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 .In VitroIn 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoOral 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:EGFR L858R/T790M EGFR L858R EGFR Exon 19 deletion EGFR Exon 19 deletion/T790M EGFR 230 nM (IC 50 ). Specification: 0.98 Molecular Formula: C31H46N8O6S Molecular Weight: 658.81 PubChem CID: 92135932 Isomeric SMILES: CCC1=C(N=C(C(=N1)C(=O)N)NC2=CC=C(C=C2)N3CCC(CC3)N4CCN(CC4)C)O[C@@H]5CCN(C5)C(=O)C=C.CS(=O)(=O)O
- UPC:
- 51142310
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- N647327-25mg
- CAS:
- 1448237-05-5
- Product Size:
- 25mg
