Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class selective B-RAF inhibitor that inhibits the activity of RAFV600E and c-RAF-1 with IC50 at 31 nM and 48 nM, respectively. Vemurafenib can induce autophagy.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Related Raf Products|
Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class selective B-RAF inhibitor that inhibits the activity of RAFV600E and c-RAF-1 with IC50 at 31 nM and 48 nM, respectively.
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.
GNE-9815 is one of the most selective kinase inhibitors of RAF, targeting KRAS mutant cancers by combination of drugs.
|B-Raf inhibitor 1 (Compound 13) dihydrochloride
B-Raf inhibitor 1 (Compound 13) is a type IIA Raf inhibitor which bind to the DFG-out conformation with ki of 1 nM,1 nM,and 0.3 nM for B-Raf(WT), B-Raf(V600E) and C-Raf, respectively.
|Belvarafenib (GDC5573, HM95573, RG6185)
Belvarafenib (GDC5573, HM95573, RG6185) is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively.
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