Home Protein Tyrosine Kinase c-Met inhibitor - CSF-1R inhibitor - Src inhibitor Elzovantinib (TPX-0022)

research use only

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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
SRC [1]
(Cell-free assay)
0.12 nM
MET [1]
(Cell-free assay)
0.14 nM
CSF1R [1]
(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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map