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Laulimalide

Cat. No. M10844
Laulimalide Structure
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Biological Activity

Laulimalide is an Microtubule stabilizing agent. Laulimalide is a potent inhibitor of cellular proliferation in cancer cell lines (IC50 reported to be 3-30 nM, dependent on cell line used). Laulimalide causes cells to arrest in the prometaphase of the cell cycle, prevents formation of bipolar spindle and increases kinetochore tension in preformed spindles.

Chemical Information
Molecular Weight 514.65
Formula C30H42O7
CAS Number 115268-43-4
Solubility (25°C) DMSO ~10 mg/mL
Storage -20°C, 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] Cassandra D M Churchill, et al. Chem Biol Drug Des. The Unique Binding Mode of Laulimalide to Two Tubulin Protofilaments

[2] Megha Bajaj, et al. PLoS One. Laulimalide induces dose-dependent modulation of microtubule behaviour in the C. elegans embryo

[3] Melissa M Gajewski, et al. Pharm Res. Peloruside, laulimalide, and noscapine interactions with beta-tubulin

[4] Erin A Clark, et al. Mol Pharm. Laulimalide and synthetic laulimalide analogues are synergistic with paclitaxel and 2-methoxyestradiol

[5] S L Mooberry, et al. Cancer Res. Laulimalide and isolaulimalide, new paclitaxel-like microtubule-stabilizing agents

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Keywords: Laulimalide supplier, Microtubule, inhibitors, activators


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