A RET kinase inhibitor
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GSK3179106

Item No. 24023

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-ethoxy-1,6-dihydro-6-oxo-3-pyridinyl)-2-fluoro-N-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-benzeneacetamide
CAS Number
1627856-64-7
Synonyms
  • RET Kinase Inhibitor 1
Molecular Formula
C22H21F4N3O4
Formula Weight
467.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50mg/mLDMSO: 50mg/mLDMSO:PBS (pH 7.2) (1:3): 0.25mg/mLEthanol: 25mg/mL
λmax
209, 233 nm
SMILES
O=C1C=C(OCC)C(C2=CC(F)=C(CC(NC3=NOC(C(C)(C)C(F)(F)F)=C3)=O)C=C2)=CN1
InChi Code
InChI=1S/C22H21F4N3O4/c1-4-32-16-9-19(30)27-11-14(16)12-5-6-13(15(23)7-12)8-20(31)28-18-10-17(33-29-18)21(2,3)22(24,25)26/h5-7,9-11H,4,8H2,1-3H3,(H,27,30)(H,28,29,31)
InChi Key
IDXKJSSOUXWLDB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    GSK3179106 is an inhibitor of rearranged during transfection (RET) kinase (IC50 = 0.4 nM).1 It is selective for RET kinase over VEGF receptor 2 (VEGFR2/KDR; IC50 = 109 nM). GSK3179106 reduces the number of abdominal contractions induced by colorectal distension in acetic acid-sensitized rats when administered at a dose of 10 mg/kg twice per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schenck Eidam, H., Russell, J., Raha, K., et al. Discovery of a first-in-class gut-restricted RET kinase inhibitor as a clinical candidate for the treatment of IBS. ACS Med. Chem. Lett. 9(7), 623-628 (2018).