research use only

Larotrectinib sulfate Trk receptor inhibitor

Name: Larotrectinib sulfate
Brand: Selleck Chemicals
SKU: S7960
Availability: InStock
Rating: 5 (21 reviews)

Cat.No.S7960

Larotrectinib sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.

Chemical Structure

Molecular Weight: 526.51

Jump to

Quality Control

Batch: Purity: 99.76%

99.76

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other Trk receptor Inhibitors	ANA-12 GW441756 7,8-Dihydroxyflavone GNF-5837 Selitrectinib (LOXO-195) Altiratinib N-Acetyl-5-hydroxytryptamine LM22A-4 CH7057288 PF-06273340

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
KM12 cells	Function assay	0, 10, 100, 1000 nM	3 hours	LOXO-101 inhibited NTRK1 phosphorylation at 100 nmol/L	28751539
Ba/F3	Function assay	0, 10, 100, 1000 nM	3 hours	LOXO-101 inhibited NTRK1 phosphorylation at 100 nmol/L,	28751539
CR20	Function assay	0, 10, 100, 1000 nM	3 hours	NTRK1 phosphorylation was inhibited	28751539
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (189.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	526.51	Formula	C₂₁H₂₂F₂N₆O₂.H₂SO₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1223405-08-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LOXO-101 sulfate, ARRY-470 sulfate			Smiles	C1CC(N(C1)C2=NC3=C(C=NN3C=C2)NC(=O)N4CCC(C4)O)C5=C(C=CC(=C5)F)F.OS(=O)(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	TRK
In vitro	ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) 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) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21138586/ [2] https://pubmed.ncbi.nlm.nih.gov/24162815/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pTRKA / TRKA / pTRKC / TRKC / p-AKT / AKT p-NTRK(Y490) / p-ERK (T202/Y204) / p-Eif4e		26216294
Growth inhibition assay	Cell proliferation		26216294

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04655404	Recruiting	High Grade Glioma\|Diffuse Intrinsic Pontine Glioma	Nationwide Children''s Hospital	April 8 2021	Early Phase 1
NCT04814667	Active not recruiting	Solid Tumor Adult\|Locally Advanced Solid Tumor\|Metastatic Cancer	Centre Leon Berard\|Bayer	February 23 2021	--
NCT04142437	Recruiting	Locally Advanced or Metastatic Solid Tumor Harboring an NTRK Gene Fusion	Bayer	April 3 2020	--
NCT03834961	Active not recruiting	Central Nervous System Neoplasm\|Infantile Fibrosarcoma\|Recurrent Acute Leukemia\|Refractory Acute Leukemia\|Solid Neoplasm	Children''s Oncology Group\|National Cancer Institute (NCI)	October 25 2019	Phase 2
NCT02637687	Active not recruiting	Solid Tumors Harboring NTRK Fusion	Bayer	December 16 2015	Phase 1\|Phase 2
NCT02576431	Active not recruiting	Solid Tumors Harboring NTRK Fusion	Bayer	September 30 2015	Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):