Home Protein Tyrosine Kinase c-Met inhibitor Elzovantinib (TPX-0022)

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Elzovantinib (TPX-0022) c-Met inhibitor

Cat.No.S9620

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) c-Met inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 409.42

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Quality Control

Batch: S962001 Ethanol]5 mg/mL]false]DMSO]Insoluble]false]Water]Insoluble]false Purity: 99.98%
99.98

Chemical Information, Storage & Stability

Molecular Weight 409.42 Formula

C20H20FN7O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2271119-26-5 -- Storage of Stock Solutions

Solubility

In vitro
Batch:

Ethanol : 5 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
SRC
(Cell-free assay)
0.12 nM
MET
(Cell-free assay)
0.14 nM
CSF1R
(Cell-free assay)
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>
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03993873 Active not recruiting
Advanced Solid Tumor|Metastatic Solid Tumors|MET Gene Alterations
Turning Point Therapeutics Inc.
 September 21 2019 Phase 1|Phase 2

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