PLX-4720 is a selective BRAFV600E inhibitor with the IC50 values of 160 nM and 130 nM for B-Raf and BRK respectively. PLX-4720 shows remarkable selectivity for BRAF over a panel of 70 protein kinases due to its unusual binding mode, 40 and a similar selectivity is observed for its analogues. PLX-4720 has a BRAF IC50 of 13 nM, and in a panel of melanoma cell lines inhibits ERK activity only in those cell types that harbour the V600E mutation (pERK GI50 14–46 nM) whereas ERK remains unaffected in cells with WTBRAF.
J Nucl Med. 2018 Nov 21.
MEK inhibition induces therapeutic iodine uptake in a murine model of anaplastic thyroid cancer.
PLX-4720 purchased from AbMole
Cell Experiment | |
---|---|
Cell lines | A375, UACC-903, and BRAF wt cell lines |
Preparation method | Cell proliferation assays Cellular proliferation was evaluated by MTT assay (Sigma-Aldrich) following the manufacturer's instructions. Cells were plated in 96-well plates at 1,000 to 10,000 cells per well in 100 μL of media 24 hours after treatment and MTT signal was read at 72 hours after treatment. The IC50 and combination index (CI) by Chou–Talalay (16) were determined from the regression plot logarithm of the concentration versus effect using Calcusyn Software (Biosoft) v1.1. In addition, conservative isobolograms were used to show synergism and/or antagonism. |
Concentrations | 0~10µM |
Incubation time | 72h |
Animal Experiment | |
---|---|
Animal models | Athymic nude mice Nu/Nu (Crl:NU-Foxn1nu) A375, A2058 (BRAF V600E-mutant), and Mel-Juso [BRAF wild-type (WT) and NRAS-mutant] xenograft tumor model |
Formulation | dimethyl sulfoxide (DMSO) |
Dosages | 50 mg/kg everyday |
Administration | intraperitoneal (i.p.) injections |
Molecular Weight | 413.83 |
Formula | C17H14ClF2N3O3S |
CAS Number | 918505-84-7 |
Solubility (25°C) | DMSO 60 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.
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.