For research use only. Not for therapeutic Use.
Naquotinib mesylate（Cat No.:I008240）is an investigational small molecule drug that acts as a tyrosine kinase inhibitor (TKI). It selectively targets epidermal growth factor receptor (EGFR) mutations, particularly those associated with non-small cell lung cancer (NSCLC), including T790M and other resistant mutations. By inhibiting EGFR signaling, Naquotinib mesylate blocks tumor cell proliferation and survival, offering a potential treatment for patients with EGFR-mutant NSCLC who have developed resistance to first- and second-generation EGFR inhibitors. It is being studied in clinical trials to evaluate its safety, efficacy, and ability to overcome drug resistance in lung cancer.
| Catalog Number | I008240 |
| CAS Number | 1448237-05-5 (mesylate) |
| Synonyms | ASP8273; ASP-8273; ASP 8273; ASP8273 mesilate; Naquotinib mesylate;6-Ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-(((3R)-1-(1-oxoprop-2-en-1-yl)pyrrolidin-3-yl)oxy)pyrazine-2-carboxamide monomethanesulfonate |
| Molecular Formula | C31H46N8O6S |
| Purity | ≥95% |
| Target | Protein Tyrosine Kinase/RTK |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IUPAC Name | 6-ethyl-3-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-[(3R)-1-prop-2-enoylpyrrolidin-3-yl]oxypyrazine-2-carboxamide;methanesulfonic acid |
| InChI | InChI=1S/C30H42N8O3.CH4O3S/c1-4-25-30(41-24-12-15-38(20-24)26(39)5-2)34-29(27(33-25)28(31)40)32-21-6-8-22(9-7-21)36-13-10-23(11-14-36)37-18-16-35(3)17-19-37;1-5(2,3)4/h5-9,23-24H,2,4,10-20H2,1,3H3,(H2,31,40)(H,32,34);1H3,(H,2,3,4)/t24-;/m1./s1 |
| InChIKey | ALDUQYYVQWGTMR-GJFSDDNBSA-N |
| SMILES | CCC1=C(N=C(C(=N1)C(=O)N)NC2=CC=C(C=C2)N3CCC(CC3)N4CCN(CC4)C)O[C@@H]5CCN(C5)C(=O)C=C.CS(=O)(=O)O |
| Reference | </br>1:Balancing Low-density Lipoprotein Cholesterol Reduction and Hepatotoxicity With Lomitapide Mesylate and Mipomersen in Patients With Homozygous Familial Hypercholesterolemia. Won JI, Zhang J, Tecson KM, McCullough PA.Rev Cardiovasc Med. 2017;18(1):21-28. PMID: 28509890 </br>2:Formulation and characterization of Phospholipon® 90 G and Tween<sup>®</sup> 80 based transfersomes for transdermal delivery of eprosartan mesylate. Ahad A, Al-Saleh AA, Al-Mohizea AM, Al-Jenoobi FI, Raish M, Yassin AEB, Alam MA.Pharm Dev Technol. 2017 May 15:1-27. doi: 10.1080/10837450.2017.1330345. [Epub ahead of print] PMID: 28504046 </br>3:Imatinib mesylate- and dasatinib-induced eosinophilia in a patient with chronic myelocytic leukemia. McGrath K, Stein B, Kalhagen L, Leighton L.Ann Allergy Asthma Immunol. 2017 May 9. pii: S1081-1206(17)30338-1. doi: 10.1016/j.anai.2017.04.022. [Epub ahead of print] No abstract available. PMID: 28499700 </br>4:Clinical efficacy of eribulin mesylate for the treatment of metastatic soft tissue sarcoma. Emambux S, Italiano A.Expert Opin Pharmacother. 2017 May 4. doi: 10.1080/14656566.2017.1326908. [Epub ahead of print] PMID: 28468516 </br>5:Effects of deferoxamine mesylate on hematoma and perihematoma edema after traumatic intracerebral hemorrhage. Yu J, Yuan Q, Sun YR, Wu X, Du ZY, Li ZQ, Wu XH, Zhou LF, Wu G, Hu J.J Neurotrauma. 2017 May 2. doi: 10.1089/neu.2017.5033. [Epub ahead of print] PMID: 28462672 </br>6:Novel t(5;11)(q32;q13.4) with NUMA1-PDGFRB fusion in a myeloid neoplasm with eosinophilia with response to imatinib mesylate. Zou YS, Hoppman NL, Singh ZN, Sawhney S, Kotiah SD, Baer MR.Cancer Genet. 2017 Apr;212-213:38-44. doi: 10.1016/j.cancergen.2017.03.004. Epub 2017 Mar 27. PMID: 28449810 </br>7:Inhibition of the platelet-derived growth factor receptor beta (PDGFRB) using gene silencing, crenolanib besylate, or imatinib mesylate hampers the malignant phenotype of mesothelioma cell lines. Melaiu O, Catalano C, De Santi C, Cipollini M, Figlioli G, Pellè L, Barone E, Evangelista M, Guazzelli A, Boldrini L, Sensi E, Bonotti A, Foddis R, Cristaudo A, Mutti L, Fontanini G, Gemignani F, Landi S.Genes Cancer. 2017 Jan;8(1-2):438-452. doi: 10.18632/genesandcancer.129. PMID: 28435517 Free PMC Article</br>8:Efficacy of the dual PI3K and mTOR inhibitor NVP-BEZ235 in combination with imatinib mesylate against chronic myelogenous leukemia cell lines. Xin P, Li C, Zheng Y, Peng Q, Xiao H, Huang Y, Zhu X.Drug Des Devel Ther. 2017 Apr 3;11:1115-1126. doi: 10.2147/DDDT.S132092. eCollection 2017. PMID: 28435223 Free PMC Article</br>9:Neuroendocrine tumor of cecum in patient treated with imatinib mesylate for blastic phase of chronic myeloid leukemia. Novaković S, Kovač Peić A, Holik H, Coha B.Acta Clin Belg. 2017 Apr 19:1-4. doi: 10.1080/17843286.2017.1316005. [Epub ahead of print] PMID: 28420292 </br>10:A case of xanthoma disseminatum treated with imatinib mesylate. Sawatkar GU, Vinay K, Malhotra P, Nahar Saikia U, Dogra S.Dermatol Ther. 2017 Apr 12. doi: 10.1111/dth.12489. [Epub ahead of print] No abstract available. PMID: 28401671 |
