Elzovantinib (TPX-0022)

Catalog No.S9620 Synonyms: CSF1R-IN-2

For research use only.

Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.

Elzovantinib (TPX-0022)  Chemical Structure

CAS No. 2271119-26-5

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Biological Activity

Description Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.
Targets
SRC [1]
(Cell-free assay)
MET [1]
(Cell-free assay)
CSF1R [1]
(Cell-free assay)
0.12 nM 0.14 nM 0.71 nM
In vitro

In a Ba/F3 ETV6-CSF1R cell model, TPX-0022 inhibits both autophosphorylation of CSF1R with an IC50 <3 nM and cell growth with an IC50 of 14 nM, thus effectively inhibits tumor growth .<sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

TPX-0022 effectively inhibits the growth of Ba/F3 ETV6-CSF1R xenograft tumors in vivo.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO Insoluble
Water Insoluble
Ethanol ''''5 mg/mL

Chemical Information

Molecular Weight 409.42
Formula

C20H20FN7O2

CAS No. 2271119-26-5
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03993873 Recruiting Drug: TPX-0022 Advanced Solid Tumor|Metastatic Solid Tumors|MET Gene Alterations Turning Point Therapeutics Inc. August 20 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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