Iruplinalkib is an orally active, small-molecule tyrosine kinase inhibitor that selectively targets anaplastic lymphoma kinase (ALK) and ROS1. It is also known by the development code WX-0593 and has been developed as an antineoplastic agent for the treatment of advanced non-small cell lung cancer (NSCLC) associated with ALK or ROS1 rearrangements.
Iruplinalkib is chemically identified by the CAS Number 1854943-32-0, molecular formula C₂₉H₃₈ClN₆O₂P, and molecular weight 569.08 g/mol. FDA's Global Substance Registration System identifies Iruplinalkib with the UNII Z5F65W1YAZ. PubChem lists the compound under CID 118639856.
The IUPAC name of Iruplinalkib is 5-chloro-4-N-(2-dimethylphosphorylphenyl)-2-N-[2-methoxy-4-(9-methyl-3,9-diazaspiro[5.5]undecan-3-yl)phenyl]pyrimidine-2,4-diamine. It is an achiral synthetic organic compound with no defined stereocenters.
Iruplinalkib works by inhibiting ALK-mediated signaling. ALK rearrangements and mutations can drive abnormal cellular proliferation in certain cancers. By inhibiting ALK and related signaling pathways, Iruplinalkib can interfere with tumor-cell growth and survival. NCI describes activity against ALK tyrosine kinase, ALK fusion proteins and selected ALK mutation variants.
Iruplinalkib has also been characterized as a selective ALK/ROS1 inhibitor. Preclinical research has demonstrated inhibition of ALK and ROS1 signaling, while clinical studies have evaluated its activity in patients with advanced NSCLC containing ALK or ROS1 rearrangements.
Iruplinalkib has the molecular formula C₂₉H₃₈ClN₆O₂P and molecular weight 569.08 g/mol. Its PubChem-recorded exact mass is 568.2482392 Da, and its calculated XLogP3-AA is 5.4. The compound has 2 hydrogen-bond donors and 8 hydrogen-bond acceptors.
The compound is generally described as an off-white to light-yellow solid. Research-grade material has been reported to be insoluble in water, with solubility in organic solvents such as ethanol and DMSO. One reported specification gives ethanol solubility of approximately 25 mg/mL and DMSO solubility of approximately 6 mg/mL at 25°C.
Iruplinalkib is an antineoplastic tyrosine kinase inhibitor. Its principal clinical application is associated with ALK-positive advanced or metastatic non-small cell lung cancer. It has also been investigated in ROS1-rearranged NSCLC. Iruplinalkib was approved in China in 2023 for locally advanced or metastatic ALK-positive NSCLC.
Iruplinalkib inhibits ALK tyrosine kinase activity and suppresses signaling from ALK fusion proteins and mutant ALK. It also has activity against ROS1. Inhibition of these signaling pathways can reduce downstream phosphorylation and interfere with cellular proliferation and tumor growth.
These synonyms and development identifiers are documented in public pharmaceutical and chemical databases.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | ≥99.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 5.0 – 7.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |