An ALK inhibitor
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Iruplinalkib

Item No. 46228

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-chloro-N-[2-(dimethylphosphinyl)phenyl]-N-[2-methoxy-4-(9-methyl-3,9-diazaspiro[5.5]undec-3-yl)phenyl]-2,4-pyrimidinediamine
CAS Number
1854943-32-0
Synonyms
  • WX-0593
Molecular Formula
C29H38ClN6O2P
Formula Weight
569.1
Purity
≥95%
Formulation (Request formulation change)
A solid
SMILES
ClC1=CN=C(NC2=CC=C(N3CCC4(CCN(CC4)C)CC3)C=C2OC)N=C1NC5=C(P(C)(C)=O)C=CC=C5
InChi Code
InChI=1S/C29H38ClN6O2P/c1-35-15-11-29(12-16-35)13-17-36(18-14-29)21-9-10-23(25(19-21)38-2)33-28-31-20-22(30)27(34-28)32-24-7-5-6-8-26(24)39(3,4)37/h5-10,19-20H,11-18H2,1-4H3,(H2,31,32,33,34)
InChi Key
ZPCCNHQDFZCULN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Iruplinalkib is an inhibitor of anaplastic lymphoma kinase (ALK), ALKL1196M, and ALKC1156Y (IC50s = 1.6, 1.7, and 1.8 nM, respectively).1 It inhibits the proliferation of Ba/F3 cells expressing wild-type ALK, ALKL1196M, ALKC1156Y, or a variety of ALK fusion proteins (IC50s = 13, 24, 21, and 1-96 nM, respectively) and Karpas 299 anaplastic large-cell lymphoma (ALCL) cells (IC50 = 14.5 nM). Iruplinalkib also inhibits the proliferation of Ba/F3 cells expressing wild-type c-Ros oncogene 1 (ROS1) or ROS1 fusion proteins (IC50s = 11 and 12-22 nM, respectively). It reduces tumor growth in a crizotinib-resistant patient-derived xenograft (PDX) mouse model of non-small cell lung cancer (NSCLC) at 2.5-10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, X., Zhang, L., Wan, H., et al. Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. Bioorg. Med. Chem. Lett. 66, 128730 (2022).