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Tubulin inhibitor 36

Cat. No. M41520
Tubulin inhibitor 36 Structure
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Biological Activity

Tubulin inhibitor 36 is a novel and potent tubulin inhibitor and inhibits the polymerization of microtubular protein then induces apoptosis with an IC50 value of 1.5±0.1 μM.

Chemical Information
Molecular Weight 356.83
Formula C16H13ClN6S
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] Hanbing Ning et al. Invest New Drugs. Discovery of oxyepiberberine as a novel tubulin polymerization inhibitor and an anti-colon cancer agent against LS-1034 cells

[2] Hairong Tang et al. Eur J Med Chem. Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy

[3] Michal Jurášek et al. J Steroid Biochem Mol Biol. Estradiol dimer inhibits tubulin polymerization and microtubule dynamics

[4] Ali Fan et al. Eur J Pharm Sci. Pharmacodynamic and pharmacokinetic characteristics of YMR-65, a tubulin inhibitor, in tumor-bearing mice

[5] Maja de Jonge et al. J Clin Oncol. The epothilone dilemma

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