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CAS No.: 181223-80-3

DEL-22379 inhibits ERK dimerization with IC50 of 0.5 μM.

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400-920-2911

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靶点 ERK

IC50:0.5μM
描述The extracellular regulated protein kinases (ERK) play important roles in regulating cellular proliferation and survival. DEL-22379 is a small molecule inhibitor of ERK dimerization with an IC50 value of ~0.5μM. It inhibited ERK dimerization in DLD1 (KRAS mutant), RKO (BRAF mutant) and T47D (WT/WT) cell lines at concentrations of 0.1-10μM. Treatment with DEL-22379 (10μM) for 12 h induced apoptosis in tumor cell lines harboring oncogenic RAS or BRAF. In mouse xenograft models, the treatment with DEL-22379 (15mg/kg/day) for 15 days significantly inhibited the progression of tumors derived from A375 cells (BRAF mutant) but not in mice injected with CHL cells (WT/WT). In a mouse model of BRAF mutant colorectal cancer patient-derived xenograft, the treatment with DEL-22379 (15mg/kg/day) for 21 days markedly suppressed tumor growth compared to the control group^[2].
作用机制DEL-22379 inhibits ERK dimerization by binding to ERK2 within the dimerization interface^[2].
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技术信息

CAS号

181223-80-3

储存条件

分子式

C26H28N4O3

运输

蓝冰

分子量

444.53

别名

溶解度

动物实验配方

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