1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

Naquotinib mesylate (Synonyms: ASP8273)

Cat. No.: HY-19803 Purity: 98.59% ee.: 99.85%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
Naquotinib mesylate Chemical Structure

Naquotinib mesylate Chemical Structure

CAS No. : 1448237-05-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO $507 In-stock
1 mg $120 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
25 mg $990 In-stock
50 mg $1500 In-stock
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Description

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

IC50 & Target

IC50: 230 nM (EGFR); 8-33 (EGFR mutants)[1]

In Vitro

In assays using endogenously EGFR-dependent cells, Naquotinib inhibits the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC50s values of 8-33 nM[1]. Naquotinib selectively inhibits phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective[2].

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].

Clinical Trial
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References
Molecular Weight

658.81

Formula

C₃₁H₄₆N₈O₆S

CAS No.

1448237-05-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 12.5 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Naquotinib mesylate
Cat. No.:
HY-19803
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