AZD-3759

    • 货号:MC0949
      • CasNo:
      • 1626387-80-1
      • 分子式:
      • C22H23ClFN5O3
      • 纯度:
      • >98%
      • 靶点:
      • EGFR
      • IC50:
      • IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 nM (EGFRexon 19Del)[1]
      • 体外研究:
      • At 2 mM of ATP concentrations, the IC50s are 102, 7.6, and 2.4 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively. AZD3759 also inhibits pEGFR in H838wt, H3255L858R, and PC-9exon 19Del with IC50 of 64.5, 7.2, and 7.4 nM, respectively. In cellular phosphorylation studies, AZD3759 also demonstrates 9-fold inhibition selectivity in EGFR-activating mutant cell lines over EGFR wild-type cell lines (H838 cell line)[1].
      • 体内研究:
      • Following oral dosing in rats at 2 mg/kg, absorption of AZD3759 is rapid with blood Cmax of 0.58 μM achieved at 1.0 h. Subsequently, blood concentrations of AZD3759 decline monoexponentially with a mean elimination half-life of 4.3 h, which is close to the same parameter obtained from intravenous dosing of 4.1 h. The bioavailability following an oral dose in rats is 91%. Blood pharmacokinetic parameters of AZD3759 in male dogs are determined following both a single dose intravenous infusion and oral administration. Following the IV dose in dogs, AZD3759 blood clearance is determined as 14 mL/min per kg, and the volume of distribution is 6.4 L/kg. Its elimination half-life is 6.2 h. Absorption of AZD3759 is rapid with blood Cmax (698 nM) occurring between 0.5 and 1.5 h. The oral bioavailability of AZD3759 is excellent at 90%. AZD3759 demonstrated significant dose-dependent antitumor efficacy (78% tumor growth inhibition at 7.5 mg/kg qd and tumor regression at 15 mg/kg qd, respectively,
      • 简介:
      • AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 nM (EGFRexon 19Del)[1]
      • 特异性:
      • Target: EGFR . Fields: AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 n
      • 来源:
      • Rabbit
      • 稀释:
      • IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 nM (EGFRexon 19Del)[1]
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • AZD-3759,AZD 3759,,AZD3759
      • 分子量:
      • 459.14
      • 产品图片