Naquotinib (mesylate)
- Product Name
- Naquotinib (mesylate)
- CAS No.
- 1448237-05-5
- Chemical Name
- Naquotinib (mesylate)
- Synonyms
- ASP8273 (mesylate);Naquotinib (mesylate);Naquotinib mesylate (ASP-8273);Naquotinib mesylate (ASP8273 mesylate);EGFR,ASP8273,ErbB-1,ASP 8273,Inhibitor,Naquotinib mesylate,ASP-8273,HER1,Epidermal growth factor receptor,inhibit,Naquotinib
- CBNumber
- CB63155066
- Molecular Formula
- C31H46N8O6S
- Formula Weight
- 658.81194
- MOL File
- 1448237-05-5.mol
Naquotinib (mesylate) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : 12.5 mg/mL (18.97 mM)
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-5468
- Product name
- Naquotinibmesylate
- Purity
- 98.19%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-5468
- Product name
- Naquotinibmesylate
- Purity
- 98.19%
- Packaging
- 10mg
- Price
- $170
- Updated
- 2021/12/16
- Product number
- CS-5468
- Product name
- Naquotinibmesylate
- Purity
- 98.19%
- Packaging
- 25mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-5468
- Product name
- Naquotinibmesylate
- Purity
- 98.19%
- Packaging
- 50mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- orb611426
- Product name
- Naquotinib mesylate
- Packaging
- 5mg
- Price
- $569.5
- Updated
- 2021/12/16
Naquotinib (mesylate) Chemical Properties,Usage,Production
Uses
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.
in vivo
Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor is achieved after 14-days of Naquotinib treatment. Complete regression is maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment[2].
IC 50
EGFRL858R/T790M; EGFRL858R; EGFRExon 19 deletion; EGFRExon 19 deletion/T790M; EGFR: 230 nM (IC50)
References
[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
Naquotinib (mesylate) Preparation Products And Raw materials
Raw materials
Preparation Products
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