Selitrectinib (LOXO-195)

Catalog No.S8636 Batch:S863602

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Technical Data

Formula

C20H21FN6O 
Molecular Weight 380.42 CAS No. 2097002-61-2
Solubility (25°C)* In vitro DMSO 42 mg/mL (110.4 mM)
Ethanol 15 mg/mL (39.43 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)		 View More
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 (from reference)

Cell Assay:

[2]
  • Cell lines

    GON4L-NTRK cells

  • Concentrations

    50 nM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentration of drug for 24 h.
Animal Study:

[3]
  • Animal Models

    Mice

  • Dosages

    10 mg/kg

  • Administration

    p.o.

Selleck's Selitrectinib (LOXO-195) has been cited by 3 publications

Hepatic stellate cells maintain liver homeostasis through paracrine neurotrophin-3 signaling that induces hepatocyte proliferation [ Sci Signal, 2023, 16(787):eadf6696] PubMed: 37253090
JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo [ Molecules, 2022, 27(19)6500] PubMed: 36235036
TRK Fusions are Enriched in Cancers with Uncommon Histologies and the Absence of Canonical Driver Mutations. [ Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-3165] PubMed: 31871300

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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