Pirtobrutinib (LOXO-305)

Catalog No.S9825 Batch:S982501

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Technical Data

Formula

C22H21F4N5O3

Molecular Weight 479.43 CAS No. 2101700-15-4
Solubility (25°C)* In vitro DMSO 96 mg/mL (200.23 mM)
Ethanol 48 mg/mL (100.11 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
0.8mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.9mg/ml
* <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

Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases.

Targets
BTK [1]
(in WT BTK HEK cells)
5.69 nM
In vitro

Pirtobrutinib (LOXO-305) is a highly selective, non-covalent, next-generation Bruton's tyrosine kinase (BTK) inhibitor, which potently inhibits the cellular activity of BTK C481S, T and R mutations and displays strong equilibrium binding to WT BTK and several BTK C481 substitution mutations.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Cell Assay:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Cell lines

    WT BTK HEK293T cells

  • Concentrations

    --

  • Incubation Time

    2 h

  • Method

    HEK293T cell lines transiently expressing WT BTK and BTK C481 substitution mutations were incubated with LOXO-305, ibrutinib or acalabrutinib for 30 min followed by the addition of orthovanadate. After 2 h, cells were lysed, and phosphorylated Y223 BTK and total BTK levels were detected by immunoblot (BTK WT, C481S, and C481T) or MesoScale (C481R). Bands and MSD signals were quantified, and the IC50 values calculated with GraphPad Prism.

Selleck's Pirtobrutinib (LOXO-305) has been cited by 1 publication

Cotargeting of BTK and MALT1 overcomes resistance to BTK inhibitors in mantle cell lymphoma [ J Clin Invest, 2023, 133(3)e165694] PubMed: 36719376

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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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