Home Angiogenesis BTK inhibitor Nemtabrutinib (ARQ 531) For research use only.

Nemtabrutinib (ARQ 531)

Synonyms: MK-1026

Nemtabrutinib (ARQ 531, MK-1026) is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases.

Nemtabrutinib (ARQ 531) Chemical Structure

Nemtabrutinib (ARQ 531) Chemical Structure

CAS No. 2095393-15-8

Purity & Quality Control

Batch: S871101 DMSO]95 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Purity: 99.31%
99.31

Nemtabrutinib (ARQ 531) Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Biological Activity

Description Nemtabrutinib (ARQ 531, MK-1026) is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases.
Targets
BTK [1]
(Cell-free assay)		 BRK [1]
(Cell-dree)		 BRK [1]
(Cell-free assay)		 LCK [1]
(Cell-free)		 LCK [1]
(Cell-free assay)		 Click to View More Targets
0.85 nM 2.45 nM 2.45 nM 3.86 nM 3.86 nM
In vitro
In vitro

ARQ 531 potently inhibited BTK (IC50 = 0.85 nM), the binding potency was accompanied by long residence time (51 min). ARQ 531 selectively inhibits BCR signaling dependent PI3K/AKT/mTOR, Ras/Raf/Erk and Rap-GTPase-Cofilin pathways in TMD8 cells.  In GCB-DLBCL cell lines (SUDHL-4 and DOHH-2), ARQ 531 potently suppressed expression of anti-apoptotic c-Myc and BCL6 oncoproteins in a dose dependent fashion, and concomitantly induced apoptotic cleavage of PARP protein[2].
Cell Research Cell lines CLL cells
Concentrations 0.1 μM, 1.0 μM, or 10.0 μM
Incubation Time 72 h
Method

--
In Vivo
In vivo

ARQ 531 has potent anti-tumor activity was observed in both ABC-DLBCL and GCB-DLBCL mouse xenograft models[1]. ARQ 531 crosses the blood, brain-barrier[2]. In a single oral dose study of 10mg/kg in monkeys, the bioavailability of ARQ 531 is 72.4% with a Cmax of 9 μM and a half-life greater than 24 hours[3].
Animal Research Animal Models B6 mice engrafted with 1E7 CD5+/CD19+ TCL1 lymphocytes via tail vein injection
Dosages 50 or 75 mg/kg
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05673460 Active not recruiting
Mature B-cell Neoplasms
Merck Sharp & Dohme LLC
 February 13 2023 Phase 1
NCT05347225 Active not recruiting
Hematological Malignancies
Merck Sharp & Dohme LLC
 June 9 2022 Phase 1
NCT04728893 Recruiting
Hematologic Malignancies|Waldenstroms Macroglobulinaemia|Non-Hodgkins Lymphoma|Chronic Lymphocytic Leukaemia
Merck Sharp & Dohme LLC
 April 5 2021 Phase 2
NCT03162536 Active not recruiting
Lymphoma B-Cell|Small Lymphocytic Lymphoma|Chronic Lymphocytic Leukemia|Waldenstrom Macroglobulinemia|Mantle Cell Lymphoma|Diffuse Large B Cell Lymphoma|Richter''s Transformation|Follicular Lymphoma|Marginal Zone Lymphoma
ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA)
 June 26 2017 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 478.93 Formula

C25H23ClN4O4
CAS No. 2095393-15-8 SDF --
Smiles C1CC(OCC1NC2=NC=NC3=C2C(=CN3)C(=O)C4=C(C=C(C=C4)OC5=CC=CC=C5)Cl)CO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (198.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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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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