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  • AD80
    • AD 80
    货号: abs814470
    CAS号: 1384071-99-1
    分子式: C22H19F4N7
    分子量: 473.43
    产品说明书
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    货号-规格 货期 价格 数量
    abs814470-5mg 1-2周 ¥2252.00
    - +
    abs814470-25mg 1-2周 ¥7819.00
    - +
    大包装询价
    产品描述
    描述

    AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.

    纯度
    >98%
    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.
    基本信息
    别名
    AD 80
    外观
    Powder
    可溶性/溶解性
    DMSO : ≥ 150 mg/mL (316.84 mM)
    生物活性
    靶点
    RET,RAF,RC,S6K
    In vitro(体外研究)
    AD80 prevents the phosphorylation of RET as well as of extracellular signa-regulated kinase (ERK), AKT, and S6K at low nanomolar concentrations in kinesin family member 5B (KIF5B)-RET-expressing Ba/F3 cells. Treatment with AD80 results in up-regulation of genes that are typically repressed by active KRAS. On the contrary, genes that are activated by KRAS were down-regulated[1]. On the basis of in vitro human kinase profiles, AD80 and AD81 inhibit RET, RAF, SRC and S6K, with greatly reduced mTOR activity relative to AD57 and AD58. AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis.
    In vivo(体内研究)
    AD80 is a highly potent RET inhibitor with a favorable pharmacokinetic profile in clinically relevant RET fusion-driven tumor models. AD80 potently shrinks RET-rearranged tumors in patient-derived xenografts. A pronounced reduction in phosphorylation of RET as well as AKT and ERK in tumors treated with AD80 (25 mg/kg) is observed but not in tumors treated with cabozantinib or vandetanib.
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