A BTK inhibitor
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ARQ 531

Item No. 30165

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,5-anhydro-2-[[5-(2-chloro-4-phenoxybenzoyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2,3,4-trideoxy-D-erythro-hexitol
CAS Number
2095393-15-8
Synonyms
  • MK-1026
  • Nemtabrutinib
Molecular Formula
C25H23ClN4O4
Formula Weight
478.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
O=C(C1=CC=C(OC2=CC=CC=C2)C=C1Cl)C3=CNC4=C3C(N[C@H]5CO[C@H](CO)CC5)=NC=N4
InChi Code
InChI=1S/C25H23ClN4O4/c26-21-10-17(34-16-4-2-1-3-5-16)8-9-19(21)23(32)20-11-27-24-22(20)25(29-14-28-24)30-15-6-7-18(12-31)33-13-15/h1-5,8-11,14-15,18,31H,6-7,12-13H2,(H2,27,28,29,30)/t15-,18+/m1/s1
InChi Key
JSFCZQSJQXFJDS-QAPCUYQASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $97

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    10 mg

    $165

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    25 mg

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    Product Description

    ARQ 531 is an inhibitor of Bruton's tyrosine kinase (BTK; IC50 = 0.85 nM).1 It reduces the viability of, and inhibits BTK autophosphorylation in, OCI-AML-2 acute myeloid leukemia (AML) cells when used at concentrations of 0.3 and 1 µM.2 In vivo, ARQ 531 (75 mg/kg) reduces tumor growth in an SU-DHL-4 B cell lymphoma mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Eathiraj, S., Yu, Y., Savage, R., et al. Abstract 1963: ARQ 531, a potent reversible BTK inhibitor, exhibits potent antitumor activity in ibrutinib-resistant diffuse large B-cell lymphoma. Cancer Res. 78(13 Suppl), 1963 (2018).

    2. Soncini, D., Orecchioni, S., Ruberti, S., et al. The new small tyrosine kinase inhibitor ARQ531 targets acute myeloid leukemia cells by disrupting multiple tumor-addicted programs. Haematologica 105(10), 2420-2431 (2020).