apexbio.B5953-5 Dovitinib (TKI258) Lactate 5mg

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货品编号：apexbio.B5953-5

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品牌：APEXBIO
所属分类：工具酶

货品编号：  apexbio.B5953-5       品       牌：  <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); cursor: text; font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 400; letter-spacing: normal; orphans: 2; overflow-wrap: break-word; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">apexbio      品       名：  <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); cursor: text; font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 400; letter-spacing: normal; orphans: 2; overflow-wrap: break-word; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">Dovitinib (TKI258) Lactate        规       格：  <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); cursor: text; font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 400; letter-spacing: normal; orphans: 2; overflow-wrap: break-word; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">5mg             产品描述：      Background <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     Dovitinib (TKI258) Lactate对FGFR1–3的IC50值约为10 nmol/L. <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     在约10%的乳腺癌中,观察到成纤维细胞生长因子受体1(FGFR1)与FGFR2扩增,此现象与乳腺癌不良预后相关.Dovitinib(TKI258)<span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     是一种口服的酪氨酸激酶抑制剂(TKI),作用于FGFR1-3\VEGFR1-3和血小板衍生生长因子受体(PDGFR). <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     体外:在FGFR1与FGFR2扩增的细胞系中,Dovitinib呈剂量依赖性地降低pFRS2和pERK/MAPK的浓度.在MDA-MB-134细胞与SUM52<span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     细胞中,Dovitinib对细胞生长抑制的IC50值分别为190 nmol/L和180 nmol/L.相反地,在无FGFR1和FGFR2扩增的11种乳腺癌细胞系中,<span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     Dovitinib的IC50值均大于2,000 nmol/L[1]. <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     体内:在体内模型(携带8个FGFR1基因拷贝的HBCx-2乳腺癌原代细胞异种移植模型)中,30 mg/kg Dovitinib抑制肿瘤生长,50 mg/kg <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     Dovitinib使肿瘤消退.此外,在HBCx-3细胞异种移植模型中,给予40 mg/kg Dovitinib,每天1次,持续35天,可以使肿瘤消退[1]. <span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     临床试验:共81例患者入组.在5例FGFR1扩增/HR阳性乳腺癌患者与1例FGFR1非扩增/HR阳性乳腺癌患者中,观察到持续6个月以上的<span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     未确定反应或病情稳定.使用qPCR鉴定FGFR1\FGFR2或FGF3扩增,基于不同的FGF扩增,对HR阳性乳腺癌患者进行分组.相对于非FGF<span style="display: inline !important; float: none; background-color: rgb(255, 255, 255); color: rgb(0, 0, 0); font-family: Arial,Verdana,sans-serif; font-size: 12px; font-style: normal; font-variant: normal; font-weight: 700; letter-spacing: normal; orphans: 2; text-align: left; text-decoration: none; text-indent: 0px; text-transform: none; -webkit-text-stroke-width: 0px; white-space: normal; word-spacing: 0px;">     途径扩增的乳腺癌患者(目标病灶增加了12.0%),FGF途径扩增的乳腺癌患者目标病灶平均减少了21.1%[1].

apexbio.B5953-5 Dovitinib (TKI258) Lactate 5mg

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