Iruplinalkib
Iruplinalkib Basic information
- Product Name:
- Iruplinalkib
- Synonyms:
-
- 2,4-Pyrimidinediamine, 5-chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-(9-methyl-3,9-diazaspiro[5.5]undec-3-yl)phenyl]-
- Iruplinalkib
- lruplinalkib
- Iruplinalkib/WX-0593
- (2-((5-Chloro-2-((2-methoxy-4-(9-methyl-3,9-diazaspiro[5.5]undecan-3-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide
- CAS:1854943-32-0
- CAS:
- 1854943-32-0
- MF:
- C29H38ClN6O2P
- MW:
- 569.08
- Mol File:
- 1854943-32-0.mol
Iruplinalkib Chemical Properties
- Boiling point:
- 769.1±70.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- pka
- 10.12±0.20(Predicted)
- form
- Solid
- color
- Off-white to light yellow
- InChIKey
- ZPCCNHQDFZCULN-UHFFFAOYSA-N
- SMILES
- C1(NC2=CC=C(N3CCC4(CCN(C)CC4)CC3)C=C2OC)=NC=C(Cl)C(NC2=CC=CC=C2P(C)(C)=O)=N1
Iruplinalkib Usage And Synthesis
Uses
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer[1][2].
in vivo
Iruplinalkib (2.5-10 mg/kg; Oral administration; 3 weeks) has antitumor effect in mouse model of non-small cell lung cancer[1]
| Animal Model: | EML4-ALK transfected NCI-H3122 treated female BALB/c nude mice (4-6 weeks old)[1] |
| Dosage: | 2.5, 5 and 10 mg/kg |
| Administration: | Oral administration (p.o.); 3 weeks |
| Result: | Inhibited tumor growth. Had inhibitory effects on the phosphorylation of ALK, AKT and ERK. Decreased the levels of phosphorylation of STAT3 and STAT5. Had no effect on the body weight. |
References
[1] Yang Y, et al. Iruplinalkib (WX 0593), a novel ALK/ROS1 inhibitor, overcomes crizotinib resistance in preclinical models for non-small cell lung cancer. Invest New Drugs. 2023 Apr;41(2):254-266. DOI:10.1007/s10637-023-01350-x
[2] Shi Y, et al. Safety and activity of WX-0593 (Iruplinalkib) in patients with ALK- or ROS1-rearranged advanced non-small cell lung cancer: a phase 1 dose-escalation and dose-expansion trial. Signal Transduct Target Ther. 2022;7(1):25. DOI:10.1038/s41392-021-00841-8
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