Home Protein Tyrosine Kinase c-RET inhibitor - Src inhibitor TPX-0046 For research use only.

TPX-0046

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

TPX-0046 Chemical Structure

CAS No. 2359650-19-2

Purity & Quality Control

TPX-0046 Related Products

Signaling Pathway

c-RET Signaling Pathways

c-RET Signaling Pathway

Biological Activity

Description

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.
Targets
RET [1] SRC [1]
In vitro
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.[2]
Cell Research 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
In Vivo
In vivo

TPX-0046 demonstrates marked anti-tumor efficacy in vivo in multiple RET-driven cancer cell-derived and patient-derived xenograft tumor models.[2]
Animal Research Animal Models Ba/F3 KIF5B-RET xenograft model
Dosages 5 mg/kg
Administration --
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04161391 Terminated
Non Small Cell Lung Cancer|Medullary Thyroid Cancer|RET Gene Mutation|Metastatic Solid Tumor|Advanced Solid Tumor
Turning Point Therapeutics Inc.
 December 6 2019 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 424.43 Formula

C21H21FN6O3
CAS No. 2359650-19-2 SDF --
Smiles CC1CNC(=O)C2=C3N=C4N(CC5=C(O1)N=CC(=C5)F)C6CCCC6OC4=C[N]3N=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 2 mg/mL ( (4.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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