CCT241161

A multi-kinase inhibitor

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库存: 现货

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包装

价格

促销价

数量
500ug

￥1087.00

870.00

- +
1mg

￥2037.00

1630.00

- +
5mg

￥8012.00

6410.00

- +
10mg

￥13750.00

11000.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

CCT241161 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 252, 15, 6, 15, and 3 nM, respectively). It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 µM. CCT241161 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner. In vivo, CCT241161 (20 mg/kg per day) induces tumor regression in a B-RAF mutant A375 mouse xenograft model. CCT241161 also inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant patient-derived xenograft (PDX) mouse models including those resistant to both dabrafenib and trametinib .