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BRAF inhibitor 

Cat. No. M30908
BRAF inhibitor  Structure
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Biological Activity

BRAF inhibitor is a B-Raf inhibitor.

Chemical Information
Molecular Weight 456.47
Formula C22H18F2N4O3S
CAS Number 918505-61-0
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
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] Kelli-Ann Monaco, et al. Clin Cancer Res. LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors

[2] Qing-Shan Li, et al. Anticancer Agents Med Chem. Promising Strategies for Overcoming BRAF Inhibitor Resistance Based on Known Resistance Mechanisms

[3] Sascha Dietrich, et al. Best Pract Res Clin Haematol. BRAF inhibitor therapy in HCL

[4] Erick J Morris, et al. Cancer Discov. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors

[5] Paolo A Ascierto, et al. J Transl Med. The role of BRAF V600 mutation in melanoma

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  Catalog
Abmole Inhibitor Catalog




Keywords: BRAF inhibitor  supplier, Raf, inhibitors, activators


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