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  1. 首頁 > 小分子化合物 > 信號通路 > MAPK 信號通路 > TAK-733

TAK-733

    
≥96%

TAK-733

源葉(MedMol)
S80044 一鍵復制產(chǎn)品信息
1035555-63-5
C17H15F2IN4O4
504.23
(R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione
貨號 規(guī)格 價格 上海 北京 武漢 南京 購買數(shù)量
S80044-1mg ≥96% ￥142.00 10 - - -
S80044-5mg ≥96% ￥499.00 10 - - -
S80044-10mg ≥96% ￥799.00 9 - - -
S80044-25mg ≥96% ￥1599.00 4 - - -
S80044-50mg ≥96% ￥2727.00 3 - - -
S80044-100mg ≥96% ￥4637.00 2 - - -
產(chǎn)品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產(chǎn)品

產(chǎn)品介紹

TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.

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);MEK
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.
溶解性： 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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參考文獻

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