Naquotinib

SKU: orb1296210

Description

Naquotinib

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1448232-80-1
• MW: 562.71
• Purity: 97.49%
• Formula: C₃₀H₄₂N₈O₃
• SMILES: CCc1nc(C(N)=O)c(Nc2ccc(cc2)N2CCC(CC2)N2CCN(C)CC2)nc1O[C@@H]1CCN(C1)C(=O)C=C
• Target: EGFR
• Solubility: Ethanol:80 mg/mL (142.17 mM);H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.55 mM);DMSO:40 mg/mL (71.08 mM)

Bioactivity

• Target IC50:
  EGFR (mutants):8-33 nM |EGFR:230 nM
• In Vivo:
  In NCI-H1975 (L858R/T790M), HCC827 (del ex19), and PC-9 (del ex19) xenograft models, oral administration of Naquotinib results in dose-dependent tumor regression, with the dosing schedules having no impact on its efficacy. Specifically, in an NCI-H1975 xenograft model, Naquotinib leads to complete tumor regression after a 14-day treatment period. Remarkably, 50% of the mice maintain complete regression for over 85 days following the cessation of Naquotinib treatment .
• In Vitro:
  In studies utilizing cells inherently dependent on EGFR, Naquotinib effectively hinders the proliferation of various cancer cell lines, including PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M), and PC-9ER(del ex19/T790M), demonstrating IC50 values ranging from 8 to 33 nM . It specifically targets and suppresses the phosphorylation of EGFR along with the subsequent activation of the ERK and Akt signaling pathways, starting at concentrations as low as 10nM in HCC827 and NCI-H1975 cells. However, this effect requires a much higher concentration of 1000nM in A431 cells. Notably, in NCI-H1650 (del ex19) cells, Naquotinib significantly curtails cell growth with an IC50 value of 70nM, showing its efficacy where other EGFR-TKIs have limited effectiveness .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ASP 8273, ASP8273, ASP-8273, Naquotinib, inhibit, Inhibitor, HER1, ErbB-1, Epidermal growth factor receptor, EGFR, EGFR (mutant)

Compound Identifiers

PubChem CID

71667668