Description
PLX7904 is a potent and selective paradox-breaker RAF inhibitor. PLX7904 efficiently inhibits activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Importantly, it inhibits ERK1/2 phosphorylation in mutant BRAF melanoma cells with acquired resistance to Vemurafenib/PLX4720 that is mediated by a secondary mutation in NRAS. Consistent with ERK1/2 reactivation driving the re-acquisition of malignant properties, PLX7904 promotes apoptosis and inhibits entry into S phase and anchorage-independent growth in mutant N-RAS-mediated Vemurafenib-resistant cells.
PLX7904 is a potent and selective paradox-breaker RAF inhibitor. PLX7904 efficiently inhibits activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.
Alternate Name/Synonyms: 5-(2-Cyclopropylpyrimidin-5-yl)-3-[3-[[ethyl(methyl)sulfamoyl]amino]-2,6-difluorobenzoyl]-1H-pyrrolo[2,3-b]pyridine
Appearance: Off white to brown solid
Formulation: N/A
CAS Number: 1393465-84-3
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₂₄H₂₂F₂N₆O₃S
Molecular Weight: 512.54
Cell-Permeable?: Yes
Purity: ≥98% by HPLC
Solubilities: DMSO(>5 mg/ml)
Handling: Protect from air and light
Country of Origin: USA
Tag Line: A potent and selective paradox-breaker RAF inhibitor.
MDL Number: N/A
PubChem CID: 90116945
SMILES: O=C(C1=CNC2=NC=C(C3=CN=C(C4CC4)N=C3)C=C21)C5=C(F)C=CC(NS(=O)(N(CC)C)=O)=C5F
InChi: InChI=1S/C24H22F2N6O3S/c1-3-32(2)36(34,35)31-19-7-6-18(25)20(21(19)26)22(33)17-12-30-24-16(17)8-14(9-29-24)15-10-27-23(28-11-15)13-4-5-13/h6-13,31H,3-5H2,1-2H3,(H,29,30)
InChi Key: DKNZQPXIIHLUHU-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |