TPX-0046 | 99.75%(HPLC) | In Stock

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RET^G810R in Ba/F3 cell proliferation assay.

TPX-0046 Chemical Structure

CAS: 2359650-19-2

Purity & Quality Control

Batch: Purity: 99.75%

99.75

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Signaling Pathway

c-RET Signaling Pathway

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Biological Activity

Description

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RET^G810R 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References
[1] Noura J Choudhury, Alexander Drilon. Transl Lung Cancer Res. 2020 Dec;9(6):2571-2580. [2] Alexander E Drilon, et al. Journal of Clinical. 2020 May; 38(15_suppl): 3616.

References

[1] Noura J Choudhury, Alexander Drilon. Transl Lung Cancer Res. 2020 Dec;9(6):2571-2580.
[2] Alexander E Drilon, et al. Journal of Clinical. 2020 May; 38(15_suppl): 3616.

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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
Batch:

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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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