产品
编 号：F478227
分子式：C23H25ClFN5O3
分子量：473.93
分子式：C23H25ClFN5O3
分子量：473.93
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 848942-61-0
产品详情
生物活性：
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
体内研究：
AZD8931 (6.25-50 mg/kg, p.o.) significantly inhibits BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 is active in xenograft tumor models responsive to EGFR inhibition alone (LoVo and PC-9) or EGFR or erbB2 inhibition (BT474c, Calu-3, and FaDu). AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models. AZD8931 (25 mg/kg, p.o.) significantly inhibits the growth of SUM149 and FC-IBC-02 cells in vivo in SCID mice. AZD8931 displays favorable oral pharmacokinetics in rat and dog (low clearance and good bioavailability) and low human hepatocyte turnover (Clint < 4.5 μL/min/106 cells). In nude mouse after oral administration at 50 mg/kg, AZD8931 shows improved exposure, and at at 100 mg/kg oral dose once daily, it shows potent tumor growth inhibition activity in the LoVo mouse xenograft model.
体外研究：
AZD8931 shows potent inhibitory effect on erbB2 in the ligand-independent MCF-7 cl24 cells, with IC50 of 59 nM. AZD8931 (1 μM) has no significant effect on EGFR expression level, but significantly inhibits phosphorylation of Akt in a time- and dose-dependent manner in both SUM149 and FC-IBC-02 cells. AZD8931 (0.01, 0.1, 1, or 2 μM) inhibits proliferation and induces apoptosis in human IBC cells. At the cellular level, AZD8931 inhibits EGF-stimulated phosphorylation of EGFR in the KB cell line (IC50: 4 nM) and heregulin-stimulated phosphorylation of HER2 (IC50: 3 nM) and HER3 (IC50: 4 nM) in the MCF-7 cell line. However, AZD8931 exhibits no CYP P450 inhibition (IC50 > 10 μM against 1A2, 2C9, 2C19, 2D6, and 3A4).
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
体内研究：
AZD8931 (6.25-50 mg/kg, p.o.) significantly inhibits BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 is active in xenograft tumor models responsive to EGFR inhibition alone (LoVo and PC-9) or EGFR or erbB2 inhibition (BT474c, Calu-3, and FaDu). AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models. AZD8931 (25 mg/kg, p.o.) significantly inhibits the growth of SUM149 and FC-IBC-02 cells in vivo in SCID mice. AZD8931 displays favorable oral pharmacokinetics in rat and dog (low clearance and good bioavailability) and low human hepatocyte turnover (Clint < 4.5 μL/min/106 cells). In nude mouse after oral administration at 50 mg/kg, AZD8931 shows improved exposure, and at at 100 mg/kg oral dose once daily, it shows potent tumor growth inhibition activity in the LoVo mouse xenograft model.
体外研究：
AZD8931 shows potent inhibitory effect on erbB2 in the ligand-independent MCF-7 cl24 cells, with IC50 of 59 nM. AZD8931 (1 μM) has no significant effect on EGFR expression level, but significantly inhibits phosphorylation of Akt in a time- and dose-dependent manner in both SUM149 and FC-IBC-02 cells. AZD8931 (0.01, 0.1, 1, or 2 μM) inhibits proliferation and induces apoptosis in human IBC cells. At the cellular level, AZD8931 inhibits EGF-stimulated phosphorylation of EGFR in the KB cell line (IC50: 4 nM) and heregulin-stimulated phosphorylation of HER2 (IC50: 3 nM) and HER3 (IC50: 4 nM) in the MCF-7 cell line. However, AZD8931 exhibits no CYP P450 inhibition (IC50 > 10 μM against 1A2, 2C9, 2C19, 2D6, and 3A4).
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