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

Naquotinib mesylate (Synonyms: ASP8273 (mesylate))

Cat. No.: HY-19803 Purity: 98.19%
Handling Instructions

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.

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 USD 174 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 200 In-stock
Estimated Time of Arrival: December 31
25 mg USD 400 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Naquotinib mesylate:

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Description

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.

IC50 & Target[1]

EGFRL858R/T790M

 

EGFRL858R

 

EGFRExon 19 deletion

 

EGFRExon 19 deletion/T790M

 

EGFR

230 nM (IC50)

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 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
Molecular Weight

658.81

Formula

C₃₁H₄₆N₈O₆S

CAS No.

1448237-05-5

SMILES

O=C(C1=NC(CC)=C(O[[email protected]]2CN(C(C=C)=O)CC2)N=C1NC3=CC=C(N4CCC(N5CCN(C)CC5)CC4)C=C3)N.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (18.97 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5179 mL 7.5894 mL 15.1789 mL
5 mM 0.3036 mL 1.5179 mL 3.0358 mL
10 mM 0.1518 mL 0.7589 mL 1.5179 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
Naquotinib mesylate
Cat. No.:
HY-19803
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