A pan-TEAD inhibitor
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GNE-7883

Item No. 39332

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(4-cyclohexylphenyl)-3-[[3-(fluoromethyl)-1-azetidinyl]carbonyl]-2-(3-methyl-2-pyrazinyl)-pyrazolo[1,5-a]pyrimidin-7(4H)-one
CAS Number
2648450-42-2
Molecular Formula
C28H29FN6O2
Formula Weight
500.6
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=C1C=C(C2=CC=C(C3CCCCC3)C=C2)NC4=C(C(C5=C(C)N=CC=N5)=NN14)C(N6CC(C6)CF)=O
InChi Code
InChI=1S/C28H29FN6O2/c1-17-25(31-12-11-30-17)26-24(28(37)34-15-18(14-29)16-34)27-32-22(13-23(36)35(27)33-26)21-9-7-20(8-10-21)19-5-3-2-4-6-19/h7-13,18-19,32H,2-6,14-16H2,1H3
InChi Key
UNRTVIQQMJRQLZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $117

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    50 mg

    $380

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    100 mg

    $621

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    Cayman Chemical
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    Product Description

    GNE-7883 is an allosteric pan-TEA domain transcription factor (pan-TEAD) inhibitor.1 It binds to the lipid-binding pockets of TEAD1-4 (IC50s = 0.01-0.05 µM) and inhibits the protein-protein interactions between TEAD1-4 and YAP (IC50s = 0.01-0.09 µM) and between TEAD1-4 and TAZ (IC50s = 0.01-0.1 µM). GNE-7883 inhibits the proliferation of YAP-amplified OVCAR-8 ovarian cancer and NF2-null HCC1576 adrenocortical carcinoma cells (IC50s = 0.17 and 0.29 µM, respectively). In vivo, GNE-7883 (250 mg/kg) reduces tumor volume in NCI H226 lung cancer and MSTO-211H mesothelioma mouse xenograft models. It also resensitizes sotorasib-resistant NCI H358 non-small cell lung cancer (NSCLC) cells to the K-RasG12C inhibitor sotorasib (AMG 510; Item No. 29465) in a mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hagenbeek, T.J., Zbieg, J.R., Hafner, M., et al. An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance. Nat. Cancer 4(6), 812-828 (2023).