A RAF inhibitor
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PLX7904

Item No. 20710

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N'-[3-[[5-(2-cyclopropyl-5-pyrimidinyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-N-ethyl-N-methyl-sulfamide
CAS Number
1393465-84-3
Molecular Formula
C24H22F2N6O3S
Formula Weight
512.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: >5mg/ml
λmax
258, 305 nm
SMILES
O=C(C1=C(F)C(NS(N(CC)C)(=O)=O)=CC=C1F)C2=CNC(C2=C3)=NC=C3C4=CN=C(C5CC5)N=C4
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $183

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    10 mg

    $303

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    25 mg

    $653

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    Product Description

    PLX7904 is a RAF inhibitor (IC50s = 2.4, 140, and 91 nM for mutant B-RAFV600E, wild-type B-RAF, and C-RAF, respectively).1 It inhibits phosphorylation of ERK in A375 and COLO 829 cells (IC50s = 16 and 18 nM, respectively). Unlike PLX4032 (Item No. 10618), BAY 43-9006 (Item No. 10009644), and dabrafenib (Item No. 16989), PLX7904 does not induce paradoxical pERK activation and proliferation of cancer cell lines (EC50s = >200 μM). PLX7904 (25 mg/kg twice per day) inhibits tumor growth in a mouse COLO 205 colon cancer xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, C., Spevak, W., Zhang, Y., et al. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature 526(7574), 583-586 (2015).