An inhibitor of the YAP/TAZ-TEAD protein-protein interaction
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Product Type

Biochemicals

Research Area

Cancer
Cell Signaling

IAG933

Item No. 45726

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4S-[(2S)-5-chloro-6-fluoro-2,3-dihydro-2-phenyl-2-(2S)-2-pyrrolidinyl-4-benzofuranyl]-5-fluoro-6-(2-hydroxyethoxy)-N-methyl-3-pyridinecarboxamide
CAS Number
2714434-21-4
Molecular Formula
C27H26ClF2N3O4
Formula Weight
530.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
ClC([C@]([C@](C(F)=C(N=C1)OCCO)=C1C(NC)=O)=C2C3)=C(C=C2O[C@]3([C@H]4NCCC4)C5=CC=CC=C5)F
InChi Code
InChI=1S/C27H26ClF2N3O4/c1-31-25(35)17-14-33-26(36-11-10-34)24(30)22(17)21-16-13-27(20-8-5-9-32-20,15-6-3-2-4-7-15)37-19(16)12-18(29)23(21)28/h2-4,6-7,12,14,20,32,34H,5,8-11,13H2,1H3,(H,31,35)/t20-,27-/m0/s1
InChi Key
HUVOYQMXUNTUAI-DCFHFQCYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $325

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    5 mg

    $894

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    10 mg

    $1,300

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    25 mg

    $1,625

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    Cayman Chemical
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    Product Description

    IAG933 is an inhibitor of the protein-protein interaction between YAP/TAZ and TEAD (IC50 = 8.6 nM in a TR-FRET assay), downstream effectors of Hippo/MST1/2 signaling, which regulates cell proliferation and is frequently dysregulated in cancer.1 It reduces growth of Hippo-dependent NCI-H2052 mesothelioma cells and YAP-amplified SF-268 glioma cells (GI50s = 0.04 and 1.11 nM, respectively) but not Hippo-insensitive MKN45 gastric cancer cells (GI50 = >10 nM). Oral administration of IAG933 (30 mg/kg) induces tumor regression in a Hippo-driven MSTO-211H mesothelioma rat xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chapeau, E.A., Sansregret, L., Galli, G.G., et al. Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers. Nat. Cancer 5(7), 1102-1120 (2024).