PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAFV600E in mutant RAS expressing cells. PLX7904 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells.
In vivo, PLX7904 inhibits the COLO205 xenograft growth in eight mice per group.
Cell Experiment | |
---|---|
Cell lines | WM793, WM115, WM9, WM278, WM1346, WM1366, WM1361A, Sbcl2, 1205Lu, A375, SK-MEL 24, SKMEL-2, and SK-MEL 207 cells |
Preparation method | Cells are treated with PLX7904 at different concentrations (0, 0.05, 0.1, 1, 5 μM) for 24 h. Cells are lysed and analyzed by Western blotting with phospho-MEK1/2, total MEK1/2, phospho-ERK1/2 and total ERK1/2 antibodies. |
Concentrations | 0, 0.05, 0.1, 1, 5 μM |
Incubation time | 24 h |
Animal Experiment | |
---|---|
Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 512.53 |
Formula | C24H22F2N6O3S |
CAS Number | 1393465-84-3 |
Solubility (25°C) | DMSO: ≥ 40 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
[1] Zhang C, et al. Nature. RAF inhibitors that evade paradoxical MAPK pathway activation.
Related Raf Products |
---|
Cyclorasin 9A5
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM. |
R18
R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. |
PROTAC RAF degrader 1
PROTAC RAF degrader 1 is a PROTAC RAF degrader. |
B-Raf IN 15
B-Raf IN 15 is a BRAF inhibitor. |
Raf inhibitor 3
Raf inhibitor 3 is a Raf inhibitor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.