Selitrectinib (LOXO-195)

For research use only.

Catalog No.S8636 Synonyms: BAY 2731954

1 publication

Selitrectinib (LOXO-195) Chemical Structure

CAS No. 2097002-61-2

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.

Selleck's Selitrectinib (LOXO-195) has been cited by 1 publication

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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)
0.6 nM 2 nM 2.3 nM 2.5 nM 2.5 nM
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].

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].

Protocol

Solubility (25°C)

In vitro DMSO 38 mg/mL (99.88 mM)
Ethanol 15 mg/mL (39.43 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.42
Formula

C20H21FN6

CAS No. 2097002-61-2
Storage powder
in solvent
Synonyms BAY 2731954
Smiles CC1CCC2=C(C=C(C=N2)F)C3CCCN3C4=NC5=C(C=NN5C=C4)C(=O)N1

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04275960 Completed Drug: Selitrectinib (BAY2731954) Solid Tumors Harboring NTRK Fusion Bayer February 28 2020 Phase 1
NCT03215511 Recruiting Drug: Selitrectinib (BAY2731954) Solid Tumors Harboring NTRK Fusion Bayer July 3 2017 Phase 1|Phase 2

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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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID