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

Name: Larotrectinib
Brand: MedChemExpress
SKU: HY-12866
Rating: 5.0 (16 reviews)

Cat. No.: HY-12866 Purity: 99.93%: Data Sheet
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Larotrectinib (LOXO-101) 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. : 1223403-58-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Larotrectinib:

16 Publications Citing Use of MCE Larotrectinib

Cell Imaging/Staining

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: Larotrectinib 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 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 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 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 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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TrkA TrkB TrkC Trk

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

TrkA

TrkB

TrkC

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35007864]
BaF3	GI₅₀	10.2 nM Compound: 18	Antiproliferative activity against mouse BaF3 cells harbouring wild type TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring wild type TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
BaF3	GI₅₀	1024 nM Compound: 18	Antiproliferative activity against mouse BaF3 cells harbouring TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
BaF3	GI₅₀	3293 nM Compound: 18	Antiproliferative activity against mouse BaF3 cells harbouring TRKC G623R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKC G623R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
BaF3	GI₅₀	742.3 nM Compound: 18	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method	[PMID: 38389874]
BaF3	GI₅₀	> 10 μM Compound: 1; LOXO-101	Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 32949955]
BaF3	IC₅₀	0.007 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.009 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.013 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.016 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.018 μM Compound: LOXO-101	Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1 Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1	[PMID: 34628036]
BaF3	IC₅₀	0.04 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.054 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.11 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.184 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.539 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	1 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	1.201 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	1.55 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	10.1 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	10.1 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	11 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	1256 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	14.6 nM Compound: Larotrectinib	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKA wildtype assessed as cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKA wildtype assessed as cell viability measured after 72 hrs by CCK-8 method	[PMID: 38271867]
BaF3	IC₅₀	14.8 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	14.8 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	1487 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	15.4 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	173 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	18 nM Compound: Larotrectinib	Antiproliferative activity against mouse BaF3 cells harbouring LMNA-NTRK1 incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring LMNA-NTRK1 incubated for 3 days by CCK8 method	[PMID: 38754142]
BaF3	IC₅₀	18.4 nM Compound: LOX0-101	Antiproliferative activity against mouse BaF3-LMNA-NTRK1 cells assessed as cell viability measured after 72 hrs Antiproliferative activity against mouse BaF3-LMNA-NTRK1 cells assessed as cell viability measured after 72 hrs	[PMID: 33069129]
BaF3	IC₅₀	2.24 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	2.495 μM Compound: LOXO-101	Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1 G595R mutant Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1 G595R mutant	[PMID: 34628036]
BaF3	IC₅₀	2495 nM Compound: Larotrectinib	Antiproliferative activity against mouse BaF3 cells harbouring LMNA-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring LMNA-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 38754142]
BaF3	IC₅₀	2504.7 nM Compound: LOX0-101	Antiproliferative activity against mouse BaF3-LMNA-NTRK1-G595 mutant cells assessed as cell viability measured after 72 hrs Antiproliferative activity against mouse BaF3-LMNA-NTRK1-G595 mutant cells assessed as cell viability measured after 72 hrs	[PMID: 33069129]
BaF3	IC₅₀	284.4 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	2886.4 nM Compound: Larotrectinib	Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G595R mutant assessed as cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G595R mutant assessed as cell viability measured after 72 hrs by CCK-8 method	[PMID: 38271867]
BaF3	IC₅₀	29.7 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	321 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	332 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	332 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	3570 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	38.2 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	38.2 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	4.9 nM Compound: Larotrectinib	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB wildtype assessed as cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB wildtype assessed as cell viability measured after 72 hrs by CCK-8 method	[PMID: 38271867]
BaF3	IC₅₀	4060 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	46 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	46 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	547 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	586 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	59 nM Compound: Larotrectinib	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	755 nM Compound: Larotrectinib	Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G667C mutant assessed as cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G667C mutant assessed as cell viability measured after 72 hrs by CCK-8 method	[PMID: 38271867]
BaF3	IC₅₀	9.3 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	96 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	96 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623E mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623E mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	> 1000 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	> 1000 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	> 1000 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	> 2000 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	> 3 μM Compound: 1	Antiproliferative activity against mouse BaF3 cells habouring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells habouring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35007864]
EKVX	IC₅₀	7.33 μM Compound: Larotrectinib	Antiproliferative activity against human EKVX cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human EKVX cells assessed as inhibition of cell viability by MTT assay	[PMID: 37922829]
KM12	IC₅₀	0.005 μM Compound: 1	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35007864]
KM12	IC₅₀	0.012 μM Compound: 1; LOXO-101	Antiproliferative activity against human KM12 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36760745]
KM12	IC₅₀	34.5 nM Compound: 1	Antiproliferative activity against human KM12 cells harboring TPM3-NTRK1 incubated for 72 hrs by CCK8 cell counting assay Antiproliferative activity against human KM12 cells harboring TPM3-NTRK1 incubated for 72 hrs by CCK8 cell counting assay	[PMID: 38227770]
KM12	IC₅₀	4.68 μM Compound: Larotrectinib	Antiproliferative activity against human KM12 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell viability by MTT assay	[PMID: 37922829]
MCF7	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35007864]
MCF7	IC₅₀	> 40 μM Compound: 1; LOXO-101	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36760745]
NIH3T3	GI₅₀	1018 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells harbouring TRKA V573M mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells harbouring TRKA V573M mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	172 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	18.8 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells expressing wild type TRKC mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing wild type TRKC mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]
NIH3T3	GI₅₀	315 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells transfected with TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells transfected with TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	47 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]
NIH3T3	GI₅₀	5 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells transfected with wild type TRKA assessed as cell growth inhibition Antiproliferative activity against mouse NIH3T3 cells transfected with wild type TRKA assessed as cell growth inhibition	[PMID: 38389874]
NIH3T3	GI₅₀	70 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells expressing TRKA G667S mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing TRKA G667S mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]
NIH3T3	GI₅₀	819 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells harbouring TRKC G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells harbouring TRKC G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	> 10000 nM Compound: 18	Antiproliferative activity against mouse NIH3T3 cells expressing TRKC G623R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing TRKC G623R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]

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 (LOXO-101) 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 (LOXO-101) 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.

Clinical Trial

Molecular Weight

428.44

Formula

C₂₁H₂₂F₂N₆O₂

CAS No.

1223403-58-4

Appearance

Solid

Color

White to yellow

SMILES

O=C(N1C[C@@H](O)CC1)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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : ≥ 4.6 mg/mL (10.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3340 mL	11.6702 mL	23.3405 mL
5 mM	0.4668 mL	2.3340 mL	4.6681 mL
10 mM	0.2334 mL	1.1670 mL	2.3340 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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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: 99.93%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (254 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[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]

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

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3340 mL	11.6702 mL	23.3405 mL	58.3512 mL
	5 mM	0.4668 mL	2.3340 mL	4.6681 mL	11.6702 mL
	10 mM	0.2334 mL	1.1670 mL	2.3340 mL	5.8351 mL

Larotrectinib 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:

Larotrectinib1223403-58-4LOXO-101 ARRY-470LOXO101LOXO 101ARRY470ARRY 470ARRY-470Trk ReceptorApoptosisTropomyosin related kinase receptor Inhibitorinhibitorinhibit

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

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