Selitrectinib (Synonyms: LOXO-195)

Name: Selitrectinib
Brand: MedChemExpress
SKU: HY-101977
Rating: 5.0 (5 reviews)

Cat. No.: HY-101977 Purity: 99.74%: Data Sheet
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Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC₅₀s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively.

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

CAS No. : 2097002-61-2

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Selitrectinib:

5 Publications Citing Use of MCE Selitrectinib

Cell Proliferation/Viability Assay

: Selitrectinib purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Jun;13(12):e7393. [Abstract]; Cell viabilities were significantly reduced in NTRK‐TKI resistant cells after silibinin and NTRK‐TKIs treatment compared to NTRK‐TKIs alone. Treatments were with 100 nM NTRK‐TKIs (KM12‐LR: Larotrectinib, KM12‐ER: Entrectinib and KM12‐SR: Selitrectinib) and 20 μM silibinin for 72 h.

: Selitrectinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Aug 24;15(17):4246.; Western blot analysis showing the influence of Selitrectinib (LOXO-195) (100 nM) on the protein levels of EN variants in stable cell lines.

: Selitrectinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Aug 24;15(17):4246.; Fluorescence microscopy images portraying the subcellular localization of EN variants under two conditions: cells untreated and cells treated with Selitrectinib (LOXO-195) (100 nM).

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TrkA TrkB TrkC Trk

Biological Activity
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Description

Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC₅₀s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively^[1].

IC₅₀ & Target^[1]

TrkA

0.6 nM (IC₅₀)

TrkC

<2.5 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.001 μM Compound: 3	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	0.001 μM Compound: 3	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	0.0082 μM Compound: LOXO-195	Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.013 μM Compound: 3	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	0.013 μM Compound: LOXO-195	Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.018 μM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay	[PMID: 35080890]
BaF3	IC₅₀	0.018 μM Compound: LOXO-195	Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.041 μM Compound: 3	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	1 nM Compound: LOX0195	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	1.1 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKA assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKA assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	1.2 nM Compound: 3; LOXO-195	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	1.35 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.36 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.4 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKB assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKB assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	1.6 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKC assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKC assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	1.7 nM Compound: 3; LOXO-195	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	10.28 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	10.5 nM Compound: 3	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	10.7 nM Compound: 3	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	10.98 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	109 nM Compound: LOX0195	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	113.1 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
BaF3	IC₅₀	12 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
BaF3	IC₅₀	12.6 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA F589L mutant assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA F589L mutant assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	13 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA G595R mutant assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA G595R mutant assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	15 nM Compound: LOX0195	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	15.2 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
BaF3	IC₅₀	16.7 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	16.7 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
BaF3	IC₅₀	17 nM Compound: LOX0195	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	17.2 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	18 nM Compound: LOX0195	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	2.32 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.4 nM Compound: 3	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	2.7 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	22.23 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	23.2 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
BaF3	IC₅₀	24.4 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA G667A mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA G667A mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	25.4 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	26.11 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	26.38 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	27.8 nM Compound: selitrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition	[PMID: 36395392]
BaF3	IC₅₀	28.2 nM Compound: 3	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	3.2 nM Compound: 3	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	3.39 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	30 nM Compound: LOX0195	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	30.66 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	31.5 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	35.79 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	36.7 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	37 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4 nM Compound: LOX0195	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	4.15 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4.9 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	41.06 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	41.4 nM Compound: 3; LOXO-195	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	42.04 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	423.15 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	48.16 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.08 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.2 nM Compound: 3; LOXO-195	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	5.7 nM Compound: 3	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	50 nM Compound: LOX0195	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	6.8 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	7.48 nM Compound: 3	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: 37676745]
BaF3	IC₅₀	72.6 nM Compound: 3	Antiproliferative activity aganist mouse BAF3 cells transfected with LMNA-TRKA G667C mutant assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity aganist mouse BAF3 cells transfected with LMNA-TRKA G667C mutant assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	8.2 nM Compound: 3	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	8.5 nM Compound: 3	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	84.5 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
BaF3	IC₅₀	9 nM Compound: LOX0195	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	95.6 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
BaF3	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	> 10000 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	> 10000 nM Compound: LOX0195	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	> 20000 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
KM12	IC₅₀	0.0028 μM Compound: LOXO-195	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
KM12	IC₅₀	1.7 nM Compound: Selitrectinib	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: 38029466]
KM12	IC₅₀	2.9 nM Compound: Selitrectinib	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
KM12	IC₅₀	6.8 nM Compound: Selitrectinib	Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
KM12	IC₅₀	<= 5 nM Compound: LOXO-195	Inhibition of cell proliferation in TPM3-NTRK1 fusion positive human KM12 cells incubated for 72 hrs by DAPI staining based analysis Inhibition of cell proliferation in TPM3-NTRK1 fusion positive human KM12 cells incubated for 72 hrs by DAPI staining based analysis	[PMID: 28578312]
KM12	IC₅₀	<= 5 nM Compound: LOXO-195	Antiproliferative activity against TrK fused human KM12 cells Antiproliferative activity against TrK fused human KM12 cells	[PMID: 34253025]
MCF7	IC₅₀	> 10000 nM Compound: Selitrectinib	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
MCF7	IC₅₀	> 20000 nM Compound: Selitrectinib	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: 38029466]
NIH3T3	GI₅₀	1.6 nM Compound: 19; LOXO-195	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	17.5 nM Compound: 19; LOXO-195	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	2 nM Compound: 19; LOXO-195	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	25 nM Compound: 19; LOXO-195	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	29 nM Compound: 19; LOXO-195	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	45.5 nM Compound: 19; LOXO-195	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]
NIH3T3	GI₅₀	64 nM Compound: 19; LOXO-195	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	7 nM Compound: 19; LOXO-195	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	9 nM Compound: 19; LOXO-195	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]

