产品
编 号：F751525
分子式：C31H31FN8O3
分子量：582.63
分子式：C31H31FN8O3
分子量：582.63
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2364326-23-6
产品详情
生物活性：
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer.
体内研究：
SPH5030 (5-40 mg/kg; p.o. once per day for 13 or 21 days) shows in vivo antitumor efficacy in mice with xenograft tumor models.1.19Pharmacokinetic Properties of SPH5030 in Mice and Rats.MiceIV 3 mg/kg MicePO 10 mg/kgRatsIV 3 mg/kg RatsPO 6 mg/kg
CL (L/kg·h)0.70±0.200.78±0.13
t1/2 (h)3.76±0.153.60±0.594.56±0.204.38±0.35
Vss (L/kg)2.96±0.96 3.55±0.64
Cmax (μg/mL) 1.90±0.14 0.76±0.33
tmax (h) 2.67±1.15 3.33±1.15
AUC0-t (h·μg/mL) 13.07±0.48 5.47±2.82
F (%) 87.66 71.35
Animal Model:BALB/c nude mouse with NCI-N87 and BT474 xenografts, and NPSG mouse with BAF3 HER2 A775_G776insYVMA xenografts
Dosage:5, 10, 20 and 40 mg/kg
Administration:Oral gavage; 5-40 mg/kg once per day; for 13 or 21 days
Result:Dose-dependently inhibited tumor growth in NCI-N87, BT474 and BAF3 HER2 A775_G776insYVMA xenograft mouse models, and showed an equivalent or better activity of tumor inhibition compared with neratinib and pyrotinib at a dose of 20 mg/kg. Showed no mortality or significant loss of body weight in xenograft mouse models.
体外研究：
SPH5030 (0-10 μM; 72 h) shows anti-proliferation activities against tumor cell lines.
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer.
体内研究：
SPH5030 (5-40 mg/kg; p.o. once per day for 13 or 21 days) shows in vivo antitumor efficacy in mice with xenograft tumor models.1.19Pharmacokinetic Properties of SPH5030 in Mice and Rats.MiceIV 3 mg/kg MicePO 10 mg/kgRatsIV 3 mg/kg RatsPO 6 mg/kg
CL (L/kg·h)0.70±0.200.78±0.13
t1/2 (h)3.76±0.153.60±0.594.56±0.204.38±0.35
Vss (L/kg)2.96±0.96 3.55±0.64
Cmax (μg/mL) 1.90±0.14 0.76±0.33
tmax (h) 2.67±1.15 3.33±1.15
AUC0-t (h·μg/mL) 13.07±0.48 5.47±2.82
F (%) 87.66 71.35
Animal Model:BALB/c nude mouse with NCI-N87 and BT474 xenografts, and NPSG mouse with BAF3 HER2 A775_G776insYVMA xenografts
Dosage:5, 10, 20 and 40 mg/kg
Administration:Oral gavage; 5-40 mg/kg once per day; for 13 or 21 days
Result:Dose-dependently inhibited tumor growth in NCI-N87, BT474 and BAF3 HER2 A775_G776insYVMA xenograft mouse models, and showed an equivalent or better activity of tumor inhibition compared with neratinib and pyrotinib at a dose of 20 mg/kg. Showed no mortality or significant loss of body weight in xenograft mouse models.
体外研究：
SPH5030 (0-10 μM; 72 h) shows anti-proliferation activities against tumor cell lines.
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