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Larotrectinib sulfate

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

Catalog No. T6880Cas No. 1223405-08-0

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Purity:99.69%

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COA HPLC HNMR

Larotrectinib sulfate

Catalog No. T6880Cas No. 1223405-08-0

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

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.

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

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

Chemical Properties

Molecular Weight	526.51
Formula	C₂₁H₂₂F₂N₆O₂·H₂O₄S
Cas No.	1223405-08-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 50 mg/mL (94.96 mM)

Ethanol: 10 mg/mL (19 mM)

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

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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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