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Alternative_name
5-(2-Cyclopropylpyrimidin-5-yl)-3-[3-[[ethyl(methyl)sulfamoyl]amino]-2,6-difluorobenzoyl]-1H-pyrrolo[2,3-b]pyridine
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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.
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CAS Number
1393465-84-3
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Structure Available
Yes
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Salt Form
No
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Molecular Formula
C₂₄H₂₂F₂N₆O₃S
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Molecular Weight
512.54
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Cell Permeable
Yes
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Purity
≥98% by HPLC
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Solubilities
DMSO(>5 mg/ml)
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Handling
Protect from air and light
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Tag Line
A potent and selective paradox-breaker RAF inhibitor.
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Storage Condition
-20°C
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Shipping Condition
gel pack
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Shelf Life
36 months
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PubChem CID
90116945
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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
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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)
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InChi Key
DKNZQPXIIHLUHU-UHFFFAOYSA-N
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MSDS Available
Yes
