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Larotrectinib sulfate

Name: Larotrectinib sulfate
Brand: TargetMol
SKU: T6880
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6880Cas No. 1223405-08-0

Alias LOXO-101 sulfate, LOXO-101 (sulfate), ARRY-470 (sulfate)

Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Larotrectinib sulfate

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Purity: 99.76%

Catalog No. T6880Alias LOXO-101 sulfate, LOXO-101 (sulfate), ARRY-470 (sulfate)Cas No. 1223405-08-0

Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$33	In Stock	In Stock
5 mg	$52	In Stock	In Stock
10 mg	$85	In Stock	In Stock
25 mg	$133	In Stock	In Stock
50 mg	$166	In Stock	In Stock
100 mg	$288	In Stock	In Stock
500 mg	$693	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$60	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:99.76%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
In vitro	Larotrectinib is a specific kinase inhibitor with nanomolar activity against TRKA/TRKB/TRKC but no other notable kinase inhibition (1 μM). Larotrectinib hasn't the inhibitory of the proliferation of Ba/F3 cells expressing other oncogene targets (EGFR, ROS1 or ALK) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells.
In vivo	Early/sustained but not late/acute administration of ARRY-470(LOXO-101) obviously attenuates bone cancer pain and blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor-bearing bone, but no significant inhibition for tumor growth or bone remodeling. It has very limited ability crossing of the blood-brain barrier.
Cell Research	Concentrations: 10,100,1000 nM. Method: Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G,gefitinib 1,000 nM) or DMSO control.The cell lysate is used for western blot analysis.
Animal Research	Animal Models: Adult male C3H/HeJ mice. Formulation: Labrafac; polygly-colyzed glyceride. Dosages: 10-100 mg/kg. Administration: p.o.
Synonyms	LOXO-101 sulfate, LOXO-101 (sulfate), ARRY-470 (sulfate)

Chemical Properties

Molecular Weight	526.51
Formula	C₂₁H₂₂F₂N₆O₂·H₂O₄S
Cas No.	1223405-08-0
Smiles	OS(O)(=O)=O.O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 50 mg/mL (94.96 mM), Sonication is recommended.

Ethanol: 10 mg/mL (18.99 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (4.75 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8993 mL	9.4965 mL	18.9930 mL	94.9650 mL
5 mM	0.3799 mL	1.8993 mL	3.7986 mL	18.9930 mL
10 mM	0.1899 mL	0.9496 mL	1.8993 mL	9.4965 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.0950 mL	0.4748 mL	0.9496 mL	4.7482 mL
50 mM	0.0380 mL	0.1899 mL	0.3799 mL	1.8993 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