Pirtobrutinib (LOXO-305)

Catalog No.S9825 Batch:S982501

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 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.9mg/ml
	5% DMSO 1 95% Corn oil	0.8mg/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.

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.

References

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

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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