S80044
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- 公司名稱 上海源葉生物科技有限公司
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- 更新時間 2024/7/3 19:14:59
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- 產(chǎn)品描述： TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
- 靶點： MEK:3.2 nM (IC50)
- 體內(nèi)研究： The pharmacokinetics of TAK-733 is evaluated in nude mouse, rat, dog and monkey. Low clearance and high oral bioavailability are observed in all species. TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. Daily oral administration of 1, 3, 10, and 30 mg/kg of TAK-733 for 14 days (Days 10 to 23) results in tumor growth delay in the A375 cell-implanted mice (5/group). TAK-733 (35, 70, 100, and 160 mg/kg) also significantly inhibits tumor growth on an intermittent dosing schedule of 3 days per week for 2 weeks (Days 10, 13, 15, 17, 20, and 22). Three partial regressions (PR), a 60% response rate, are observed in mice administered with 30 mg/kg of TAK-733 daily and in mice administered with 160 mg/kg of TAK-733 intermittently. Responses, CR (complete regression) and partial regressions (PR) are also observed in mice administered with 70, 100, and 160 mg/kg of TAK-733 intermittently. The tumor regression rate is more pronounced with the intermittent administration regimen; the greatest reduction in tumor volume is observed at 160 mg/kg (57.29%), versus a maximum reduction of 46.97% at 30 mg/kg once daily. By the last day of administration, tumor growth is significantly (p<0.05 for="" %t/c,="" student's="" t-test)="" inhibited="" in="" mice="" administered="" 3,="" 10,="" and="" 30="" mg/kg="" once="" daily="" or="" 35,="" 70,="" 100,="" and="" 160="" mg/kg="" intermittently="">
- 參考文獻：
1. Dong Q, et al. Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9. 2. Micel LN, et al. Antitumor activity of the MEK inhibitor TAK-733 against melanoma cell lines and patient-derived tumor explants. Mol Cancer Ther. 2015 Feb;14(2):317-25.
- 溶解度： Soluble in DMSO
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 1.983 ml 9.916 ml 19.832 ml 5 mM 0.397 ml 1.983 ml 3.966 ml 10 mM 0.198 ml 0.992 ml 1.983 ml 50 mM 0.04 ml 0.198 ml 0.397 ml
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