Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 43.00 | |
2 mg | In stock | $ 61.00 | |
5 mg | In stock | $ 98.00 | |
50 mg | In stock | Inquiry | |
1 mL * 10 mM (in DMSO) | In stock | $ 135.00 |
Description | Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR. |
Targets&IC50 | EGFR:230 nM, EGFR mutants:8-33 nM |
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 downstream 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 | In NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models, oral Naquotinib treatment dose-dependently induces tumor regression. Dosing schedules do 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]. |
Synonyms | ASP8273 |
Molecular Weight | 562.71 |
Formula | C30H42N8O3 |
CAS No. | 1448232-80-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
H2O: Insoluble
Ethanol: 80 mg/mL (142.16 mM)
DMSO: 40 mg/mL (71.08 mM)
You can also refer to dose conversion for different animals. More
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Naquotinib 1448232-80-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Epidermal growth factor receptor HER1 ErbB-1 ASP-8273 inhibit ASP8273 ASP 8273 Inhibitor inhibitor