In Vitro

Selitrectinib (LOXO-195) demonstrates strong binding to the wild-type TRKA, TRKB and TRKC kinase domains. Selitrectinib (LOXO-195) has potent (IC₅₀<1 nM) inhibitory activity in kinase enzyme assays. Importantly, Selitrectinib (LOXO-195) achieves low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, with IC₅₀s ranging from 2.0-9.8 nM. 228 individual kinases in vitro are profiled at a Selitrectinib (LOXO-195) concentration of 1 μM, which is ~1667-fold higher than its IC₅₀ for TRKA (0.6 nM). Selitrectinib (LOXO-195) is more than 1000-fold selective for 98% of non-TRK kinases tested. Selitrectinib (LOXO-195) demonstrates potent inhibition of cell proliferation in TRK fusion-containing KM12, CUTO-3, and MO-91 cell lines (IC₅₀≤5 nM)^[1].

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

In Vivo

Stably transfected NIH-3T3 ΔTRKA and ΔTRKA-G595R cells are implanted subcutaneously into the flanks of nude mice. Both larotrectinib and Selitrectinib (LOXO-195) are effective at reducing phosphorylated TRKA in tumors driven by ΔTRKA. In contrast, only Selitrectinib (LOXO-195) strongly suppresses phospho-TRKA in ΔTRKA-G595R cells in a dose-dependent manner. Selitrectinib (LOXO-195) also causes inhibition of tumor growth relative to vehicle at all doses in four TRKA-dependent tumor models (ΔTRKA, ΔTRKA-G595R, ΔTRKAG667C, and TPM3-NTRK1 fusion-positive KM12 colorectal cancer cells. Larotrectinib inhibits KM12 and NIH 3T3-ΔTRKA tumors to a similar degree. Group mean body weight loss does not exceed 5% for any agent. Selitrectinib (LOXO-195) displays high selectivity for the TRK proteins^[1]

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

Clinical Trial

Molecular Weight

380.42

Formula

C₂₀H₂₁FN₆O

CAS No.

