A B-Raf inhibitor
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L-779,450

Item No. 17807

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-imidazol-5-yl]-phenol
CAS Number
303727-31-3
Synonyms
  • Raf Kinase Inhibitor IV
Molecular Formula
C20H14ClN3O
Formula Weight
347.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMF:PBS (pH 7.2); (1:7): 0.12 mg/mLDMSO: 30 mg/mLEthanol: 2 mg/mL
λmax
251, 295 nm
SMILES
OC1=CC(C(N2)=C(C3=CC=NC=C3)N=C2C4=CC=CC=C4)=CC=C1Cl
InChi Code
InChI=1S/C20H14ClN3O/c21-16-7-6-15(12-17(16)25)19-18(13-8-10-22-11-9-13)23-20(24-19)14-4-2-1-3-5-14/h1-12,25H,(H,23,24)
InChi Key
WXJLXRNWMLWVFB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

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    50 mg

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    Product Description

    L-779,450 is an ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that displays >7, >30, and >70-fold selectivity over p38α, GSK3β, and Lck, respectively.1 It has been shown to inhibit cell proliferation both in B-Raf mutated and wild-type melanoma cell lines, as well as to enhance tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis in these cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takle, A.K., Brown, M.B., Savies, S., et al. The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase. Bioorg. Med. Chem. Lett. 18(15), 4373-4376 (2008).

    2. Berger, A., Quast, S.A., Plötz, M., et al. RAF inhibition overcomes resistance to TRAIL-induced apoptosis in melanoma cells. J. Invest. Dermatol. 134(2), 430-440 (2014).