Naquotinib (mesylate)

Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

Product Specifications

CAS Number

[1448237-05-5]

Product Name Alternative

ASP8273 (mesylate)

UNSPSC

12352005

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Naquotinib-mesylate.html

Concentration

10mM

Purity

98.05

Solubility

DMSO : 12.5 mg/mL (ultrasonic; warming)

Smiles

O=C(C1=NC(CC)=C(O[C@H]2CN(C(C=C)=O)CC2)N=C1NC3=CC=C(N4CCC(N5CCN(C)CC5)CC4)C=C3)N.CS(=O)(O)=O

Molecular Formula

C31H46N8O6S

Molecular Weight

658.81

References & Citations

[1]Sakagami H, et al. ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA) : AACR; Cancer Res 2014;74 (19 Suppl) :Abstract nr 1728. doi:10.1158/1538-7445.AM2014-1728|[2]Konagai S, et al. ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA) : AACR; Cancer Res 2015;75 (15 Suppl) :Abstract nr 2586. doi:10.1158/1538-7445.AM2015-2586