Art. -Nr.: HY-12866A

Larotrectinib sulfate

(Synonyms: LOXO-101 sulfate; ARRY-470 sulfate)

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

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Reinheit: 99.02%
CAS. Nr.: 1223405-08-0
Formel: C₂₁H₂₄F₂N₆O₆S
Molecular Weight:526.51

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Larotrectinib sulfate Chemical Structure

CAS. Nr.: 1223405-08-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

TrkA

TrkB

TrkC

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
KM12	IC₅₀	1.9 nM Compound: 3; LOXO-101, ARRY-470	Growth inhibition of human KM12 cells Growth inhibition of human KM12 cells	[PMID: 31077998]
KM12	IC₅₀	≤5 nM Compound: 3; LOXO-101, ARRY-470	Inhibition of NTRK1 in human KM12 cells co-expressing TPM3 assessed as reduction in phospho TRKA level after 1 hr by ELISA Inhibition of NTRK1 in human KM12 cells co-expressing TPM3 assessed as reduction in phospho TRKA level after 1 hr by ELISA	[PMID: 31077998]

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^[1]^[2]. Measurement of proliferation following treatment with Larotrectinib (LOXO-101) demonstrates a dose-dependent inhibition of cell proliferation in all three cell lines. The IC₅₀ is less than 100 nM for CUTO-3.29 and less than 10 nM for KM12 and MO-91 consistent with the known potency of this drug for the TRK kinase family^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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%^[1]. Athymic nude mice injected with KM12 cells are treated with Larotrectinib sulfate orally daily for 2 weeks. Dose-dependent tumor inhibition is observed demonstrating the ability of this selective compound to inhibit tumor growth in vivo^[4]. Larotrectinib (LOXO-101) (200mg/kg/day p.o for six weeks) reduces leukemic infiltration to undetectable levels in the bone marrow and spleen compared to vehicle-treated mice. Mice treated with Larotrectinib sulfate are still alive and leukemia-free four weeks after the cessation of treatment, as determined by Xenogen imaging^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1223405-08-0
Appearance Solid
Molecular Weight 526.51
Formel C₂₁H₂₄F₂N₆O₆S
Color Light yellow to brown
SMILES

O=S(O)(O)=O.O=C(N1CC[C@H](O)C1)NC2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2
Synonyms

LOXO-101 sulfate; ARRY-470 sulfate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Publications (17)

All Cell Imaging/StainingCell Proliferation/Viability AssayWBBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Nat Nanotechnol

Targeted intervention in nerve-cancer crosstalk enhances pancreatic cancer chemotherapy. [Abstract]

2025 Feb;20(2):311-324. PMID: 39496914
Bioact Mater

Composite hydrogel-microsphere delivery system promotes early nerve-mediated bone regeneration and late-stage mechanotransduction-driven bone remodeling via sequential release of NGF and Yoda1. [Abstract]

2025 Nov 20:57:531-550. PMID: 41340637

Larotrectinib sulfate purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2025 Nov 20:57:531-550. [Abstract]

The TrkA inhibitor Larotrectinib (100 ng/mL) effectively blocked the promotion of PC-12 neurite outgrowth yielded by NGF.
Nat Commun

Somatic gene delivery faithfully recapitulates a molecular spectrum of high-risk sarcomas. [Abstract]

2025 Jun 16;16(1):5283. PMID: 40523919

Larotrectinib sulfate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 16;16(1):5283. [Abstract]

NTRK inhibitor Larotrectinib (0-10000 nM) showed specific and significant activity in NTRK-Mono and NTRK-Pleo cell lines in vitro, comparable to response rates in a rare patient-derived cell model acquired from a patient suffering from NTRK-driven Inflammatory Myofibroblastic Tumor (IMT).

Larotrectinib sulfate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 16;16(1):5283. [Abstract]

NTRK inhibitor Larotrectinib (10 µL/g; p.o.; twice a week) resulted in profound antitumor activity and tumor regression in mice bearing a NTRK-Mono allograft model.
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Mol Biomed

Targeting ANXA1/TRKA axis enhances immunotherapy sensitivity in neural invasion-positive gastric cancer. [Abstract]

2026 Apr 9;7(1):48. PMID: 41954859
Mol Cancer Ther

Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations. [Abstract]

2021 Dec;20(12):2446-2456. PMID: 34625502

Larotrectinib sulfate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2021 Dec;20(12):2446-2456. [Abstract]

Larotrectinib (0-300 nM; 4 h) inhibited TRKA autophosphorylation in KM12 tumor cells harboring a wild-type TPM3-TRKA fusion.
Eur J Med Chem

Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants. [Abstract]

