An inhibitor of Src, MET, and FMS kinases
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TPX-0022

Item No. 36118

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(7S)-3-amino-14-ethyl-11-fluoro-4,5,6,7,13,14-hexahydro-7-methyl-4-oxo-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecine-12-carbonitrile
CAS Number
2271119-26-5
Synonyms
  • CSF1R-IN-2
  • CSF1R Inhibitor 2
  • Elzovantinib
Molecular Formula
C20H20FN7O2
Formula Weight
409.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Ethanol: 5mg/ml
λmax
215, 271 nm
SMILES
CCN(CC1=C(C#N)C(F)=CC=C1O[C@H](CNC2=O)C)C3=NC4=C2C(N)=NN4C=C3
InChi Code
InChI=1S/C20H20FN7O2/c1-3-27-10-13-12(8-22)14(21)4-5-15(13)30-11(2)9-24-20(29)17-18(23)26-28-7-6-16(27)25-19(17)28/h4-7,11H,3,9-10H2,1-2H3,(H2,23,26)(H,24,29)/t11-/m0/s1
InChi Key
UUDPUQDMSHQSKH-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    TPX-0022 is an inhibitor of Src, MET, and CSF-1 receptor tyrosine kinase (FMS) kinases (IC50s = 0.12, 0.14, and 0.76 nM, respectively).1 It inhibits the proliferation of MKN45 and SNU-5 human gastric cancer cells (IC50s = 0.2 and 0.17 nM, respectively), as well as Ba/F3 pro-B cells expressing TEL-CSF1R (IC50 = 19.3 nM). TPX-0022 (100 nM) inhibits cell migration of HCC827 human lung cancer cells. It inhibits tumor growth in an MKN45 mouse xenograft model when administered at doses of 10 and 30 mg/kg. TPX-0022 (10 mg/kg) also inhibits phosphorylation of MET at Tyr1234 and Tyr1349 in the same model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cui, J.J., Rogers, E.W., Ung, J., et al. Macrocyclic compounds and uses thereof. (2019).