PLX-7904 | B1249

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.

B1249 | PLX-7904 DataSheet

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