[CAS NO. 1448237-05-5] Naquotinibmesylate

Name: Naquotinibmesylate
Brand: Arctom Scientific
SKU: AS938856

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PRODUCTS SPECIFICATIONS [1448237-05-5]

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Catalog

AS938856

Brand

Arctom Scientific

CAS

1448237-05-5

DESCRIPTION [1448237-05-5]

Overview

MDL	MFCD30496702
Molecular Weight	658.81
Molecular Formula	C31H46N8O6S
SMILES	O=C(C1=NC(CC)=C(O[C@H]2CN(C(C=C)=O)CC2)N=C1NC3=CC=C(N4CCC(N5CCN(C)CC5)CC4)C=C3)N.CS(=O)(O)=O

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC ₅₀ s of 8-33 nM toward EGFR mutants and 230 nM for EGFR .

IC50 & Target

EGFR ^L858R/T790M

EGFR ^L858R

EGFR ^{Exon 19 deletion}

EGFR ^{Exon 19 deletion/T790M}

EGFR

230 nM (IC ₅₀ )

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 IC ₅₀ s 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 IC ₅₀ value of 70nM while other EGFR-TKIs are only partially effective ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02113813	Astellas Pharma Global Development, Inc.\|Astellas Pharma Inc	Non-Small-Cell Lung Cancer (NSCLC)\|Epidermal Growth Factor Receptor Mutations	April 9, 2014	Phase 1
NCT03042013	Astellas Pharma Global Development, Inc.\|Astellas Pharma Inc	Subjects With NSCLC With an EGFR Activating Mutation	February 28, 2017	Phase 2
NCT02192697	Astellas Pharma Inc	Non-small Cell Lung Cancer	January 23, 2014	Phase 1\|Phase 2
NCT02674555	Astellas Pharma Global Development, Inc.\|Astellas Pharma Inc	Epidermal Growth Factor Receptor (EGFR) Mutations\|Solid Tumors	November 15, 2016	Phase 1
NCT02588261	Astellas Pharma Global Development, Inc.\|Astellas Pharma Inc	Non-small Cell Lung Cancer (NSCLC)	February 11, 2016	Phase 3
NCT02500927	Astellas Pharma Inc	EGFR-TKI-naïve Patients With NSCLC Harboring EGFR Activating Mutations	June 25, 2015	Phase 2
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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2 mg/mL (3.04 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2 mg/mL (3.04 mM); Clear solution

* All of the co-solvents are available by MCE.