TAK-285
更新时间：2024-07-15 12:37:13
采购访问：25次
| 常用名 | TAK 285 | CAS号 | 871026-44-7 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
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℃ |
上海化源生化科技有限公司
认证状态：已认证供应商
商品数：396719件
电话：13311869306
地址：上海市普陀区金沙江路1759号圣诺亚大厦B座508室
地区： 上海市 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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- 上海化源生化科技有限公司
- 上海市 上海市 普陀区
- 产品名：TAK-285
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
- 上海脉铂医药科技有限公司
- 上海市 上海市 嘉定区
- 产品名：TAK-285
- 价格： ￥3279.0/10mg ￥1879.0/5mg ￥2639.0/1g ￥需询单/1g
- 纯度：98.0%
- 备货期：2天
- 联系人：李先生
- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：TAK-285
- 价格： ￥2265.9/10mg ￥402.9/1mg ￥1338.9/5mg ￥4531.9/25mg
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
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参考价格：$318/10mM*1mLinDMSO