产品
编 号：F741339
分子式：C31H37N7O2
分子量：539.67
分子式：C31H37N7O2
分子量：539.67
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2035089-28-0
产品详情
生物活性：
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
体内研究：
Oral administration of Oritinib at a daily dose of 5 mg/kg significantly inhibits proliferation of tumor cells with EGFR sensitive mutation (exon 19 del) and resistant mutation (T790 M) for consecutive 14 days, with no TKI-induced weight loss in mouse xenograft models. Oritinib shows good bioavailability, and is distributed extensively from the plasma to the tissues.Animal Model:6-8 weeks old female mice bearing NCI-H1975 and A431 xenograft models
Dosage:2.5, 5, and 15 mg/kg
Administration:Orally administrated once daily for consecutive 14 days
Result:Led to a significant inhibition of tumor cell growth in both PC-9 (exon 19 del) and NCI-H1975 (L858R/T790M) xenograft models.
Animal Model:NCI-H1975 tumor-bearing mice
Dosage:2.5, 5, and 15 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration for 1 day or 14 consecutive days.
Result:The Tmax is 1.5-2 h, indicating rapidly distributed into tissues, including lung tumor tissues. The AUC0–t values in plasma were 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively.
体外研究：
Oritinib (SH-1028) binds irreversibly to EGFR kinase by targeting cysteine-797 residue in the ATP binding site via covalent bond formation.Oritinib (0.001-10 μM) potently and selectively targets mutant EGFR cell lines in vitro.Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells at lower concentrations or even drug-free for at least 6 h.
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
体内研究：
Oral administration of Oritinib at a daily dose of 5 mg/kg significantly inhibits proliferation of tumor cells with EGFR sensitive mutation (exon 19 del) and resistant mutation (T790 M) for consecutive 14 days, with no TKI-induced weight loss in mouse xenograft models. Oritinib shows good bioavailability, and is distributed extensively from the plasma to the tissues.Animal Model:6-8 weeks old female mice bearing NCI-H1975 and A431 xenograft models
Dosage:2.5, 5, and 15 mg/kg
Administration:Orally administrated once daily for consecutive 14 days
Result:Led to a significant inhibition of tumor cell growth in both PC-9 (exon 19 del) and NCI-H1975 (L858R/T790M) xenograft models.
Animal Model:NCI-H1975 tumor-bearing mice
Dosage:2.5, 5, and 15 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration for 1 day or 14 consecutive days.
Result:The Tmax is 1.5-2 h, indicating rapidly distributed into tissues, including lung tumor tissues. The AUC0–t values in plasma were 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively.
体外研究：
Oritinib (SH-1028) binds irreversibly to EGFR kinase by targeting cysteine-797 residue in the ATP binding site via covalent bond formation.Oritinib (0.001-10 μM) potently and selectively targets mutant EGFR cell lines in vitro.Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells at lower concentrations or even drug-free for at least 6 h.
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