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Tubulin inhibitor 35

Cat. No. M41525
Tubulin inhibitor 35 Structure
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Biological Activity

Tubulin inhibitor 35 is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM).

Chemical Information
Molecular Weight 331.41
Formula C21H21N3O
CAS Number 2247047-77-2
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] Ruoli Bai et al. Arch Biochem Biophys. The interaction of spongistatin 1 with tubulin

[2] Hossein Borghaei et al. J Clin Oncol. Five-Year Outcomes From the Randomized, Phase III Trials CheckMate 017 and 057: Nivolumab Versus Docetaxel in Previously Treated Non-Small-Cell Lung Cancer

[3] Naoki Takegawa et al. Int J Cancer. DS-8201a, a new HER2-targeting antibody-drug conjugate incorporating a novel DNA topoisomerase I inhibitor, overcomes HER2-positive gastric cancer T-DM1 resistance

[4] No authors listed. Drugs R D. Brentuximab vedotin

[5] William N Hait et al. Cancer Chemother Biol Response Modif. Tubulin-targeting agents

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