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Pirtobrutinib (LOXO-305)

Name: Pirtobrutinib (LOXO-305)
Brand: Selleck Chemicals
SKU: S9825
Rating: 5 (1 reviews)

Synonyms: LY 3527727, RXC-005

Catalog No.S9825 Purity: 99.92%

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.

Pirtobrutinib (LOXO-305) Chemical Structure

CAS: 2101700-15-4

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

Purity & Quality Control

Batch: S982501 DMSO] 96 mg/mL] false] Ethanol] 48 mg/mL] false] Water] Insoluble] false Purity: 99.92%

99.92

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Biological Activity

Description

Targets

BTK ^[1]
(in WT BTK HEK cells)

5.69 nM

In vitro
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>
Cell Research	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.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06104683	Not yet recruiting	Relapsing Multiple Sclerosis\|Multiple Sclerosis	Loxo Oncology Inc.\|Eli Lilly and Company	May 1 2024	Phase 2
NCT05990465	Not yet recruiting	Non Hodgkin Lymphoma\|Diffuse Large B Cell Lymphoma\|Follicular Lymphoma\|Marginal Zone Lymphoma\|Mantle Cell Lymphoma\|Burkitt Lymphoma	Medical College of Wisconsin	February 2024	Phase 1
NCT05023980	Recruiting	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	Loxo Oncology Inc.\|Eli Lilly and Company	September 23 2021	Phase 3
NCT04965493	Recruiting	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	Loxo Oncology Inc.\|Eli Lilly and Company	September 20 2021	Phase 3
NCT05024045	Active not recruiting	Leukemia Lymphocytic Chronic B-Cell\|Lymphoma B-cell Marginal Zone\|Lymphoma Non-Hodgkin\|Multiple Myeloma\|B-cell Lymphoma\|Waldenstrom Macroglobulinemia\|Lymphoma Mantle-Cell	Eli Lilly and Company\|Loxo Oncology Inc.	September 30 2021	Phase 1

References

Chemical lnformation & Solubility

Molecular Weight	479.43	Formula	C₂₂H₂₁F₄N₅O₃
CAS No.	2101700-15-4	SDF	--
Smiles	COC1=CC=C(F)C=C1C(=O)NCC2=CC=C(C=C2)C3=N[N](C(C)C(F)(F)F)C(=C3C(N)=O)N
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 96 mg/mL ( (200.23 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

Handling Instructions

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