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Repotrectinib

Name: Repotrectinib
Brand: TargetMol
SKU: T4071
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4071Cas No. 1802220-02-5

Alias TPX-0005, TPX0005, TPX 0005

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.

Repotrectinib

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Purity: 99.92%

Catalog No. T4071Alias TPX-0005, TPX0005, TPX 0005Cas No. 1802220-02-5

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$39	In Stock	In Stock
5 mg	$89	In Stock	In Stock
10 mg	$143	In Stock	In Stock
25 mg	$289	In Stock	In Stock
50 mg	$438	In Stock	In Stock
100 mg	$658	In Stock	In Stock
200 mg	$919	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.92%

Appearance:Solid

Color:White

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COA HPLC LCMS HNMR

Product Introduction

Repotrectinib AI Summary

Repotrectinib demonstrates potent bioactivity across various targets, particularly exhibiting strong inhibitory effects on mutant receptor tyrosine kinases including TRKA, TRKC, and TRKB, with low IC50 values ranging from 0.2 nM to 1.9 nM. It effectively inhibits the ROS1 G2032R mutant with an IC50 of 8.4 nM and shows significant potency against ALK, including resistant mutations like ALK G1202R and L1196M, with IC50 values of 7.9 nM and 1.38 nM, respectively. Moreover, Repotrectinib demonstrates inhibitory activity against the SARS-CoV-2 3CL-Pro protease, with observable antiviral effects in SARS-CoV-2 induced cytotoxicity assays. In anti-cancer studies, it exhibits antiproliferative activity against cells expressing KRAS G12C mutant and various TRKA mutants, with IC50 values highlighting its high efficacy. Additionally, the compound has shown to reduce cell viability in HepG2 cells and demonstrated metabolic stability in liver microsomes, indicating potential for therapeutic applications in targeting kinase-related diseases and viral infections..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.
Targets&IC50	ALK (WT):1.01 nM, ALK (G1202R):1.26 nM, ALK (L1196M):1.08 nM, Src:5.3 nM
Synonyms	TPX-0005, TPX0005, TPX 0005

Chemical Properties

Molecular Weight	355.37
Formula	C₁₈H₁₈FN₅O₂
Cas No.	1802220-02-5
Smiles	C[C@H]1CNC(=O)c2cnn3ccc(N[C@H](C)c4cc(F)ccc4O1)nc23
Relative Density.	1.46 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (168.84 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.63 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8140 mL	14.0698 mL	28.1397 mL	140.6984 mL
5 mM	0.5628 mL	2.8140 mL	5.6279 mL	28.1397 mL
10 mM	0.2814 mL	1.4070 mL	2.8140 mL	14.0698 mL
20 mM	0.1407 mL	0.7035 mL	1.4070 mL	7.0349 mL
50 mM	0.0563 mL	0.2814 mL	0.5628 mL	2.8140 mL
100 mM	0.0281 mL	0.1407 mL	0.2814 mL	1.4070 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc