Naquotinib mesylate- CAS 1448237-05-5

CAS No.: 1448237-05-5

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Naquotinib mesylate,1448237-05-5
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I001730
Molecular Formula:

C31H46N8O6S

Molecular Weight:658.81
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.
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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]

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