Iruplinalkib

SKU: orb1686012

Description

Iruplinalkib (WX-0593) is an oral, selective inhibitor targeting ALK and ROS1 tyrosine kinases, exhibiting potent anticancer activity. It is a research compound used in preclinical studies for non-small cell lung cancer (NSCLC), including investigations into its efficacy in both cellular and animal models.

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1854943-32-0
• MW: 569.08
• Purity: 99.29% (May vary between batches)
• Formula: C₂₉H₃₈ClN₆O₂P
• SMILES: O=P(C=1C=CC=CC1NC2=NC(=NC=C2Cl)NC3=CC=C(C=C3OC)N4CCC5(CC4)CCN(C)CC5)(C)C
• Target: STAT,BCRP,Akt,ERK,ROS Kinase,ALK
• Solubility: DMSO:5 mg/mL (8.79 mM)

Bioactivity

• In Vivo:
  METHODS: In this open-label, randomized, multicenter, phase 3 study, patients with ALK-positive NSCLC were randomized to receive iruplinalkib 180 mg once daily (7 days, 60 mg once daily) or crizotinib 250 mg twice daily. The primary endpoint was progression-free survival (PFS) assessed by an independent review committee (IRC) according to Response Evaluation Criteria in Solid Tumors version 1.1. Secondary endpoints included PFS by investigator, objective response rate (ORR), duration of response, duration of response, intracranial ORR and time to CNS progression by IRC and investigator, overall survival, and safety. An interim analysis was planned after approximately 70% of all 192 expected PFS events assessed by IRC were observed (134 events). RESULTS: Between September 4, 2019, and December 2, 2020, a total of 292 patients were randomized; 143 to iruplinalkib and 149 to crizotinib. At this interim analysis (145 events), the median follow-up was 26.7 months (range: 3.7-37.7) in the iruplinalkib group and 25.9 months (range: 0.5-35.9) in the crizotinib group. IRC-assessed PFS was significantly prolonged in patients in the iruplinalkib group (median PFS, 27.7 months [95% confidence interval (CI): 26.3-not estimable], vs. 14.6 months [95% CI: 11.1-16.5] in the crizotinib group; hazard ratio, 0.34 [98.02% CI: 0.23-0.52], p < 0.0001). IRC-assessed ORR was 93.0% (95% CI: 87.5-96.6) in the iruplinalkib group and 89.3% (95% CI: 83.1-93.7) in the crizotinib group. For patients with measurable CNS metastases at baseline, the intracranial ORR was 90.9% with iruplinalkib (10 of 11 patients, 95% CI: 58.7-99.8) and 60.0% with crizotinib (9 of 15 patients, 95% CI: 32.3-83.7). The incidence of grade 3 or 4 treatment-related adverse events was 51.7% with iruplinalkib and 49.7% with crizotinib.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ALK, WX-0593, ROS1, ROS Kinase, ROSKinase

Compound Identifiers

PubChem CID

118639856