Naquotinib mesylate - ≥98% , CAS No.1448237-05-5

CAS: 1448237-05-5 Cat. No.: N647327 Formule: C₃₁H₄₆N₈O₆S Poids moléculaire: 658.81 PubChem CID: 92135932

GRADE & PURITY ≥98%

Storage

Store at 2-8°C,Desiccated

Shipped In

Wet ice

Vue d’ensemble

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

Form:Solid

IC50& Target:EGFR L858R/T790M EGFR L858R EGFR Exon 19 deletion EGFR Exon 19 deletion/T790M EGFR 230 nM (IC 50 )

Specifications

Spécifications et pureté

≥98%

Mécanismes biochimiques et physiologiques

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 .

Conditions de stockage de stockage

Store at 2-8°C,Desiccated

Expédié en

Wet ice

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Pureté

≥98%

Noms et identifiants

• Isomères 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
• PubChem CID: 92135932
• Poids moléculaire: 658.81

Propriétés chimiques et physiques

• Solubilité: DMSO : 12.5 mg/mL (18.97 mM; Need ultrasonic and warming)
• Poids moléculaire: 658.800 g/mol
• Hydrogen Bond Donor Count: 3
• Hydrogen Bond Acceptor Count: 12
• Rotatable Bond Count: 9
• Exact Mass: 658.326 Da
• Monoisotopic Mass: 658.326 Da
• Topological Polar Surface Area: 183.000 Ų
• Heavy Atom Count: 46
• Formal Charge: 0
• Complexity: 976.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 1
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 2

XLogP3