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Naquotinib mesylate
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Catalog No. T12175Cas No. 1448237-05-5
Alias ASP8273 (mesylate)
Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).
Naquotinib mesylate
😃Good
Catalog No. T12175Alias ASP8273 (mesylate)Cas No. 1448237-05-5
Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $58 | 5 days |
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Product Introduction
Bioactivity
Chemical Properties
| Description | Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR). |
| Targets&IC50 | EGFR:230 nM |
| In vitro | In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective.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[2]. |
| In vivo | 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]. |
| Alias | ASP8273 (mesylate) |
| Molecular Weight | 658.81 |
| Formula | C31H46N8O6S |
| Cas No. | 1448237-05-5 |
| Smiles | CS(O)(=O)=O.CCc1nc(C(N)=O)c(Nc2ccc(cc2)N2CCC(CC2)N2CCN(C)CC2)nc1O[C@@H]1CCN(C1)C(=O)C=C |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 12.5 mg/mL (18.97 mM), Sonication and heating are recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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