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MBC-11

Cat. No. M21481
MBC-11  Structure
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Biological Activity

MBC-11 is a first-in-class, bone-targeted bisphosphonate conjugate covalently bound to the antimetabolite cytarabine (araC). MBC-11 has the potential to be used in neoplastic bone disease (TIBD).

Chemical Information
Molecular Weight 511.21
Formula C11H20N3O14P3
CAS Number 332863-86-2
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Matthew Winter, et al. J Bone Oncol. A phase IB and randomised phase IIA trial of CApecitabine plus Radium-223 (Xofigo™) in breast cancer patients with BONe metastases: CARBON trial results

[2] Hakeam A Hakeam, et al. Int J Clin Pharm. Tigecycline-induced coagulopathy: a literature review

[3] Mehdi Zandhaghighi, et al. J Infect Dev Ctries. In vitro bactericidal activities of two novel dihydropyridine derivatives against Mycobacterium tuberculosis

[4] Shawn Patrick Zinnen, et al. Oncologist. First-in-Human Phase I Study of MBC-11, a Novel Bone-Targeted Cytarabine-Etidronate Conjugate in Patients with Cancer-Induced Bone Disease

[5] Monica M Reinholz, et al. Bone. A promising approach for treatment of tumor-induced bone diseases: utilizing bisphosphonate derivatives of nucleoside antimetabolites

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