2. Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. Trk Receptor Apoptosis
  4. Larotrectinib sulfate

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

Cat. No.: HY-12866A Purity: 99.02%
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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).

For research use only. We do not sell to patients.

CAS No. : 1223405-08-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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25 mg In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Larotrectinib sulfate:

Larotrectinib sulfate Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

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

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

    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.

    View All Trk Receptor Isoform Specific Products:

    View All Isoforms
    TrkA TrkB TrkC Trk

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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).

    IC50 & Target[1][2]

    TrkA

     

    TrkB

     

    TrkC

     

    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.

    Larotrectinib sulfate Related Antibodies
    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.
    Molecular Weight

    526.51

    Formula

    C21H24F2N6O6S
    CAS No.
    Appearance

    Solid

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8993 mL 9.4965 mL 18.9930 mL
    5 mM 0.3799 mL 1.8993 mL 3.7986 mL
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      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.

    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.02%

    SDS (393 KB)

    COA (259 KB) LCMS (115 KB)

    Handling Instructions (2659 KB)
    References
    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].

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

    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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    Larotrectinib sulfate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Larotrectinib1223405-08-0LOXO-101ARRY-470LOXO101LOXO 101ARRY470ARRY 470Trk ReceptorApoptosisTropomyosin related kinase receptor Inhibitorinhibitorinhibit

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