TAK-733CAS号: 1035555-63-5分子式: C17H15F2IN4O4分子量: 504.23描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
产品描述 | |
描述 |
TAK-733是一种有效的,选择性的MEK变构抑制剂,作用于MEK1,IC50为3.2 nM,抑制Abl1, AKT3, c-RAF, CamK1, CDK2及c-Met等活性。 |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO :93 mg/mL (184.4 mM)
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生物活性 | |
靶点 |
MEK1
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In vitro(体外研究) |
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.
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In vivo(体内研究) |
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. TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg.
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参考文献 | |
参考文献 |
BRAF L597 mutations in melanoma are associated with sensitivity to MEK inhibitors.
Dahlmanet al. Cancer Discov. 2012 Jul 13. PMID: 22798288. 䔸Żᩄ 族痛셌Ų 族痛셌Ų Item 褐 Count ๏ 趌๐ 侮靴 ᠠi S ñ ñ 眘⮦眀⮦敲痛๏ࠃ 馸鳘祖Item ǁdž Count 洣盜᬴叫㺍痭ᠠ靴i 縉 靴蘿敌ଧ靴ᠠi ᭰叫㺍痭ᡸ顴먲ନ魈 鸤�ଭ鶔 |
分子结构图