A c-Met inhibitor
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PF-04217903

Item No. 17931

Technical Information
Formal Name
4-[1-(6-quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol
CAS Number
956905-27-4
Molecular Formula
C19H16N8O
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 1 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2)(1:8): 0.1 mg/ml
λmax
226, 315, 346 nm
SMILES
OCCN(N=C1)C=C1C2=CN=C3C(N(CC4=CC=C5C(C=CC=N5)=C4)N=N3)=N2
InChi Code
InChI=1S/C19H16N8O/c28-7-6-26-12-15(9-22-26)17-10-21-18-19(23-17)27(25-24-18)11-13-3-4-16-14(8-13)2-1-5-20-16/h1-5,8-10,12,28H,6-7,11H2
InChi Key
PDMUGYOXRHVNMO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PF-04217903 is an inhibitor of c-Met (Ki = 4.8 nM).1 It is greater than 1,000-fold selective for c-Met over a panel of 150 kinases. PF-04217903 inhibits the proliferation of and induces apoptosis in GTL-16 gastric carcinoma cells (IC50s = 12 and 31 nM, respectively) as well as inhibits migration of NCI H441 lung cancer cells induced by hepatocyte growth factor (HGF; IC50 = 11 nM). It reduces tumor growth in a GTL-16 mouse xenograft model when administered at doses ranging from 1 to 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zou, H.Y., Li, Q., Lee, J.H., et alSensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor. Mol. Cancer Ther. 11(4), 1036-1047 (2012).