Larotrectinib sulfate (LOXO-101; ARRY-470)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
500mg	$850	In Stock
1g	$1380	In Stock
5g	$3495	In Stock

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Cat #: V2599 CAS #: 1223405-08-0 Purity ≥ 98%

Description: Larotrectinib sulfate (LOXO-101; ARRY-470; Vitrakvi), the suldate salt of Larotrectinib, is a potent, oral, selective, ATP competitive TRK inhibitor with IC50s in low nanomolar range (2 to 20 nM) for inhibition of all TRK family members in binding and cellular assays.

References: Karyn Bouhana, et al. LOXO-101, a pan TRK inhibitor, For The Treatment Of TRK-driven Cancers.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	526.51
Molecular Formula	C21H22F2N6O2.H2O4S
CAS No.	1223405-08-0
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 100 mg/mL (189.9 mM)r
	Water: <1 mg/mLr
	Ethanol: 100 mg/mL (189.9 mM)
SMILES Code	O=C(N1C[C@@H](O)CC1)NC2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2.O=S(O)(O)=O
Synonyms	ARRY 470 sulfate; ARRY-470 sulfate; ARRY470 sulfate; LOXO-101 sulfate; Larotrectinib sulfate; LOXO101 sulfate; LOXO 101 sulfate; LOXO-101; LOXO101; ARRY-470; ARRY470; ARRY 470; trade name: Vitrakvi

Protocol	In Vitro	Larotrectinib (LOXO-101) is an ATP-competitive oral inhibitor of the tropomyosin-related kinase (TRK) family of receptor kinases (TRKA, B, and C), with low nanomolar 50% inhibitory concentrations against all three isoforms, and 1,000-fold or greater selectivity relative to other kinases.
Protocol	In Vivo	In rat and monkey studies, Larotrectinib (LOXO-101) demonstrates 33-100% oral bioavailability and 60-65% plasma protein binding. It has low brain penetration, and is well tolerated in 28 day (d) GLP toxicology studies. A single dose (30 mg/kg) of Larotrectinib (LOXO-101) reduces tyrosine phosphorylation of TRKA and downstream signal transduction (pERK) in the tumor >80%.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.8993 mL	9.4965 mL	18.9930 mL	37.9860 mL
5mM	0.3799 mL	1.8993 mL	3.7986 mL	7.5972 mL
10mM	0.1899 mL	0.9496 mL	1.8993 mL	3.7986 mL
20mM	0.0950 mL	0.4748 mL	0.9496 mL	1.8993 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.