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Pirtobrutinib (LOXO-305) BTK inhibitor

Name: Pirtobrutinib (LOXO-305)
Brand: Selleck Chemicals
SKU: S9825
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S9825

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.

Chemical Structure

Molecular Weight: 479.43

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	EGFR VEGFR JAK FGFR PDGFR Src HIF FLT3 HER2 FLT
Other BTK Inhibitors	Catadegbrutinib (BGB-16673) Spebrutinib (AVL-292) tirabrutinib(ONO-4059) hydrochloride LFM-A13 CGI1746 Evobrutinib BMS-935177 CNX-774 Branebrutinib (BMS-986195) Fenebrutinib (GDC-0853)

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (200.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.900mg/ml (10.22mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.67mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	479.43	Formula	C₂₂H₂₁F₄N₅O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2101700-15-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY 3527727, RXC-005			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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	BTK (in WT BTK HEK cells) 5.69 nM
In vitro	LOXO-305 (Pirtobrutinib) 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>
References	[1] https://ashpublications.org/blood/article/134/Supplement_1/478/426456/LOXO-305-Targeting-C481S-Bruton-Tyrosine-Kinase-in [2] https://www.sciencedirect.com/science/article/pii/S0006497118625728

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-11)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07220187	NOT_YET_RECRUITING	Richter Syndrome; Transformed Chronic Lymphocytic Leukemia to Diffuse Large B-Cell Lymphoma; Transformed Small Lymphocytic Lymphoma to Diffuse Large B-Cell Lymphoma	SWOG Cancer Research Network	2026-08-31	PHASE3
NCT07548450	NOT_YET_RECRUITING	Waldenstrom Macroglobulinemia	University of Utah	2026-06	PHASE2
NCT07285590	RECRUITING	Mantle Cell Lymphoma (MCL)	Grupo Español de Linfomas y Transplante Autólogo de Médula Ósea	2025-09-30	PHASE2
NCT07784101	NOT_YET_RECRUITING	Relapsed or Refractory Mantle Cell Lymphoma (MCL)	Beijing InnoCare Pharma Tech Co., Ltd.	2026-10	PHASE3
NCT05833763	RECRUITING	Mantle Cell Lymphoma; Mantle Cell Lymphoma Refractory	Australasian Leukaemia and Lymphoma Group	2023-10-12	PHASE2
NCT06390956	RECRUITING	Marginal Zone Lymphoma	University of Utah	2025-02-20	PHASE2

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