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MU380 

Cat. No. M29247
MU380  Structure
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Biological Activity

MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity.

Chemical Information
Molecular Weight 430.23
Formula C15H15BrF3N7
CAS Number 2109805-78-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] A Mickova, et al. Klin Onkol. Advantages and limitations of 3D organoids and ex vivo tumor tissue culture in personalized medicine for prostate cancer

[2] Stanislav Drápela, et al. Mol Oncol. The CHK1 inhibitor MU380 significantly increases the sensitivity of human docetaxel-resistant prostate cancer cells to gemcitabine through the induction of mitotic catastrophe

[3] Miroslav Boudny, et al. Haematologica. Novel CHK1 inhibitor MU380 exhibits significant single-agent activity in TP53-mutated chronic lymphocytic leukemia cells

[4] Pounami Samadder, et al. Mol Cancer Ther. Synthesis and Profiling of a Novel Potent Selective Inhibitor of CHK1 Kinase Possessing Unusual N-trifluoromethylpyrazole Pharmacophore Resistant to Metabolic N-dealkylation

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  Catalog
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Keywords: MU380  supplier, Checkpoint, inhibitors, activators


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