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
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
EGFR/ErbB1/HER1
Available Sizes
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