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 is a mutant-selective irreversible EGFR inhibitor with IC50 of 70 nM for NCI-H1650 cell growth,inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations.

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Naquotinib mesylate Chemical Structure

Naquotinib mesylate Chemical Structure

CAS No. : 1448237-05-5

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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 is a mutant-selective irreversible EGFR inhibitor with IC50 of 70 nM for NCI-H1650 cell growth,inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. IC50:70nM(NCI-H1650 cell growth)[1] In vitro: Naquotinib selectively inhibited phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects were only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibited cell growth with an IC50 value of 70nM while other EGFR-TKIs were only partially effective. ERK and Akt phosphorylation were diminished after Naquotinib treatment at 1000nM, however, other EGFR-TKIs only partially reduced the phosphorylation levels of these proteins. Naquotinib potently enhanced the caspase activity in NCI-H1650 after 24h treatment, which is concordant with signal and cell growth inhibitory effect.[1] In vivo: In mouse xenograft studies, Naquotinib induced tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models by repeated oral dosing in a dose-dependent manner. Dosing schedules did not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor was achieved after 14-days of Naquotinib treatment. Complete regression was maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment.[2]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT03082300 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-small Cell Lung Cancer (NSCLC)|Epidermal Growth Factor Receptor (EGFR) Mutations March 24, 2017 Phase 1
NCT03042013 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Subjects With NSCLC With an EGFR Activating Mutation February 28, 2017 Phase 2
NCT02500927 Astellas Pharma Inc EGFR-TKI-naïve Patients With NSCLC Harboring EGFR Activating Mutations June 25, 2015 Phase 2
NCT02674555 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Epidermal Growth Factor Receptor (EGFR) Mutations|Solid Tumors August 31, 2016 Phase 1
NCT02192697 Astellas Pharma Inc Non-small Cell Lung Cancer January 23, 2014 Phase 1|Phase 2
NCT02588261 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-small Cell Lung Cancer (NSCLC) February 10, 2016 Phase 3
NCT02113813 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-Small-Cell Lung Cancer (NSCLC)|Epidermal Growth Factor Receptor Mutations April 23, 2014 Phase 1
NCT03082300 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-small Cell Lung Cancer (NSCLC)|Epidermal Growth Factor Receptor (EGFR) Mutations March 24, 2017 Phase 1
NCT03042013 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Subjects With NSCLC With an EGFR Activating Mutation February 28, 2017 Phase 2
NCT02500927 Astellas Pharma Inc EGFR-TKI-naïve Patients With NSCLC Harboring EGFR Activating Mutations June 25, 2015 Phase 2
NCT02674555 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Epidermal Growth Factor Receptor (EGFR) Mutations|Solid Tumors August 31, 2016 Phase 1
NCT02192697 Astellas Pharma Inc Non-small Cell Lung Cancer January 23, 2014 Phase 1|Phase 2
NCT02588261 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-small Cell Lung Cancer (NSCLC) February 10, 2016 Phase 3
NCT02113813 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Non-Small-Cell Lung Cancer (NSCLC)|Epidermal Growth Factor Receptor Mutations April 23, 2014 Phase 1
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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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