2020 Aug 30;207:112744. PMID: 32949955
Spectrochim Acta A Mol Biomol Spectrosc

Green synthesized nitrogen-doped carbon quantum dots for the sensitive determination of larotrectinib in biological fluids and dosage forms: Evaluation of method greenness and selectivity. [Abstract]

2023 Nov 5:300:122914. PMID: 37257322

Larotrectinib sulfate purchased from MedChemExpress. Usage Cited in: Spectrochim Acta A Mol Biomol Spectrosc. 2023 Nov 5:300:122914. [Abstract]

Larotrectinib (LARO) (5.0–28.0 μg/mL) quantitatively quenched the native fluorescence of N-CQDs in a concentration-dependent manner.
Mol Oncol

ERBB and P-glycoprotein inhibitors break resistance in relapsed neuroblastoma models through P-glycoprotein. [Abstract]

2023 Jan;17(1):37-58. PMID: 36181342
BMC Cancer

NTRK fusion promotes tumor migration and invasion through epithelial-mesenchymal transition and closely interacts with ECM1 and NOVA1. [Abstract]

2024 Dec 5;24(1):1502. PMID: 39639242
Life

NGF-TrkA Axis Enhances PDGF-C-Mediated Angiogenesis in Osteosarcoma via miR-29b-3p Suppression: A Potential Therapeutic Strategy Using Larotrectinib. [Abstract]

2025 Jan 15;15(1):99. PMID: 39860039
J Anal Sci Technol

2020 Jun.
Biophys Chem

Unraveling the molecular interaction of Larotrectinib with calf thymus DNA: A comprehensive study using multi-spectroscopic, thermodynamic, and computational techniques. [Abstract]

2025 Aug 12:327:107512. PMID: 40816098
Res Sq

2025 Apr 14.
bioRxiv

2024 Feb 1.
Ruprecht Karls University

2023 Feb 2.
bioRxiv

04 Nov 2021.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (94.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (3.80 mM; ultrasonic and adjust pH to 2 with 1M HCl)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8993 mL

9.4965 mL

18.9930 mL

5 mM

0.3799 mL

1.8993 mL

3.7986 mL

10 mM

0.1899 mL

0.9496 mL

1.8993 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3.25 mg/mL (6.17 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3.25 mg/mL (6.17 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.25 mg/mL (6.17 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 12.5 mg/mL (23.74 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[4]

Mice^[4]
Athymic nude mice are used throughout the study. 5×10⁵ KM12 cells are injected subcutaneously into the dorsal flank area of the mice. Tumor volume is monitored by direct measurement with calipers and calculated by the formula: length × (width²)/2. Following the establishment of tumor and when the tumor size is between 150-200 mm², mice are randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib (LOXO-101). Larotrectinib (LOXO-101) is administered by oral gavage once daily for 14 days. After the last dose, tissue and blood are collected at 3, 6 and 24 hours post-treatment^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Karyn Bouhana, et al. LOXO-101, a pan TRK inhibitor, For The Treatment Of TRK-driven Cancers.

[2]. Nagasubramanian R, et al. Infantile Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the Tropomyosin-Related Kinase Inhibitor LOXO-101. Pediatr Blood Cancer. 2016 Aug;63(8):1468-70. [Content Brief]

[3]. Kathryn G, et al. Genetic Modeling and Therapeutic Targeting of ETV6-NTRK3 with Loxo-101in Acute Lymphoblastic Leukemia. Blood 2016 128:278.

[4]. Doebele RC, et al. An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101. Cancer Discov. 2015 Oct;5(10):1049-57. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.8993 mL	9.4965 mL	18.9930 mL	47.4825 mL
DMSO	5 mM	0.3799 mL	1.8993 mL	3.7986 mL	9.4965 mL
	10 mM	0.1899 mL	0.9496 mL	1.8993 mL	4.7482 mL
	15 mM	0.1266 mL	0.6331 mL	1.2662 mL	3.1655 mL
	20 mM	0.0950 mL	0.4748 mL	0.9496 mL	2.3741 mL
	25 mM	0.0760 mL	0.3799 mL	0.7597 mL	1.8993 mL
	30 mM	0.0633 mL	0.3165 mL	0.6331 mL	1.5827 mL
	40 mM	0.0475 mL	0.2374 mL	0.4748 mL	1.1871 mL
	50 mM	0.0380 mL	0.1899 mL	0.3799 mL	0.9496 mL
	60 mM	0.0317 mL	0.1583 mL	0.3165 mL	0.7914 mL
	80 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5935 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Larotrectinib sulfate

17 Cited Publications

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Larotrectinib sulfate

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Publications Citing Use of MedChemExpress (MCE) Larotrectinib sulfate

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Larotrectinib sulfate Related Classifications

HY-12866A Related Classifications