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Tubulysin

Cat. No. M19969
Tubulysin  Structure
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Biological Activity

Tubulysin family are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis, and are potent microtubule destabilizing agents.

Chemical Information
Molecular Weight 842.10
Formula C44H67N5O9S
CAS Number 1943604-24-7
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] K C Nicolaou, et al. J Org Chem. Design, Synthesis, and Biological Evaluation of Tubulysin Analogues, Linker-Drugs, and Antibody-Drug Conjugates, Insights into Structure-Activity Relationships, and Tubulysin-Tubulin Binding Derived from X-ray Crystallographic Analysis

[2] Joseph Z Hamilton, et al. ChemMedChem. Improving Antibody-Tubulysin Conjugates through Linker Chemistry and Site-Specific Conjugation

[3] Bohua Long, et al. Org Biomol Chem. Total synthesis of tubulysin U and N14-desacetoxytubulysin H

[4] Thimmalapura M Vishwanatha, et al. Org Lett. Tubulysin Synthesis Featuring Stereoselective Catalysis and Highly Convergent Multicomponent Assembly

[5] Joel R Courter, et al. Bioorg Med Chem Lett. Structure-activity relationships of tubulysin analogues

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