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Verubulin hydrochloride

Cat. No. M30904
Verubulin hydrochloride Structure
Synonym:

MPC-6827 hydrochloride

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Biological Activity

Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types.

Chemical Information
Molecular Weight 315.8
Formula C17H18ClN3O
CAS Number 917369-31-4
Form Solid
Solubility (25°C) DMSO 62.5 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, dry, sealed
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] Anton Lindberg, et al. Front Neurosci. Preliminary Evaluations of [11C]Verubulin: Implications for Microtubule Imaging With PET

[2] Wenlong Li, et al. Bioorg Chem. Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain

[3] Marc C Chamberlain, et al. J Neurooncol. A phase 2 trial of verubulin for recurrent glioblastoma: a prospective study by the Brain Tumor Investigational Consortium (BTIC)

[4] Katharina Mahal, et al. ChemMedChem. Effects of the tumor-vasculature-disrupting agent verubulin and two heteroaryl analogues on cancer cells, endothelial cells, and blood vessels

[5] Kenneth F Grossmann, et al. J Neurooncol. Phase I trial of verubulin (MPC-6827) plus carboplatin in patients with relapsed glioblastoma multiforme

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