An ERK1/2 inhibitor
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LY3214996

Item No. 27936

Technical Information
Formal Name
5,6-dihydro-6,6-dimethyl-2-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-5-[2-(4-morpholinyl)ethyl]-4H-thieno[2,3-c]pyrrol-4-one
CAS Number
1951483-29-6
Molecular Formula
C22H27N7O2S
Formula Weight
Purity
≥98%
A crystalline solid
λmax
213, 227, 301 nm
SMILES
CN1C(NC2=NC(C3=CC(C(N(CCN4CCOCC4)C5(C)C)=O)=C5S3)=CC=N2)=CC=N1
InChi Code
InChI=1S/C22H27N7O2S/c1-22(2)19-15(20(30)29(22)9-8-28-10-12-31-13-11-28)14-17(32-19)16-4-6-23-21(25-16)26-18-5-7-24-27(18)3/h4-7,14H,8-13H2,1-3H3,(H,23,25,26)
InChi Key
JNPRPMBJODOFEC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).1 It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bhagwat, S.V., McMillen, W.T., Cai, S., et alAbstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Cancer Res. 77(Suppl. 13), (2017).