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LUT014

Cat. No. M21146
LUT014  Structure
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Quality Control & Documentation
Biological Activity

LUT014, a B-Raf inhibitor with an IC50 value of 11.7 nM, was developed for the study of reducing acne-like lesions associated with EGFR inhibitors at restricted doses.

Chemical Information
Molecular Weight 528.49
Formula C27H19F3N8O
CAS Number 2274819-46-2
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage 2-8°C, protect from light
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] Mario E Lacouture, et al. Cancer Discov. Reducing Skin Toxicities from EGFR Inhibitors with Topical BRAF Inhibitor Therapy

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  Catalog
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