VX-11e又称为TCS ERK 11e,是一种有效的、选择性ERK抑制剂,抑制BRAFV600E突变的黑素瘤细胞,平均GI50值为0.77 μM,并有效抑制HT29细胞增殖,IC50值为48 nM。在大鼠和小鼠中,VX-11e表现出良好的口服生物活性。在负荷人黑色素瘤RPDX肿瘤的NSG小鼠中,VX-11e导致pRSK被强烈抑制,并抑制肿瘤生长。与BKM120联合使用时,VX-11e抑制肿瘤生长的作用显著提高。
参考文献
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冰袋运输。粉末直接保存于-20℃,有效期2年。溶于DMSO。建议分装后-20℃避光保存,避免反复冻融。