TAK-285

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更新时间： 2025-08-29 12:24:23

CAS号：871026-44-7

常用名： TAK 285

价格：

纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. IC50 value: 17/23 nM (HER2/1) [1]Target: HER1/2in vitro: MEK1, MEK5, c-Met, Aurora B, Lck, CSK, and Lyn B with IC50 of 1.1 μM, 5.7 μM, 4.2 μM, 1.7 μM, 2.4 μM, 4.7 μM, and 5.2 μM, respectively, and displays no activity against other kinases with IC50 of >10 μM. TAK-285 shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM [1]. Compared with SYR127063 a potent inhibitor of HER2, TAK-285 displays similar in vitro potency against HER2 and EGFR. Compared with the full cytoplasmic domains of the wild-type proteins, the mutations and shortened boundaries used for structure determination of HER2-KD and EGFR-KD do not significantly change the inhibitory activity (IC50) of TAK-285. TAK-285 binds to the inactive conformation of EGFR, and shows a similar binding mode with lapatinib in the active site [2]. in vivo: The oral bioavailability of TAK-285 is 97.7% in rats and 72.2% in mice at a dose of 50 mg/kg. Oral administration of TAK-285 at 100 mg/kg twice daily for 14 days displays significant antitumor efficacy in the HER2-overexpressing BT-474 tumor xenograft mouse model with tumor/control (T/C) ratio of 29%, without affecting body weight. Similar to the BT-474 model, TAK-285 exhibits dose-dependent tumor growth inhibition of 4-1ST (HER2-overexpressing human gastric cancer tumor) xenografts in mice, with T/C of 44% and 11% at doses of 50 mg/kg and 100 mg/kg, twice daily, respectively, without significant body weight loss in mice [1]. After oral administration of TAK-285, a significant amount of TAK-285 is present in the brain of rats in pharmacologically active, unbound form (approximately 20% of its free plasma level), indicating that TAK-285 has a potential in the therapy of CNS malignancies/metastases [3]. 物理化学性质： CAS号：871026-44-7 常用中文名：TAK 285 常用英文名：TAK-285 分子式：C26H25ClF3N5O3 分子量：547.957 密度：1.4±0.1 g/cm3 沸点：705.5±60.0 °C at 760 mmHg 熔点：167-169℃ 闪点：380.4±32.9 °C 储存条件：-20℃

供应商信息：

公司名：上海化源世纪贸易有限公司推荐

认证状态： 已认证供应商

商品数： 396716件

电话： 53555033

地址： 上海市普陀区金沙江路1759号圣诺亚大厦B座

地区： 上海市普陀区

联系人： 徐经理

联系人电话： 13311869306

邮件：xuqm@chemsrc.com

网址：http://www.chemsrc.com

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公司介绍：
化源网，2015 年正式成立，是专注服务全球精细化学与生物医药研发领域的专业社群电商平台。
平台严选优质品牌商家直供，以正品低价为核心优势，搭配简洁易操作的商城界面，为研发人员提供一站式采购方案，全程保障高效便捷的服务体验。

其他供应商价格：

2022-03-04 价格：￥2265.9 TAK-285

2021-02-06 价格：￥3279.0 TAK-285

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TAK 285价格

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