Nemtabrutinib (ARQ-531)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$1450	Check With Us
500mg	$2080	Check With Us
1g	$3120	Check With Us

: [email protected] [email protected]

Cat #: V4775 CAS #: 2095393-15-8 Purity ≥ 98%

Description: Nemtabrutinib (ARQ531; ARQ-531; MK-1026) is a novel, potent, orally bioavailable, and reversible / non-covalent BTK (Bruton's Tyrosine Kinase) inhibitor with potential antitumor activity. It inhibits WT-BTK and C481S-BTK with IC50s of 0.85 nM and 0.39 nM, respectively.

References: [1]. S Eathiraj, et al. Targeting PCI-32765-Resistant BTK-C481S Mutation with ARQ 531, a Reversible Non-Covalent Inhibitor of BTK. Clinical Lymphoma Myeloma & Leukemia, 2016, 16: S47-S48.

Top Publications Citing Invivochem Products

Product Catalog 2022

Guide to Product Handling

Publications Citing InvivoChem Products

Product Promise

Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	478.933
Molecular Formula	C25H23ClN4O4
CAS No.	2095393-15-8
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
SMILES Code	O=C(C1=CC=C(OC2=CC=CC=C2)C=C1Cl)C3=CNC4=NC=NC(N[C@H]5CO[C@H](CO)CC5)=C43
Synonyms	ARQ531; MK1026; ARQ-531; MK-1026; ARQ 531;

Protocol	In Vitro	ARQ 531 shows strong target inhibition in TMD8 cell line. The IC50 values are 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively, in biochemical assay. Additionally, ARQ 531 also shows strong inhibition of TEK kinases with IC50s of 5.23 nM (BMX), 5.80 nM (TEC), 36.4 nM (TXK). The IC50s of ARQ 531 for SRC kinases are 3.86 nM (LCK), 4.22 nM (YES), 9.71 nM (BLK), 18.3 nM (HCK), 18.8 nM (LYNa), 25.9 nM (FGR), 32.2 nM (FYN), 48.0 nM (FRK) and for TRK kinases are 11.7 nM (TrkB), 13.1 nM (TrkA), 19.1 nM (TrkC). ARQ 531 inhibits proliferation of diverse types of cell lines (TMD8: GI50=0.13 μM, REC1: GI50=0.18 nM) and shows potency in cell lines that are addict to BCR, Src-family kinase and PI3K/AKT pathways.
Protocol	In Vivo	ARQ 531 is efficacious in TMD-8 tumor xenograft model. ARQ 531 causes complete tumor regression after 14 days of treatment. ARQ 531 is also efficacious in collagen induced arthritis model. ARQ 531 demonstrates potent efficacy against arthritis in mouse model. In the BTK driven TMD8 xenograft mouse model, ARQ 531 demonstrates excellent anti-tumor activity with durable response. ARQ 531 demonstrates in vivo efficacy in a mouse collagen-induced arthritis (CIA) model.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.0880 mL	10.4399 mL	20.8797 mL	41.7595 mL
5mM	0.4176 mL	2.0880 mL	4.1759 mL	8.3519 mL
10mM	0.2088 mL	1.0440 mL	2.0880 mL	4.1759 mL
20mM	0.1044 mL	0.5220 mL	1.0440 mL	2.0880 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.