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Larotrectinib

Name: Larotrectinib
Brand: TargetMol
SKU: T5995
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5995Cas No. 1223403-58-4

Alias LOXO-101, ARRY-470

Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).

Larotrectinib

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Purity: 99.24%

Catalog No. T5995Alias LOXO-101, ARRY-470Cas No. 1223403-58-4

Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$33	In Stock	In Stock
5 mg	$72	In Stock	In Stock
10 mg	$97	In Stock	In Stock
25 mg	$168	In Stock	In Stock
50 mg	$263	In Stock	In Stock
100 mg	$396	In Stock	In Stock
500 mg	$912	-	In Stock
1 mL x 10 mM (in DMSO)	$78	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:99.24%

Appearance:Solid

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).
Targets&IC50	Trk:2-20 nM
In vivo	In vivo, Larotrectinib?(60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model[1].
Animal Research	Mice were maintained under aseptic conditions.?The care and treatment of experimental animals was in accordance with institutional guidelines.?5 × 10^5 KM12 cells were injected subcutaneously into the dorsal flank area of the mice.?Tumor volume was monitored by direct measurement with calipers and calculated by the formula: length × (width^2)/2.?Following the establishment of tumor and when the tumor size was between 150–200 mm^2, mice were randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib(LOXO-101).?LOXO-101 was administered by oral gavage once daily for 14 days.?After the last dose, tissue and blood were collected at 3, 6 and 24 hours post-treatment[1].
Synonyms	LOXO-101, ARRY-470

Chemical Properties

Molecular Weight	428.44
Formula	C₂₁H₂₂F₂N₆O₂
Cas No.	1223403-58-4
Smiles	O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F
Relative Density.	1.55 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from direct sunlight,keep away from moisture,store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 83.33 mg/mL (194.5 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.33 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	2.3340 mL	11.6702 mL	23.3405 mL	116.7025 mL
5 mM	0.4668 mL	2.3340 mL	4.6681 mL	23.3405 mL
10 mM	0.2334 mL	1.1670 mL	2.3340 mL	11.6702 mL
20 mM	0.1167 mL	0.5835 mL	1.1670 mL	5.8351 mL
50 mM	0.0467 mL	0.2334 mL	0.4668 mL	2.3340 mL
100 mM	0.0233 mL	0.1167 mL	0.2334 mL	1.1670 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