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Raf inhibitor 2 

Cat. No. M29356
Raf inhibitor 2  Structure
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Biological Activity

Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.

Chemical Information
Molecular Weight 429.49
Formula C15H8Br2ClNO2
CAS Number 220904-99-4
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder -20°C
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] Ana Portelinha, et al. Cell Rep Med. ASN007 is a selective ERK1/2 inhibitor with preferential activity against RAS-and RAF-mutant tumors

[2] Savithri Ramurthy, et al. J Med Chem. Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic

[3] Robert Roskoski Jr. Pharmacol Res. Targeting oncogenic Raf protein-serine/threonine kinases in human cancers

[4] R Mandal, et al. Oncogene. Stamping out RAF and MEK1/2 to inhibit the ERK1/2 pathway: an emerging threat to anticancer therapy

[5] Minmin Yu, et al. Bioorg Med Chem. Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma

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  Catalog
Abmole Inhibitor Catalog




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