Limertinib
Limertinib, also known as ASK120067, is an EGFR inhibitor. ASK120067 displayed potent in vitro inhibitory efficacy against Bruton's tyrosine kinase protein and interleukin-2-inducible T cell kinase protein via covalent binding. In cell-based assays, ASK120067 dose-dependently suppressed Bruton's tyrosine kinase phosphorylation and exhibited anti-proliferation potency by inducing apoptosis in numerous B-lymphoma cells. Meanwhile, it caused growth arrest and induced the apoptosis of T-cell leukemia cells by attenuating interleukin-2-inducible T cell kinase activation. Oral administration of ASK120067 led to significant tumor regression in B-cell lymphoma and T-cell leukemia xenograft models by weakening Bruton's tyrosine kinase and interleukin-2-inducible T cell kinase signaling, respectively.
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Chemical Information
| Name | Limertinib |
|---|---|
| Iupac Chemical Name | N-(5-((5-chloro-4-(naphthalen-2-ylamino)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide |
| Synonyms | ASK120067; ASK 120067; ASK-120067; limertinib, |
| Molecular Formula | C29H32ClN7O2 |
| Molecular Weight | 546.06 |
| Smile | CN(CCN(C)C)C1=CC(OC)=C(NC2=NC=C(Cl)C(NC3=CC(C=CC=C4)=C4C=C3)=N2)C=C1NC(C=C)=O |
| InChiKey | QHPVTCLSVVUPOF-UHFFFAOYSA-N |
| InChi | InChI=1S/C29H32ClN7O2/c1-6-27(38)33-23-16-24(26(39-5)17-25(23)37(4)14-13-36(2)3)34-29-31-18-22(30)28(35-29)32-21-12-11-19-9-7-8-10-20(19)15-21/h6-12,15-18H,1,13-14H2,2-5H3,(H,33,38)(H2,31,32,34,35) |
| CAS Number | 1934259-00-3 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Cui X, Wang S, Gao H, Li B, Shi Y, Guo H, Song T, Zheng X. Development of an LC-MS/MS method for quantifying ASK120067, a novel mutant-selective inhibitor of the epidermal growth factor receptor (EGFR) as well as its main metabolite in human plasma and its application in a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2021 Jan 1;1162:122488. doi: 10.1016/j.jchromb.2020.122488. Epub 2020 Dec 7. PMID: 33360679.
2: Zhang T, Qu R, Chan S, Lai M, Tong L, Feng F, Chen H, Song T, Song P, Bai G, Liu Y, Wang Y, Li Y, Su Y, Shen Y, Sun Y, Chen Y, Geng M, Ding K, Ding J, Xie H. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90. doi: 10.1186/s12943-020-01202-9. Erratum in: Mol Cancer. 2021 Aug 17;20(1):102. PMID: 32404161; PMCID: PMC7218543.
Chemical Structure
