TAK-733は、強力な、選択的な、ATP-非競争的MEKアロステリック部位阻害剤で、IC50 が 3.2nMです。

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TAK-733 化学構造
分子量: 504.23



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情報 TAK-733は、強力な、選択的な、ATP-非競争的MEKアロステリック部位阻害剤で、IC50 が 3.2nMです。
目標 MEK1
IC50 3.2 nM [1]
In vitro試験 TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. [1]
In vivo試験 TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. [1] TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. [2]
臨床試験 A Multicenter, Open-label, Dose-escalation, Phase I Study of TAK-733, an Oral MEK Inhibitor, in Adult Patients With Advanced Nonhematologic Malignancies.

推薦された実験操作 (公開の文献だけ)

動物実験: [2]

動物モデル Human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]) Pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice.
製剤 Saline
投薬量 10 mg/kg
管理 Orally administrated once daily for 21 days



Download TAK-733 SDF
分子量 504.23


CAS No. 1035555-63-5
別名 N/A
溶解度 (25°C)
  • DMSO 101 mg/mL
  • 水 <1 mg/mL
  • エタノール <1 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 (R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione


カスタマーレビュー (3)

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Source Jonas Nilsson, PhD from University of Gothenburg. TAK-733 purchased from Selleck
Method Western blot, cell apoptosis assays
Cell Lines Mouse carcinoma cells
Concentrations 1-1000 nM
Incubation Time 16/40 h
Results (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10 nM, GSK1120212=<1 nM.

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Source , , Dr.Wang from Southern Medical Hospital . TAK-733 purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-10 uM
Incubation Time 2 h
Results Effect of MEK inhibitor TAK-733 in A549 cells. A549 cells were incubated with increasing concentrations of TAK-733 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.

Click to enlarge
Source Dr. Zhang of Tianjin Medical University. TAK-733 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations 0-10 μM
Incubation Time 3 h
Results Reduction of ERK1/2 phosphorylation in T47D cells treated with TAK-733 was observed.



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