2097002-61-2

Appearance

Solid

Color

White to yellow

SMILES

FC1=CN=C(CC[C@H](N2)C)C([C@](CCC3)([H])N3C(C=CN4N=C5)=NC4=C5C2=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (164.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6287 mL	13.1434 mL	26.2867 mL
5 mM	0.5257 mL	2.6287 mL	5.2573 mL
10 mM	0.2629 mL	1.3143 mL	2.6287 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.08 mg/mL (5.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.90% ee.: 99.77%

Select Batch:

Data Sheet (280 KB) SDS (396 KB)

COA (250 KB) HNMR (207 KB) LCMS (121 KB)

Handling Instructions (2659 KB)

References

[1]. Drilon A, et al. A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors. Cancer Discov. 2017 Sep;7(9):963-972. [Content Brief]

Cell Assay ^[1]	For assessment of cellular inhibition potency, cells are harvested per a standard protocol, counted and added to flat-bottom, collagen I-coated 96-well assay plates at 3×10⁴ cells/well (wild-type cell line) or 5×10⁴ cells/well (mutant cell lines) in 100 μL/well of DMEM growth medium containing 10% FBS. Plates are then incubated at room temperature for 30 minutes prior to an overnight incubation at 37°C with 5% CO₂. Next, cells are treated for 1 hour at 37°C, 5% CO₂ with TRK inhibitor compounds (e.g., Selitrectinib (LOXO-195)). Control wells contain either 0.25% DMSO alone or 1 μM larotrectinib or LOXO-195. Following compound incubation, growth medium is discarded and cells are lysed by addition of 60 μL/well of ice-cold lysis buffer containing protease and phosphatase inhibitors^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] The ΔTRKA, ΔTRKA-G595R, and ΔTRKA -G667C NIH-3T3 tumor cell lines (~2-3x10⁶ cells) and KM12 cells (5x10⁶ cells) are injected subcutaneously into the right flank of female nu/nu NCr mice. Tumors are allowed to grow to ~100-200 mm³ or ~500 mm³, and animals are randomized by tumor size into dosing groups of 5 (KM12), 7 (NIH 3T3 ΔTRKA variants) or 3-4 (for PK-PD) animals. Animals are dosed by oral gavage with vehicle, Selitrectinib (LOXO-195) in 1% carboxymethylcellulose/0.5% Tween-80 or larotrectinib in 100% Labrafac lipophile. All animals are obtained at 6-8 weeks of age, housed in groups of 5 and allowed a one-week acclimation period before cancer cell injection. Animals are dosed with vehicle twice daily, Selitrectinib (LOXO-195) at 30 mg/kg, 100 mg/kg and 300 mg/kg twice daily and larotrectinib at 60 mg/kg daily for 9-12 days. Body weight and tumor size are monitored after cell implantation and at regular intervals during dosing^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Drilon A, et al. A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors. Cancer Discov. 2017 Sep;7(9):963-972. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.6287 mL	13.1434 mL	26.2867 mL	65.7168 mL
	5 mM	0.5257 mL	2.6287 mL	5.2573 mL	13.1434 mL
	10 mM	0.2629 mL	1.3143 mL	2.6287 mL	6.5717 mL
	15 mM	0.1752 mL	0.8762 mL	1.7524 mL	4.3811 mL
	20 mM	0.1314 mL	0.6572 mL	1.3143 mL	3.2858 mL
	25 mM	0.1051 mL	0.5257 mL	1.0515 mL	2.6287 mL
	30 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1906 mL
	40 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6429 mL
	50 mM	0.0526 mL	0.2629 mL	0.5257 mL	1.3143 mL
	60 mM	0.0438 mL	0.2191 mL	0.4381 mL	1.0953 mL
	80 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8215 mL
	100 mM	0.0263 mL	0.1314 mL	0.2629 mL	0.6572 mL

Selitrectinib 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:

Selitrectinib2097002-61-2LOXO-195LOXO195LOXO 195Trk ReceptorTropomyosin related kinase receptorInhibitorinhibitorinhibit

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Selitrectinib (Synonyms: LOXO-195)

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