Selpercatinib (LOXO-292)

Catalog No.S8781 Batch:S878103

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Technical Data

Formula

C29H31N7O3
Molecular Weight 525.60 CAS No. 2152628-33-4
Solubility (25°C)* In vitro DMSO 33 mg/mL (62.78 mM)
Water Insoluble
Ethanol Insoluble
* <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 Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively.
Targets
RET wt [1]
(Cell-free assay)		 RET V804M [1]
(Cell-free assay)		 RET V804L [1]
(Cell-free assay)		 RET M918T [1]
(Cell-free assay)		 RET S891A [1]
(Cell-free assay)		 View More
1 nM 2 nM 2 nM 2 nM 2 nM
In vitro

Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor.

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    NB1 cells

  • Concentrations

    1 μM

  • Incubation Time

    2 h

  • Method

    Cells were pre-treated with LOXO292 (1 µM) for 2 h before stimulation with ALKAL2 or GDNF.
Animal Study:

[3]
  • Animal Models

    Female nu/nu BALB/c mice

  • Dosages

    3 mg/kg

  • Administration

    o.g.

Selleck's Selpercatinib (LOXO-292) has been cited by 6 publications

Loss of tumor suppressor TMEM127 drives RET-mediated transformation through disrupted membrane dynamics [ Elife, 2024, 12RP89100] PubMed: 38687678
Novel therapeutic strategies targeting bypass pathways and mitochondrial dysfunction to combat resistance to RET inhibitors in NSCLC [ Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249] PubMed: 38768929
Loss of Tumour Suppressor TMEM127 Drives RET-mediated Transformation Through Disrupted Membrane Dynamics [ bioRxiv, 2023, 2023.06.28.546955] PubMed: 37425958
Novel Calcium-Binding Ablating Mutations Induce Constitutive RET Activity and Drive Tumorigenesis [ Cancer Res, 2022, 82(20):3751-3762] PubMed: 36166639
CIC-mediated modulation of MAPK signaling opposes receptor tyrosine kinase inhibitor response in kinase-addicted sarcoma [ Cancer Res, 2022, canres.1397.2021] PubMed: 35074756
Selpercatinib-Induced Hypothyroidism Through Off-Target Inhibition of Type 2 Iodothyronine Deiodinase [ JCO Precis Oncol, 2022, 6:e2100496] PubMed: 35704797

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.