)=O)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MBC-11 Related Classifications
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