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Pirtobrutinib (LOXO-305) BTK inhibitor

Name: Pirtobrutinib (LOXO-305)
Brand: Selleck Chemicals
SKU: S9825
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S9825

LOXO-305 (Pirtobrutinib, 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. This compound 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 PDGFR FGFR Src HIF FLT FLT3 HER2
Other BTK Inhibitors	Catadegbrutinib (BGB-16673) Spebrutinib (AVL-292) tirabrutinib(ONO-4059) hydrochloride CGI1746 LFM-A13 Evobrutinib CNX-774 Branebrutinib (BMS-986195) BMS-935177 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

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 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06104683	Withdrawn	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	April 2024	Phase 1
NCT06333262	Recruiting	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	Inhye Ahn\|Loxo Oncology Inc.\|Dana-Farber Cancer Institute	April 22 2024	Phase 2
NCT06258174	Completed	Healthy	Eli Lilly and Company\|Loxo Oncology Inc.	September 28 2021	Phase 1
NCT05023980	Active not recruiting	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	Loxo Oncology Inc.\|Eli Lilly and Company	September 23 2021	Phase 3

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