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Naquotinib

Product Name: Naquotinib
CAS No.: 1448232-80-1
Chemical Name: Naquotinib
Synonyms: ASP-8273;Naquotinib;Naquotinib,ASP-8273;ASP8273 (Naquotinib);NAQUOTINIB (FREE BASE);Naquotinib, 10 mM in DMSO;Epidermal growth factor receptor,EGFR,ASP 8273,HER1,ErbB-1,ASP-8273,inhibit,Naquotinib,Inhibitor;(R)-5-((1-acryloylpyrrolidin-3-yl)oxy)-6-ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrazine-2-carboxamide;6-Ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-2-pyrazinecarboxamide;2-Pyrazinecarboxamide, 6-ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-
CBNumber: CB53062789
Molecular Formula: C30H42N8O3
Formula Weight: 562.71
MOL File: 1448232-80-1.mol

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Naquotinib Property

Boiling point:: 717.6±60.0 °C(Predicted)
Density: 1.248±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMF: 30mg/ml; DMSO: 2 mg/ml; Ethanol: 30mg/ml
form: A crystalline solid
pka: 14.10±0.50(Predicted)
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23498
Product name: Naquotinib
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 23498
Product name: Naquotinib
Purity: ≥98%
Packaging: 5mg
Price: $151
Updated: 2024/03/01

Cayman Chemical

Product number: 23498
Product name: Naquotinib
Purity: ≥98%
Packaging: 10mg
Price: $278
Updated: 2024/03/01

TRC

Product number: N378710
Product name: Naquotinib
Packaging: 1mg
Price: $80
Updated: 2021/12/16

AK Scientific

Product number: 0883DV
Product name: Naquotinib
Packaging: 5mg
Price: $266
Updated: 2021/12/16

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Naquotinib Chemical Properties,Usage,Production

Uses

Naquotinib is an epidermal growth factor receptor (EGFR) inhibitor.

Biological Activity

Naquotinib (ASP8273) is an orally active, irreversible, mutant-selective epidermal growth factor receptor (EGFR) inhibitor with potential antitumor activity.

in vitro

ASP8273 is an irreversible TKI small molecule inhibitor that inhibits the kinase activity of EGFR mutants including T97M with limited activity against wild-type EGFR. In in vitro enzymatic activity and cellular assays, ASP8273 covalently bound to an EGFR mutant (L858R/T790M) through cysteine residues and long-term inhibited EGFR phosphorylation for 24 hours. In NSCLC cell lines with the above-mentioned EGFR mutations, ASP8273 has IC50 values in the range of 8-33 nM for EGFR mutants, more potent than WT EGFR (IC50 for WT EGFR is 230 nM).

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].

target

Target	Value
mutant EGFR

IC 50

EGFR: 230 nM (IC₅₀); EGFR^T790M; EGFR^L858R/T790M; EGFR^L858R; EGFR^{Exon 19 deletion/T790M}

Naquotinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Naquotinib Suppliers

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1448232-80-1, NaquotinibRelated Search:

Naquotinib

ASP-8273

6-Ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-2-pyrazinecarboxamide

(R)-5-((1-acryloylpyrrolidin-3-yl)oxy)-6-ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrazine-2-carboxamide

Naquotinib,ASP-8273

NAQUOTINIB (FREE BASE)

2-Pyrazinecarboxamide, 6-ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-

Epidermal growth factor receptor,EGFR,ASP 8273,HER1,ErbB-1,ASP-8273,inhibit,Naquotinib,Inhibitor

Naquotinib, 10 mM in DMSO

ASP8273 (Naquotinib)

1448232-80-1

448232-80-1