Catalog No.S9826

For research use only.

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.

TPX-0046 Chemical Structure


Purity & Quality Control

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Biological Activity


TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.

RET [1]
SRC [1]
In vitro

TPX-0046 is a new type of RET/SRC inhibitor and potent against a range of RET fusions and mutations including solvent front mutations (SFMs)-mediated resistance. In Ba/F3 RET engineered cells with SFMs proliferation test, the average IC50 is 1-17 nM.<sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

TPX-0046 demonstrates marked anti-tumor efficacy in vivo in multiple RET-driven cancer cell-derived and patient-derived xenograft tumor models.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Cell lines: Ba/F3 RET engineered cells with SFMs, KIF5B-RET Ba/F3, LC2/ad, and TT cells
  • Concentrations: --
  • Incubation Time: --
  • Method:

    Cell proliferation assays

Animal Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Animal Models: Ba/F3 KIF5B-RET xenograft model
  • Dosages: 5 mg/kg
  • Administration: --

Solubility (25°C)

In vitro

DMSO 2 mg/mL
(4.71 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 424.43


Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04161391 Recruiting Drug: TPX-0046 Non Small Cell Lung Cancer|Medullary Thyroid Cancer|RET Gene Mutation|Metastatic Solid Tumor|Advanced Solid Tumor Turning Point Therapeutics Inc. December 16 2019 Phase 1|Phase 2

(data from, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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