keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 37,500 | |||
5 mg | 在庫あり | ¥ 95,000 | |||
10 mg | 在庫あり | ¥ 142,000 | |||
25 mg | 在庫あり | ¥ 226,000 | |||
50 mg | 在庫あり | ¥ 305,500 | |||
100 mg | 在庫あり | ¥ 411,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 104,500 |
説明 | Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer. |
In vitro | Oritinib (0.001, 0.01, 0.1, 1, and 10 μM) selectively inhibits EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50s of 3.932, 9.39 and 7.63 nM, respectively. Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells[1]. |
In vivo | In female mice bearing NCI-H1975 and A431 xenograft models, Oritinib (2.5, 5, and 15 mg/kg; oral) significantly inhibits proliferation of tumor cells with no TKI-induced weight loss. In NCI-H1975 tumor-bearing mice, Oritinib (2.5, 5, and 15 mg/kg; oral) shows good bioavailability(Tmax = 1.5-2 h) and extensive distribution from the plasma to the tissues. The AUC0–t values in plasma are 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively[1]. |
別名 | SH-1028 |
分子量 | 539.67 |
分子式 | C31H37N7O2 |
CAS No. | 2035089-28-0 |
keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (222.36 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Oritinib 2035089-28-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR pharmacodynamics non-small cell lung cancer EGFR-T790M EGFR TKI Irreversible mutant-selective SH1028 HER1 inhibit SH-1028 Inhibitor Epidermal growth factor receptor SH 1028 ErbB-1 third-generation inhibitor