PLX4720 | Mutant B-Raf inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $55.00 | ||
| 25 mg | $145.00 |
PLX4720 (918505-84-7) is a potent and selective inhibitor of B-Raf, V600E mutant, IC50=13 nM (Wild type IC50=160 nM).1 It induces cell cycle arrest and apoptosis in B-RafV600E-positive cells and suppresses growth of B-RafV600E-positive xenografts.1 It induces tumor regression and reverses cachexia in a mouse model of human thyroid cancer harboring the B-RafV600E mutation.2 Early stage autophagy inhibitors and ER stress inhibition with 4-phenylbutyric acid increases the sensitivity of resistant cells to PLX4720.3 PLX4720 induces cytoprotective autophagy in thyroid cancer cells via AMPK-ULK1 pathway.4
References/Citations:
- Tsai et al. (2008), Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity; Proc. Natl. Acad. Sci. USA, 105 3041
- Nehs et al. (2012), Late intervention with anti-BRAF(V600E) therapy induces tumor regression in an orthotopic mouse model of human anaplastic thyroid cancer; Endocrinology, 153 985
- Yeom et al. (2021), Increase in the sensitivity to PLX4720 through inhibition of transcription factor EB-dependent autophagy in BRAF inhibitor-resistant cells; Toxicol. Res., 38 35
- Jimenez-Morah et al. (2021), V600EBRAF Inhibition Induces Cytoprotective Autophagy through AMPK in Thyroid Cancer Cells; Int. J. Mol. Sci. 22 6033
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
PLX4720 (918505-84-7) is a potent and selective inhibitor of B-Raf, V600E mutant, IC50=13 nM (Wild type IC50=160 nM).1 It induces cell cycle arrest and apoptosis in B-RafV600E-positive cells and suppresses growth of B-RafV600E-positive xenografts.1 It induces tumor regression and reverses cachexia in a mouse model of human thyroid cancer harboring the B-RafV600E mutation.2 Early stage autophagy inhibitors and ER stress inhibition with 4-phenylbutyric acid increases the sensitivity of resistant cells to PLX4720.3 PLX4720 induces cytoprotective autophagy in thyroid cancer cells via AMPK-ULK1 pathway.4
References/Citations:
- Tsai et al. (2008), Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity; Proc. Natl. Acad. Sci. USA, 105 3041
- Nehs et al. (2012), Late intervention with anti-BRAF(V600E) therapy induces tumor regression in an orthotopic mouse model of human anaplastic thyroid cancer; Endocrinology, 153 985
- Yeom et al. (2021), Increase in the sensitivity to PLX4720 through inhibition of transcription factor EB-dependent autophagy in BRAF inhibitor-resistant cells; Toxicol. Res., 38 35
- Jimenez-Morah et al. (2021), V600EBRAF Inhibition Induces Cytoprotective Autophagy through AMPK in Thyroid Cancer Cells; Int. J. Mol. Sci. 22 6033
Related products
-
AZ3146 | Mps1 kinase inhibitor
From $60.00CAS:1124329-14-1Catalog Number:10-4778Activity:Mps1 kinase inhibitorChemical Name:9-Cyclopentyl-2-[2-methoxy-4-(1-methylpiperidine-4-yl)oxyanilino]-7-methylpurin-8-oneMolecular Weight:452.56Molecular Formula:C24H32N6O3S2Solubility:Soluble in DMSO (up to 10 mg/ml) or in Ethanol (up to at least 25 mg/ml)Physical Properties:Off-white solidPurity:98% by HPLC
NMR (Conforms)Storage Temperature:-20°Stability:Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.Shipping Code:RT -
PNU 74654 | Wnt pathway blocker
From $55.00CAS:113906-27-7Catalog Number:10-4519Activity:Wnt pathway blockerChemical Name:2-Phenoxybenzoic acid [(5-methyl-2-furanyl)methylene]hydrazideMolecular Weight:320.35Molecular Formula:C19H16N2O3Solubility:Soluble in DMSO (up to 25 mg/ml).Physical Properties:Off-white solidPurity:>98% by TLC
NMR (conforms)Storage Temperature:-20°Stability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.Shipping Code:RT
Calculate the molar concentration, mass or volume in a solution.
Concentration × Volume × Molecular Weight = Mass
