Larotrectinib sulfate
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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- Pureza: 99.02%
- No. CAS: 1223405-08-0
- Fòrmula: C21H24F2N6O6S
- Peso molecular:526.51
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Larotrectinib sulfate
More- Nat Nanotechnol. 2025 Feb;20(2):311-324. [Abstract]
- Bioact Mater. 2025 Nov 20:57:531-550. [Abstract]
- Nat Commun. 2025 Jun 16;16(1):5283. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Mol Biomed. 2026 Apr 9;7(1):48. [Abstract]
- Mol Cancer Ther. 2021 Dec;20(12):2446-2456. [Abstract]
- Eur J Med Chem. 2020 Dec 1:207:112744. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2023 Nov 5:300:122914. [Abstract]
- Mol Oncol. 2023 Jan;17(1):37-58. [Abstract]
- BMC Cancer. 2024 Dec 5;24(1):1502. [Abstract]
- Life. 2025 Jan 15;15(1):99. [Abstract]
- J Anal Sci Technol. 2020 Jun.
- Biophys Chem. 2025 Dec:327:107512. [Abstract]
- Res Sq. 2025 Apr 14.
- bioRxiv. 2024 Feb 1.
- Ruprecht Karls University. 2023 Feb 2.
- bioRxiv. 04 Nov 2021.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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WB
Actividad biológica
Descripciòn
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TrkA |
TrkB |
TrkC |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KM12 | IC50 |
1.9 nM
Compound: 3; LOXO-101, ARRY-470
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Growth inhibition of human KM12 cells
Growth inhibition of human KM12 cells
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[PMID: 31077998] |
| KM12 | IC50 |
≤5 nM
Compound: 3; LOXO-101, ARRY-470
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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
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[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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1223405-08-0
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Appearance Solid
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Peso molecular 526.51
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Fòrmula C21H24F2N6O6S
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Color Light yellow to brown
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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
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Synonyms
LOXO-101 sulfate; ARRY-470 sulfate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Nanotechnol
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.
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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.
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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.
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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 Dec 1:207:112744. 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.
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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 -
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Biophys Chem
Unraveling the molecular interaction of Larotrectinib with calf thymus DNA: A comprehensive study using multi-spectroscopic, thermodynamic, and computational techniques. [Abstract]2025 Dec:327:107512. PMID: 40816098 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
Pureza y Documentación
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Ficha de datos (286 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
[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]
Complete Stock Solution Preparation Table
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.
| 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.
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