交易须知
neratinib产品活性：neratinib 是一种可口服的，不可逆的 tyrosine kinase 抑制剂，能够抑制 her2 和 egfr 的活性，ic50 值分别为 59 nm 和 92 nm。
研究领域：jak/stat signaling | protein tyrosine kinase/rtk
作用靶点：egfr
in vitro: neratinib has inhibition of tyrosine kinases kdr and src with ic50 of 0.8 μm and 1.4 μm, respectively, being 14- and 24-fold less active compared with her2. neratinib displays no activity against other serine-threonine kinases such as akt, cyclin d1/cdk4, cyclin e/cdk2, cyclin b1/cdk1, ikk-2, mk-2, pdk1, c-raf, and tpl-2, as well as the tyrosine kinase c-met. neratinib selectively inhibits the proliferation of 3t3 cells transfected with the her2 (3t3/neu), as well as two other her-2-overexpressing sk-br-3 and bt474 cells with ic50 values of 2-3 nm, displaying > 230-fold potency compared with non-transfected 3t3 cells as well as mda-mb-435 and sw620 which are egfr- and her2-negative. neratinib also inhibits the proliferation of egfr-dependent a431 cells with an ic50 of 81 nm. neratinib reduces her2 receptor autophosphorylation in bt474 cells with an ic50 of 5 nm, and egf-dependent phosphorylation of egfr in a431 cells with ic50 of 3 nm. blocking of her-2 by neratinib results in inhibition of downstream mapk and akt pathways with ic50 of 2 nm, more potently than trastuzumab. neratinib inhibits the cyclin d1 expression and the phosphorylation of the rb-susceptibility gene production in bt474 cells with ic50 of 9 nm, leading to g1-s arrest and ultimately decreased cell proliferation.
in vivo: orally treated neratinib significantly inhibits the growth of 3t3/neu xenografts, with inhibition of 34%, 53%, 98%, and 98% at dose of 10, 20, 40, and 80 mg/kg/day, respectively. consistent with the inhibition of her-2 phosphorylation by 84% within 1 hour of administration at 40 mg/kg/day, neratinib inhibits the growth of bt474 xenografts by 70-82%, 67%, and 93% at dose of 5, 10, and 40 mg/kg/day, respectively. neratinib is also effective against sk-ov-3 xenografts with inhibition of 31% and 85% at 5 and 60 mg/kg/day, respectively. neratinib is less potent against egfr-dependent a431 xenografts than her-2-dependent tumors, with 32% and 44% inhibition at 5 and 20 mg/kg/day, respectively. neratinib displays little activity against mcf-7 and mx-1 xenografts expressing low levels of her-2 and egfr, with only 28% inhibition at 80 mg/kg/day, suggesting that neratinib has selective activity for cells expressing her-2 or egfr.
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