CONTACT US
Home > Inhibitors/Agonists> > Naquotinib mesylate
Naquotinib mesylate

Naquotinib mesylate

  • CAT Number: I008240
  • CAS Number: 1448237-05-5 (mesylate)
  • Molecular Formula: C31H46N8O6S
  • Molecular Weight: 658.819
  • Purity: ≥95%
Inquiry Now

Naquotinib, also known as ASP8273, is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor with potential antineoplastic activity. Upon oral administration, ASP8273 covalently binds to and inhibits the activity of mutant forms of EGFR, including the T790M EGFR mutant, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. ASP8273 preferentially inhibits mutated forms of EGFR including T790M, a secondarily acquired resistance mutation, and may have therapeutic benefits in tumors with T790M-mediated resistance when compared to other EGFR tyrosine kinase inhibitors.

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 EGFR inhibitor
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=NC(=C(N=C1OC2CCN(C2)C(=O)C=C)NC3=CC=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)C(=O)N.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

Request a Quote

Contact Us at MuseChem

We are committed to providing you with reliable, cost-effective solutions for your chemical needs, while ensuring your safety and comfort. Our team of experts is always available to answer your questions and help you navigate the complexities of the chemical industry.

Whether you're looking for a specific product or need help with a custom synthesis project, we're here to help you discover a new world of chemical possibilities. Contact us today to learn more about how we can assist you with all of your chemical needs.

Our goal is to make the process of ordering chemicals as seamless and hassle-free as possible. Let us know how we can assist you, and we'll get back to you as soon as possible. We look forward to hearing from you!