Home Protein Tyrosine Kinase Trk receptor inhibitor Selitrectinib (LOXO-195) For research use only.

Selitrectinib (LOXO-195)

Synonyms: BAY 2731954

Selitrectinib (LOXO-195, BAY 2731954) is an orally available, highly potent, and selective TRK kinase inhibitor with low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, IC50s ranging from 2.0 to 9.8 nmol/L. It is more than 1,000-fold selective for 98% of non-TRK kinases tested.

Selitrectinib (LOXO-195) Chemical Structure

Selitrectinib (LOXO-195) Chemical Structure

CAS No. 2097002-61-2

Purity & Quality Control

Selitrectinib (LOXO-195) Related Products

Signaling Pathway

Trk receptor Signaling Pathways

Trk receptor Signaling Pathway

Biological Activity

Description Selitrectinib (LOXO-195, BAY 2731954) is an orally available, highly potent, and selective TRK kinase inhibitor with low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, IC50s ranging from 2.0 to 9.8 nmol/L. It is more than 1,000-fold selective for 98% of non-TRK kinases tested.
Targets
WT TRKA [1]
(Celll-free assay)		 TRKA G595R [1]
(Cell-free assay)		 TRKC G623R [1]
(Cell-free assay)		 WT TRKC [1]
(Cell-free assay)		 TRKC G696A [1]
(Cell-free assay)		 Click to View More Targets
0.6 nM 2 nM 2.3 nM 2.5 nM 2.5 nM
In vitro
In vitro

LOXO-195 potently inhibits diverse activated TRK kinases in vitro. At a concerntration of 1 μM, which is approximately 1,667-fold higher than its IC50 for TRKA (0.6 nmol/L), LOXO-195 is more than 1,000-fold selective for 98% of non-TRK kinases tested (228 individual kinases). LOXO-195 demonstrates potent inhibition of cell proliferation in TRK fusion–containing KM12, CUTO-3, and MO-91 cell lines (IC50 ≤ 5 nmol/L). In contrast, LOXO-195 treatment with concentrations up to 10 μmol/L has no inhibitory effect on the growth of the 84 cell lines that did not contain a TRK fusion[1].
Cell Research Cell lines GON4L-NTRK cells
Concentrations 50 nM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.
In Vivo
In vivo

LOXO-195 is effective at reducing phosphorylated TRKA in tumors driven by ΔTRKA. LOXO-195 also causes inhibition of tumor growth relative to vehicle at all doses in four TRKA-dependent tumor models (NIH 3T3 ΔTRKA, ΔTRKA G595R, ΔTRKA G667C, and TPM3-NTRK1 fusion-positive KM12 colorectal cancer cells)[1].
Animal Research Animal Models Mice
Dosages 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04275960 Completed
Solid Tumors Harboring NTRK Fusion
Bayer
 February 28 2020 Phase 1
NCT03215511 Completed
Solid Tumors Harboring NTRK Fusion
Bayer
 July 3 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 380.42 Formula

C20H21FN6O 
CAS No. 2097002-61-2 SDF --
Smiles CC1CCC2=C(C=C(C=N2)F)C3CCCN3C4=NC5=C(C=NN5C=C4)C(=O)N1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 38 mg/mL ( (99.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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